Category: imidazoles-derivatives

Epidemiology, treatment patterns and survival of chronic lymphocytic leukaemia/small lymphocytic lymphoma (CLL/SLL) in Taiwan, 2006-2015 was written by Ko, Bor-Sheng;Chen, Li-Ju;Huang, Huai-Hsuan;Chen, Ho-Min;Hsiao, Fei-Yuan. And the article was included in International Journal of Clinical Practice in 2021.Application In Synthesis of 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid The following contents are mentioned in the article:

Chronic lymphocytic leukemia/small lymphocytic lymphoma (CLL/SLL) is one of the most frequent types of leukemia/lymphoma in adults in Western countries. However, there are few studies regarding its epidemiol. and treatment patterns in Asian countries. To investigate CLL/SLL in Asian populations, we identified CLL/SLL patients diagnosed during 2006 to 2015 from the Taiwan Cancer Registry Database and estimated the incidence. Further, patients diagnosed during 2008 to 2015 were included for the anal. of treatment patterns and survivals. Treatments for CLL/SLL were retrieved from the Taiwan’s National Health Insurance Research Database and survival data from the National Death Registry. In total, 1497 patients who were older than 20 years and had newly diagnosed CLL/SLL during 2006-2015 were identified. The age-standardized incidence rates of CLL/SLL (0.36 per 100 000 persons in 2006, and 0.54 in 2015) increased during the 10-yr period. The sex ratio was ranged from 1.21 to 2.63 with male predominant during 2006 and 2015. For the anal. of treatment patterns (n = 1236), 72.8% patients received chemotherapies. The median duration between the diagnosis and start of treatments was 27 days, and monotherapy of chlorambucil, bendamustine or cyclophosphamide was the most common regimen in initial treatments. The median follow-up duration for the patients receiving therapies was 29.6 mo, and 45.0% patients experienced relapse or refractory. In patients with relapse/refractory CLL/SLL, 34.1% received rituximab-containing chemotherapies. Three hundred and ninety-nine (32.3%) patients received intensive treatments, and 175 (43.9%) of them received rituximab-containing chemotherapies. The 5-yr overall survival (OS) rate was 61%, and age was an important prognostic factor for CLL/SLL patients. This study is the first population-based study in Asia and provides comprehensive evidence of epidemiol., treatment patterns and survivals of CLL/SLL in an Asian population. This study involved multiple reactions and reactants, such as 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7Application In Synthesis of 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid).

4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7) belongs to imidazole derivatives. The solubility of imidazoles in ethers is lower than that in alcohols and decreases with increasing chain length of the ethers . In contrast, the solubility of benzimidazoles in alcohols (C3–C6) is higher than in water and generally decreases with a Imidazole derivatives have antibacterial, antifungal and anticancer functionality. It interacts with DNA and also binds to protein and stops cell division.Application In Synthesis of 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Flammability, thermal stability, and phase change characteristics of several trialkylimidazolium salts was written by Fox, Douglas M.;Awad, Walid H.;Gilman, Jeffrey W.;Maupin, Paul H.;De Long, Hugh C.;Trulove, Paul C.. And the article was included in Green Chemistry in 2003.Safety of 1,2-Dimethyl-3-propyl-1H-imidazol-3-ium hexafluorophosphate(V) The following contents are mentioned in the article:

Room temperature ionic liquids (RTILs) have emerged as tunable and potentially “greener” solvents for a multitude of applications. To investigate the solvent properties and potential use as a thermal fluid, a study was initiated to determine the effects of anion type, C-2 hydrogen substitution, and alkyl chain length on the flammability, thermal stability, and phase change characteristics of 1,2,3-trialkylimidazolium room temperature ionic liquids A Setaflash flash point apparatus was used to determine the flammabilities of the RTILs. No flash points were detected for any of the imidazolium based RTILs below 200°, the maximum temperature of the instrument. The thermal stabilities of the RTILs were measured using the technique of thermogravimetric anal. The 1,2,3-trialkylimidazolium compounds exhibit slightly higher thermal stabilities than the comparable 1,3-dialkylimidazolium compounds; RTILs with nucleophilic anions decompose about 150° lower than RTILs with bulky fluoride containing anions; the alkyl chain length does not have a large effect on the thermal stability of the RTILs; and the pyrolysis decomposition exhibits higher thermal stabilities via a different mechanism than the oxidative decomposition In addition, it was found that although the calculated onset temperatures were above 350°, significant decomposition does occur 100° or more below these temperatures The phase change behaviors of several imidazolium based RTILs were characterized by differential scanning calorimetry. The m.ps. of the RTILs increased with increasing alkyl chain length. Most of the salts studied exhibited significant undercooling, which decreased as the length of the alkyl chain was increased. The hexafluorophosphate and bromide RTILs exhibited polymorphic and liquid crystalline behaviors as the alkyl chain length was increased above C10. The clearing point temperatures increased more rapidly with alkyl chain length than the m.p. temperatures This study involved multiple reactions and reactants, such as 1,2-Dimethyl-3-propyl-1H-imidazol-3-ium hexafluorophosphate(V) (cas: 157310-73-1Safety of 1,2-Dimethyl-3-propyl-1H-imidazol-3-ium hexafluorophosphate(V)).

1,2-Dimethyl-3-propyl-1H-imidazol-3-ium hexafluorophosphate(V) (cas: 157310-73-1) belongs to imidazole derivatives. Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. Imidazole derivatives have antibacterial, antifungal and anticancer functionality. It interacts with DNA and also binds to protein and stops cell division.Safety of 1,2-Dimethyl-3-propyl-1H-imidazol-3-ium hexafluorophosphate(V)

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Optimization on the conversion of bamboo shoot shell to levulinic acid with environmentally benign acidic ionic liquid and response surface analysis was written by Zhou, Cunshan;Yu, Xiaojie;Ma, Haile;He, Ronghai;Vittayapadung, Saritporn. And the article was included in Chinese Journal of Chemical Engineering in 2013.Recommanded Product: 1-Hexyl-3-methyl-1H-imidazol-3-ium hydrogensulfate The following contents are mentioned in the article:

Levulinic acid (LA) has been identified as a promising green, biomass derived platform chem. Response surface anal. (RSA) with a four-factor-five-level central composite design (CCD) was applied to optimize the hydrolysis conditions for the conversion of bamboo (Phyllostachys Praecox f. preveynalis) shoot shell (BSS) to LA catalyzed with ionic liquid[C₄min]HSO₄. The effects of four main reaction parameters including temperature, time, C_[C4min]HSO4 (initial [C₄mim]HSO₄ concentration) and X_BSS (initial BSS intake) on the hydrolysis reaction for yield of LA were analyzed. A quadratic equation model for yield of LA was established and fitted to the data with an R² of 0.9868, and effects of main factors and their corresponding relationships were obtained with RSA. Model validation and results of CCD showed good correspondence between actual and predicted values. The anal. of variance (ANOVA) of the results indicated that the yield of LA in the range studied was significantly (P < 0.05) affected by the four factors. The optimized reaction conditions were as follows: temperature of 145°C, time of 103.8 min, C_[C4min]HSO4 of 0.9 mol · L^-1 and X_BSS of 2.04% (by mass), resp. A high yield [(71 ± 0.41)% (by mol), triplicate experiment] was obtained at the optimum conditions of temperature of 145°C, time of 104 min, C_[C4min]HSO4 of 0.9 mol · L^-1 and X_BSS of 2% (by mass), which obtained from the real experiments, concurred with the model prediction [73.8% (by mol) based on available C₆ sugars in BSS or 17.9% (by mass) based on the mass of BSS], indicating that the model was adequate for the hydrolysis process. This study involved multiple reactions and reactants, such as 1-Hexyl-3-methyl-1H-imidazol-3-ium hydrogensulfate (cas: 478935-29-4Recommanded Product: 1-Hexyl-3-methyl-1H-imidazol-3-ium hydrogensulfate).

1-Hexyl-3-methyl-1H-imidazol-3-ium hydrogensulfate (cas: 478935-29-4) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. Imidazole based anticancer drug find applications in cancer chemotherapy. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC).Recommanded Product: 1-Hexyl-3-methyl-1H-imidazol-3-ium hydrogensulfate

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Rabeprazole plus amoxicillin dual therapy is equally effective to bismuth-containing quadruple therapy for Helicobacter pylori eradication in central China: A single-center, prospective, open-label, randomized-controlled trial was written by Shao, Qiao-Qiao;Yu, Xue-Chun;Yu, Miao;Ma, Jing;Zhao, Jun-Bo;Yuan, Lin;Qi, Ya-Bin;Hu, Ruo-Bing;Wei, Pei-Ru;Xiao, Wei;Lan, Ling;Jia, Bai-Ling;Zhang, Lian-Zhong;Ding, Song-Ze. And the article was included in Helicobacter in 2022.Formula: C18H20N3NaO3S The following contents are mentioned in the article:

Background : Antibiotic resistance emerges as a major issue for Helicobacter pylori (H. pylori) treatment. High-dose dual therapy has recently shown encouraging results in H. pylori eradication, but it has yet to be validated in this H. pylori highly infected area; it is also not known if this concept can be extended to antibiotics other than amoxicillin, and factors that affect the eradication. We investigate if rabeprazole plus amoxicillin or furazolidone regimens could be a first-line therapy for H. pylori eradication, and factors that affect the curing rate. Methods : This is a single-center, prospective, open-label, randomized-controlled trial. Naive patients (n=292) were randomly treated with bismuth-containing quadruple therapy (BQT), rabeprazole plus amoxicillin (RADT), or furazolidone (RFDT) groups. RADT and FADT use three times daily regimens. H. pylori diagnosis and eradication were determined and confirmed by ¹³C-urea breath test. Results : In per-protocol (PP) anal., H. pylori eradication rate was 91.2in BQT group, 89.6in RADT, and 51.0in RFDT group. In intention-to-treat (ITT) anal., infection was eradicated in 86.7of patients in BQT group, 85.8in RADT, and 48.1in RFDT groups, resp. Noninferiority was confirmed between BQT and RADT groups. The incidence of side effects in BQT group was significantly higher than that in RADT group. Successful eradication was associated with lower body surface area (BSA) and low body mass index (BMI) in BQT group. Smoking and high BSA index reduced H. pylori eradication rate in RADT group. Conclusions : Rabeprazole-amoxicillin dual therapy is equally effective to the bismuth-containing quadruple therapy for H. pylori eradication with fewer side effects and saves use of one antibiotic per each treatment. Successful eradication is also associated with low BSA and non-smoking condition, which deserves future stratified anal. for refinement and optimization. This study involved multiple reactions and reactants, such as Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6Formula: C18H20N3NaO3S).

Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6) belongs to imidazole derivatives. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has become an important synthon in the development of new drugs. Imidazole also acts as a microtubule destabilizing agents and inhibits topoisomerase and Cytochrome P450 Family 26 Subfamily A Member 1 (CYP26A1) enzymes.Formula: C18H20N3NaO3S

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Protocol of a randomized, double-blind, placebo-controlled study of the effect of probiotics on the gut microbiome of patients with gastro-oesophageal reflux disease treated with rabeprazole was written by Liu, Wenjun;Xie, Yong;Li, Yingmeng;Zheng, Longjin;Xiao, Qiuping;Zhou, Xu;Li, Qiong;Yang, Ni;Zuo, Kexuan;Xu, Tielong;Lu, Nong-Hua;Zhang, Heping. And the article was included in BMC Gastroenterology in 2022.Computed Properties of C18H20N3NaO3S The following contents are mentioned in the article:

For patients with gastro-oesophageal reflux symptoms, the preferred treatment is proton pump inhibitor (PPI) administration for approx. 8 wk. However, long-term use of PPIs can cause gut microbiome (GM) disturbances. This study is designed to evaluate the effect of probiotics combined with a PPI on the GM and gastrointestinal symptoms of patients with gastro-oesophageal reflux disease (GERD). This is a randomized, double-blind, placebo-controlled trial. A total of 120 eligible patients with GERD will be randomized into the exptl. group or the control group. The treatment includes two phases: the initial treatment period lasts 8 wk (weeks 1-8), and the maintenance treatment period lasts 4 wk (weeks 9-12). During the initial treatment period, the exptl. group will take rabeprazole and LiHuo probiotics, and the control group will take rabeprazole and a probiotic placebo; during the maintenance treatment period, the exptl. group will take LiHuo probiotics, and the control group will take a probiotic placebo. The primary measure is the change in the GM. The secondary measures are the Reflux Disease Questionnaire (RDQ) score, Gastrointestinal Symptom Rating Scale (GSRS) score, faecal metabolome (FM), body mass index, Los Angeles grade of oesophagitis, adverse event (AE) rate and treatment compliance. Each outcome indicator will be assessed at day 0 (before administration), day 28 and/or 56 (during administration), and day 84 (end of administration) to reveal intragroup differences. AEs will be monitored to assess the safety of LiHuo probiotics. This will be the first trial to use the intestinal flora metagene method to analyze the effects of probiotics on patients with GERD receiving long-term PPI treatment. The goal is to provide evidence for the use of probiotics to reduce intestinal flora disorders and other symptoms of gastrointestinal discomfort in patients with GERD who have used PPIs for a long period. This study involved multiple reactions and reactants, such as Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6Computed Properties of C18H20N3NaO3S).

Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6) belongs to imidazole derivatives. 1H-imidazole is an imidazole tautomer which has the migrating hydrogen at position 1. It is a conjugate base of an imidazolium cation. It is a conjugate acid of an imidazolide. It is a tautomer of a 4H-imidazole. Imidazole has been usedin the lysis, wash and elution buffer for the purification of histidine tagged Sonic Hedgehog(shh-N) protein, in elution buffer in stepwise gradient for the purification of histidine tagged aldo keto reductases using nickel affinity chromatography, as a component of homogenization buffer for the purification of phagosomal compartments from dendritic cells.Computed Properties of C18H20N3NaO3S

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Graft-versus-Host Disease Prophylaxis with Post-Transplantation Bendamustine in Patients with Refractory Acute Leukemia: A Dose-Ranging Study was written by Moiseev, Ivan;Bondarenko, Sergey;Morozova, Elena;Vlasova, Yulia;Dotsenko, Anna;Epifanovskaya, Olga;Babenko, Elena;Botina, Anna;Baykov, Vadim;Surkova, Elena;Lapin, Sergey;Beynarovich, Anastasiya;Borzenkova, Evgeniya;Golosgchapov, Oleg;Kanunnikov, Mikhail;Kudyasheva, Olga;Ovechkina, Varvara;Pirogova, Olga;Porunova, Valentina;Rudakova, Tatyana;Smikova, Olesya;Smirnova, Anna;Afansyev, Boris. And the article was included in Transplantation and Cellular Therapy in 2021.HPLC of Formula: 16506-27-7 The following contents are mentioned in the article:

The prognosis of acute leukemia refractory to induction chemotherapy or immunotherapy is dismal. Salvage allogeneic hematopoietic stem cell transplantation (HSCT) is widely used option for these patients, but only 10% to 15% of patients are cured by the procedure. Preclin. studies indicate that substitution of post-transplantation cyclophosphamide with bendamustine (PTB) in a prophylaxis regimen may be associated with an augmented graft-vs.-leukemia (GVL) reaction. The aim of this study was to establish the optimal dose of PTB and evaluate the antileukemic effect of HSCT with this type of graft-vs.-host disease (GVHD) prophylaxis. In the prospective trial (NCT02799147), PTB was administered in doses of 140, 100, and 70 mg/m2 on days +3 and +4. Myeloablative conditioning with fludarabine and oral busulfan was provided to all patients. The first 12 patients received single-agent PTB, and subsequent patients received combination therapy with tacrolimus and mycophenolate mofetil (MMF). Inclusion criteria were acute myelogenous leukemia (AML) or acute lymphoblastic leukemia (ALL) refractory to at least one induction course of chemotherapy or target therapy and ≥5% clonal blasts in the bone marrow. The study cohort comprised 22 patients with AML and 5 with ALL. Seven patients were enrolled in the 140 mg/m2 group (due to a stopping rule), and 10 each were enrolled in the 100 mg/m2 and 70 mg/m2 groups. Primary refractory disease was documented in 41% of the patients, and secondary refractory was documented in 59%. The median blast count in the bone marrow at the start of the conditioning was 18% (range, 6% to 97%). Transplantation was performed with a matched sibling donor in 5 patients, a matched or mismatched unrelated donor in 15, and a haploidentical donor in 7. Engraftment was documented in 93% of the patients, including 89% with complete remission and 63% without measurable residual disease. After PTB prophylaxis, we observed an unusual complication, a cytokine release syndrome (CRS), in 70% of the patients, including grade 3 to 5 CRS in 44%. The most frequent clin. symptoms included high fever in 67% of patients, abnormal liver function tests in 67%, pancreatitis in 63%, skin vasculitis in 56%, enterocolitis in 48%, inflammation of oral mucosa in 37%, disseminated intravascular coagulation in 37%, and central nervous system toxicity in 26%. The development of CRS was associated with use of an HLA-mismatched donor (75% vs. 20%; P = .0043). Classic acute GVHD was documented in 44% of the patients. Grade II-IV acute GVHD was associated with grade 3 to 5 CRS (67% vs. 25%; P = .031). Moderate and severe chronic GVHD in the 100-day survivors were more often observed after single-agent PTB than after the combination immunosuppression (100% vs. 18%; P = .002). A relatively low relapse rate was observed for this patient population. Three-year overall survival was 28% (95% confidence interval [CI], 13% to 46%), and event-free survival was 29% (95% CI, 13% to 46%). Nonrelapse mortality was 46% (95% CI, 25% to 64%), and the cumulative incidence of relapse was 26% (95% CI, 11% to 44%). No relapses were documented after day +100. There were no statistically significant differences among the dose groups (P = .3481); however, survival was higher in the 100 mg/kg group. Survival was higher in patients with AML compared with those with ALL (35% vs. 0%; P = .0157). PTB represents a promising option to augment the GVL effect in refractory AML; however, the high CRS-associated mortality necessitates addnl. studies to reduce the risk of this complication. Thus, routine clin. application of PTB cannot be currently recommended. Combination immunosuppression with tacrolimus and MMF partially ameliorates these complications, at least in the setting of HLA-matched allografts. Biol. mechanisms of CRS and GVL after PTB require further elucidation. This study involved multiple reactions and reactants, such as 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7HPLC of Formula: 16506-27-7).

4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7) belongs to imidazole derivatives. Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. Imidazole also acts as a microtubule destabilizing agents and inhibits topoisomerase and Cytochrome P450 Family 26 Subfamily A Member 1 (CYP26A1) enzymes.HPLC of Formula: 16506-27-7

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Imidazoles. IX. A new preparation of N-alkylated imidazole compounds was written by Weidenhagen, Rudulf;Train, Gert;Wegner, Hans;Nordstrom, Ludwig. And the article was included in Berichte der Deutschen Chemischen Gesellschaft [Abteilung] B: Abhandlungen in 1942.Name: 2,3-Dimethyl-3H-imidazo[4,5-c]pyridine The following contents are mentioned in the article:

A solution of 2 g. Cu(OAc)₂, 2 cc. 40% HCHO and 30 cc. H₂O at 0° is treated with 1 g. ο-H₂NC₆H₄NHMe.2HCl in 15 cc. 50% alc. at 0°; the CuCl salt precipitates immediately and the reaction is completed by heating 10 min. at 75°; decomposition with H₂S in dilute HCl gives the HCl salt, which is liberated by K₂CO₃; the yield of 1-methylbenzimidazole (I) is 67%; AcH gives 83% of the 2-Me derivative of I; EtCHO yields the 2-Et derivative, very hygroscopic, m. 61.5-2.5° (containing 0.79 mol. H₂O), m. 54.5-5.5° (anhydrous); picrate, m. 235-6°; iso-PrCHO gives 84% of the 2-iso-Pr derivative, b_0.3 116-18° (picrate, yellow, m. 225-6°); BzH gives 87.5% of the 2-Ph derivative; p-MeOC₆H₄CHO yields 77.5% of the 2-(p-methoxyphenyl) derivative, m. 118°; 2-(p-nitrophenyl) derivative, yellow, m. 213-14°, 88%; 2-(2-furyl) derivative, with 0.5 mol. H₂O, m. 78° (anhydrous, m. 56°), 85%. ο-O₂NC₆H₄NHEt with SnCl₂ in HCl gives 69% of N-ethyl-ο-phenylenediamine (II), m. 185-7° (decomposition). II, HCHO and Cu(OAc)₂ give 71% of 1-ethylbenzimidazole (III); AcH yields 90% of the 2-Me derivative of III, b_0.3 110-12° (picrate, m. 236-7°); EtCHO gives 74% of the 2-Et derivative of III, b_0.2 106.5-7.5° (HCl salt, m. 168.5-9.5°; picrate, m. 207°); BzH yields 82% of the 2-Ph derivative of III; 2-(p-methoxyphenyl) derivative, m. 106-6.5°, 90%; 2-(m-nitrophenyl) derivative, m. 117.5-18°, 46%. ο-ClC₆H₄NO₂ and PrNH₂ in EtOH, heated 7 hrs., give 97% of N-propyl-ο-nitroaniline, red oil; reduction yields 57% of N-propyl-ο-phenylenediamine-2-HCl (IV), m. 172-3° (decomposition). IV, HCHO and Cu(OAc)₂ give 62% of 1-propylbenzimidazole (V), analyzed as the picrate, m. 180-1°; IV and AcH give 92% of the 2-Me derivative of V, hygroscopic oil, b_0.2 111-12° (picrate, m. 218-19°); 2-Et derivative, 85%; picrate, m. 212-12.5°; 2-(p-methoxyphenyl) derivative, m. 67.5-8°. 3-Amino-4-(methylamino)pyridine (VI), m. 169°, results in 95% yield on reduction of the 3-NO₂ compound with Fe in AcOH (picrate, m. 184°; HCl salt, m. 221°). VI (1.8 g.), 1 cc. AcH and 6 g. Cu(OAc)₂ in 50 cc. 50% EtOH, heated 3 hrs. at 150°, give 50% of 1′,2′-dimethylimidazolo-4′,5′,3,4-pyridine (VII), m. 174° (picrate, m. 204-5°); EtCHO gives 48% of the 2′-Et analog of VII, with 1.5 mols. H₂O, m. 76°; 2′-Pr analog, with 1.5 mols. H₂O, m. 64°, 59%; 2′-hexyl analog, a hygroscopic oil, analyzed as the dioxalate, m. 140°, 47%; 2′-Ph analog, m. 149°, 49% (hydrated, m. 79-80°); 2′-(2-furyl) analog, m. 173°, 57%. 3-Amino-4-(ethylamino)pyridine, AcH and Cu(OAc)₂ in EtOH, heated 4.5 hrs. at 150°, give 1′-ethyl-2′-methylimidazolo-4′,5′,3,4-pyridine, m. 84°; with 1 mol. of H₂O, m. 40°; picrate, m. 191°; 2′-Et analog, hygroscopic oil; with 2 mols. H₂O, m. 52°, 54%; 2′-Pr analog, very hygroscopic oil, 39%; with 2 mols. H₂O, m. 68°; 2′-(p-methoxyphenyl) analog, m. 142°, 71%; 2′-(2-furyl) analog, pale yellow, m. 125°, 68%. 3-Nitro-4-(propylamino)pyridine, in nearly theoretical yield by boiling 3-nitro-4-methoxypyridine with PrNH₂ in EtOH; 3-NH₂ derivative, with 1 mol. H₂O, m. 93°, 78%. 1′-Propyl-2′-methylimidazolo-4′,5′,3,4-pyridine, analyzed as the picrate, yellow, m. 156.5-7.5°; 1′-Bu analog, with 2 mols H₂O, m. 47°, 58%. This study involved multiple reactions and reactants, such as 2,3-Dimethyl-3H-imidazo[4,5-c]pyridine (cas: 52538-09-7Name: 2,3-Dimethyl-3H-imidazo[4,5-c]pyridine).

2,3-Dimethyl-3H-imidazo[4,5-c]pyridine (cas: 52538-09-7) belongs to imidazole derivatives. Imidazole is a heterocyclic compound with a five-membered planar ring. It is amphoteric and highly polar. Imidazole based anticancer drug find applications in cancer chemotherapy. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC).Name: 2,3-Dimethyl-3H-imidazo[4,5-c]pyridine

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Bioequivalence of a Newly Developed Dabigatran Etexilate Tablet Versus the Commercial Capsule and Impact of Rabeprazole-Induced Elevated Gastric pH on Exposure in Healthy Subjects was written by Harada, Akiko;Ikushima, Ippei;Haranaka, Miwa;Yanagihara, Aki;Nakayama, Daisuke. And the article was included in American Journal of Cardiovascular Drugs in 2020.Formula: C18H20N3NaO3S The following contents are mentioned in the article:

Background and Objective: Dabigatran etexilate (DE) is an anticoagulant with proven efficacy and tolerability for stroke prevention in patients with non-valvular atrial fibrillation. For the com. capsule, a complex formulation is used to maintain the acidic microenvironment required for maximal absorption. Consequently, its efficacy and safety are similar with or without concomitant intake of proton-pump inhibitors (PPIs). A simplified DE tablet formulation was developed and tested in two studies. One investigated bioequivalence (BE) of the novel DE tablet vs. the com. DE capsule. The other investigated DE bioavailability (BA) under pretreatment with the PPI rabeprazole and assessed the effect of elevated pH on exposure to dabigatran. Methods: BE of the novel DE tablet vs. the DE capsule was assessed in a randomized two-treatment, four-period, two-sequence crossover study (NCT03070171). The effect of rabeprazole on the BA of the DE tablet was assessed in an open-label, single-arm study (NCT03143166). Both studies were conducted at sites in Japan. Participants were healthy male volunteers, aged ≥ 20-40 years. In the BE study, participants received the DE tablet or capsule (single oral dose, 110 mg); primary endpoints were area under the concentration-time curve from baseline to the last quantifiable data point (AUC_0-tz) and maximum plasma concentration (C_max) of unconjugated dabigatran. In the relative BA study, participants received the DE tablet (single oral dose, 110 mg) with or without rabeprazole pretreatment (once daily for 5 days, 20 mg); primary endpoints were AUC_0-tz and C_max of total dabigatran. Results: In total, 160 participants were randomized in the BE study; 36 participants were enrolled in the BA study. The 90% confidence intervals of geometric mean (gMean) ratios for AUC_0-tz (101.4-116.0%) and C_max (101.8-116.6%) of unconjugated dabigatran were within pre-defined acceptance criteria for BE. In the relative BA study, the gMeans of AUC_0-tz (667 to 192 ng h/mL) and C_max (83.1 to 21.8 ng/mL) were decreased by approx. 70% when the tablet was administered under rabeprazole pretreatment. The reduction in BA was observed at a mean gastric pH of 5.3. Treatment was well tolerated; no deaths, serious adverse events (AEs) or significant AEs were reported in either study. Conclusion: The DE tablet demonstrated BE to the capsule; however, at high gastric pH, BA of the tablet was reduced by approx. 70%, which may lead to reduced efficacy. Data indicate the importance of examining not only BE under standard conditions, but relative BA at elevated gastric pH. Such investigations may avoid the reduced BA at elevated pH that is quite common in the target population (the elderly and/or patients treated with gastric-acid modifying co-medications), and therefore reduce treatment failure with DE. This study involved multiple reactions and reactants, such as Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6Formula: C18H20N3NaO3S).

Sodium 2-(((4-(3-methoxypropoxy)-3-methylpyridin-2-yl)methyl)sulfinyl)benzo[d]imidazol-1-ide (cas: 117976-90-6) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. Many drugs contain an imidazole ring, such as certain antifungal drugs, the nitroimidazole series of antibiotics, and the sedative midazolam.Formula: C18H20N3NaO3S

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Cationic Ir(III) Complexes Featuring Phenylimidazole-type Cyclometalated Ligands: Fluorine-Free Blue Phosphorescent Emitters for Light-Emitting Devices was written by Song, Yongjun;Yu, Renyou;Chen, Mengzhen;He, Lei. And the article was included in Inorganic Chemistry in 2021.HPLC of Formula: 914306-50-6 The following contents are mentioned in the article:

The development of blue emissive cationic Ir(III) complexes with no F substitutions but with sufficient blue-color purity and high phosphorescence efficiency has remained challenging. Here, F-free cyan to deep-blue emissive cationic Ir(III) complexes with phenylimidazole type cyclometalated ligands (CN̂) are reported, which are [Ir(dphim)₂(dmapzpy)]PF₆ (1), [Ir(ipr-dphim)₂(dmapzpy)]PF₆ (2), [Ir(ipr-dphim)₂(bipz)]PF₆ (3), and [Ir(ipr-dphim)₂(bicb)]PF₆ (4). 1,2-diphenyl-1H-imidazole (dphim) and 1-(2,6-diisopropylphenyl)-2-phenyl-1H-imidazole (ipr-dphim) are the phenylimidazole type CN̂ ligands, and 4-dimethylamino-2-(1H-pyrazol-1-yl)pyridine (dmapzpy), di(1H-pyrazol-1-yl)methane (bipz), and 3,3′-methylenebis(1-Me-1H-imidazol-3-ium-2-ide) (bicb) are the neutral ancillary ligands (AÂ). In both solution and diluted films, 1 shows cyan emission with the emission maximum at ∼472 and 495 nm, and 2–4 provide deep-blue emission with the emission maximum at ∼460 and 480 nm. While the complexes exhibit low to moderate phosphorescent efficiencies (0.05-0.35) in degassed MeCN solution, they exhibit high phosphorescent efficiencies (≤0.82) in diluted films. Theor. calculations revealed that the mixed ³π-π^* (CN̂-centered)/³MLCT (Ir → CN̂) states are responsible for the emission afforded by 1–4, which undergo nonradiative deactivations induced by different types of metal-centered states. Organic light-emitting diodes (OLEDs) with 1–4 as phosphorescent dopants are fabricated by solution-process, which afford blue-green to blue emission with the emission maximum at ∼460 and 490 nm for the blue devices and a high current-efficiency at 28.1 cd A^-1 for the blue-green device. Solid-state light-emitting electrochem. cells (LECs) are fabricated with 1–2 as phosphorescent dopants, which provide green-blue to blue emission with high luminance (up to 840 cd m^-2) and current-efficiency (≤16.8 cd A^-1) under a constant-current driving. By using phenylimidazole type CN̂ ligands and optimized AÂ ligands, blue emissive cationic Ir(III) complexes with no F substitutions but with sufficient blue-color purity and high phosphorescence efficiency can be developed. This study involved multiple reactions and reactants, such as 1-(2,6-Diisopropylphenyl)-2-phenyl-1H-imidazole (cas: 914306-50-6HPLC of Formula: 914306-50-6).

1-(2,6-Diisopropylphenyl)-2-phenyl-1H-imidazole (cas: 914306-50-6) belongs to imidazole derivatives. Many natural products, especially alkaloids, contain the imidazole ring. These imidazoles share the 1,3-C3N2 ring but feature varied substituents. Imidazole has been usedin the lysis, wash and elution buffer for the purification of histidine tagged Sonic Hedgehog(shh-N) protein, in elution buffer in stepwise gradient for the purification of histidine tagged aldo keto reductases using nickel affinity chromatography, as a component of homogenization buffer for the purification of phagosomal compartments from dendritic cells.HPLC of Formula: 914306-50-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

COVID-19 and CAR T cells: a report on current challenges and future directions from the EPICOVIDEHA survey by EHA-IDWP was written by Busca, Alessandro;Salmanton-Garcia, Jon;Corradini, Paolo;Marchesi, Francesco;Cabirta, Alba;Di Blasi, Roberta;Dulery, Remy;Lamure, Sylvain;Farina, Francesca;Weinbergerova, Barbora;Batinic, Josip;Nordlander, Anna;Lopez-Garcia, Alberto;Drgona, Lubos;Espigado-Tocino, Ildefonso;Falces-Romero, Iker;Garcia-Sanz, Ramon;Garcia-Vidal, Carolina;Guidetti, Anna;Khanna, Nina;Kulasekararaj, Austin;Maertens, Johan;Hoenigl, Martin;Klimko, Nikolai;Koehler, Philipp;Pagliuca, Antonio;Passamonti, Francesco;Cornely, Oliver A.;Pagano, Livio. And the article was included in Blood Advances in 2022.Reference of 16506-27-7 The following contents are mentioned in the article:

The aim of this study was to describe the clin. outcomes of patients developing COVID-19 after treatment with CAR T cells. In this retrospective observational multicenter study, collected data on all consecutive adult patients who received CAR T-cell therapy with symptomatic COVID-19 between Jan. 2020 and Feb. 2021 across 18 European centers (Spain, n = 6; France, n = 3; Italy, n = 2; and Belgium, Croatia, Czechia, Slovakia, Sweden, Switzerland, and the United Kingdom, n = 1 each) participating in the survey promoted by the European Hematol. Association (EHA) Scientific Working Group on Infection in Hematol. (EPICOVI- DEHA survey), developed by the EHA Infectious Diseases Working Party (IDWP). Patients received CAR T cells for the treatment of large B-cell lymphoma (n 5 28), multiple myeloma (n 5 1), and acute lymphoblastic leukemia (n 5 1). CAR T cells were tisagenlecleucel (Kymriah) in 16 cases and axicabtagene (Yescarta) in 13 cases, and 1 patient with multiple myeloma was treated with CAR T cells targeting B-cell maturation antigen. Median time from CAR T-cell treatment to COVID-19 diagnosis was 169 days (IQR, 37-313; range, 1-635). Cellular and humoral immune reconstitution after CAR T cells showed that 90 days after infusion, median absolute neutrophil count and absolute lymphocyte count (ALC) were 1700/mm3 and 435/mm3 resp., whereas at the time of COVID-19 diagnosis, median absolute neutrophil count and ALC were 925/mm3 and 370/mm3 resp. In total, 13 patients (43.3%) required admission to ICU after COVID-19, and 9 of them (66.7%) required mech. ventilation. Patients received treatment for COVID-19 according to local policy; 15 patients were treated with convalescent plasma alone (n = 3) or convalescent plasma combined with remdesivir with or without steroids (n = 8), remdesivir with lopinavir/ritonavir and steroids (n = 1), and tocilizumab and steroids (n = 3); 5 patients were treated with steroids alone (n = 4) or steroids combined with remdesivir and tocilizumab (n = 1); 1 patient was treated with azithromycin; and patient was treated with remdesivir alone. Severe (grade > 3) CRS after CAR T cells was observed in 1 patient only, and in total, 8 (53.3%) of 15 patients who developed CRS after CAR T-cell infusion required treatment with tocilizumab with or without steroids. Therapeutic strategies will need to be developed to ensure that CAR T-cell therapy can be delivered safely and successfully while COVID-19 remains endemic. This study involved multiple reactions and reactants, such as 4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7Reference of 16506-27-7).

4-(5-(Bis(2-chloroethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoic acid (cas: 16506-27-7) belongs to imidazole derivatives. Imidazole is the basic core of some natural products such as histidine, purine, histamine and DNA based structures, etc. Among the different heterocyclic compounds, imidazole is better known due to its broad range of chemical and biological properties. Imidazole has been usedin the lysis, wash and elution buffer for the purification of histidine tagged Sonic Hedgehog(shh-N) protein, in elution buffer in stepwise gradient for the purification of histidine tagged aldo keto reductases using nickel affinity chromatography, as a component of homogenization buffer for the purification of phagosomal compartments from dendritic cells.Reference of 16506-27-7

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem