Tag: 100-200

《Efficient synthesis of mibefradil analogues: an insight into in vitro stability》 was published in Organic & Biomolecular Chemistry in 2014. These research results belong to Lee, Ji Eun; Kwon, Tae Hui; Gu, Su Jin; Lee, Duck-Hyung; Kim, B. Moon; Lee, Jae Yeol; Lee, Jae Kyun; Seo, Seon Hee; Pae, Ae Nim; Keum, Gyochang; Cho, Yong Seo; Min, Sun-Joon. Application In Synthesis of 3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol The article mentions the following:

This article describes the synthesis and biol. evaluation of a chem. library of mibefradil analogs to investigate the effect of structural modification on in vitro stability. The construction of the dihydrobenzopyran structure in mibefradil derivatives I (X = CH2, O; R1 = H, Me, F, NO2, Cl, 5,6-(Cl)2, Br; R2 = H, iPr, CF3CH2, cyclopropyl) was achieved through two efficient approaches based on a diastereoselective intermol. Reformatsky reaction and an intramol. carbonyl-ene cyclization. In particular, the second strategy through the intramol. carbonyl-ene reaction led to the formation of a key intermediate II in a short and highly stereoselective way, which has allowed for practical and convenient preparation of analogs I. Using this protocol, we could obtain 22 new mibefradil analogs, which were biol. tested for in vitro efficacies against T-type calcium channels and metabolic stabilities. Among the synthesized compounds, we found that analog I (X = CH2, R1 = R2 = H) containing a dihydrobenzopyran ring and a secondary amine linker showed high % remaining activities of the tested CYP enzymes retaining the excellent T-type calcium channel blocking activity. These findings indicated that the structural modification of mibefradil was effective for improving in vitro stability, i.e., reducing CYP inhibition and metabolic degradation The experimental process involved the reaction of 3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol(cas: 2403-66-9Application In Synthesis of 3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol)

3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol(cas: 2403-66-9) belongs to imidazoles.Imidazole rings are part of unnatural cyclic peptides and are used as ester isosteres in peptidomimetic studies.
However, the application of imidazoles is not limited to the field of peptides and peptidomimetics. Application In Synthesis of 3-(1H-Benzo[d]imidazol-2-yl)propan-1-ol

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Application In Synthesis of 2-Chloro-1H-benzo[d]imidazoleIn 2018 ,《Molecular modeling, synthesis, antibacterial and cytotoxicity evaluation of sulfonamide derivatives of benzimidazole, indazole, benzothiazole and thiazole》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Naaz, Farha; Srivastava, Ritika; Singh, Anuradha; Singh, Nidhi; Verma, Rajesh; Singh, Vishal K.; Singh, Ramendra K.. The article conveys some information:

A new series of heterocyclic mols. bearing sulfonamide linkage has been synthesized and screened for antibacterial activity. During antibacterial screening using broth dilution method, mols. were found to be highly active (MIC value 50-3.1 μg/mL) against different human pathogens, namely B. cereus, S. aureus, E. coli and P. aeruginosa, and most effective against E. coli. A great synergistic effect was observed during determination of FIC where mols. were used in combination with reference drugs chloramphenicol and sulfamethoxazole. The MIC value of the combination – varying concentration of test compounds and 1/2 MIC of reference drugs or varying concentration of reference drugs and 1/2 MIC of test compounds, was reduced up to 1/4 or 1/32 of the original value, indicating thereby the combination was 4-32 times more potent than the test mol. The mols. also showed low degree of cytotoxicity against PBM, CEM and VERO cell lines. The results pos. indicated towards the development of lead antibacterials using the combination approach. In the experimental materials used by the author, we found 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Application In Synthesis of 2-Chloro-1H-benzo[d]imidazole)

2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1) is an analog of benzimidazole that has been synthesized by Langmuir adsorption isotherm. It is a white crystalline solid that can be dissolved in water and hydrochloric acid. 2-Chloro-1H-benzo[d]imidazole inhibits the growth of herpes simplex virus by acting as a competitive inhibitor for the viral enzyme thymidine kinase, which catalyzes the conversion of thymine to thymidine.Application In Synthesis of 2-Chloro-1H-benzo[d]imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Product Details of 530-62-1In 2022 ,《Prebiotically Plausible Autocatalytic Peptide Amyloids》 appeared in Chemistry – A European Journal. The author of the article were Rout, Saroj K.; Rhyner, David; Riek, Roland; Greenwald, Jason. The article conveys some information:

The prebiotic emergence of mols. capable both of self-replication and of storing information was a defining event at the dawn of life. Still, no plausible prebiotic self-replication of biol. relevant mols. has been demonstrated. Building upon the known templating nature of amyloids, we present two systems in which the products of a peptide-bond-forming reaction act as self-replicators to enhance the yield and stereoselectivity of their formation. This first report of an amino acid condensation that can undergo autocatalysis further supports the potential role of amyloids in prebiotic mol. evolution as an environment-responsive and information-coding system capable of self-replication. The experimental process involved the reaction of Di(1H-imidazol-1-yl)methanone(cas: 530-62-1Product Details of 530-62-1)

Di(1H-imidazol-1-yl)methanone(cas: 530-62-1) is a coupling agent in the synthesis of dipolar polyamides for nonlinear optical applications and polypeptides. It also used to make β-keto sulfones and sulfoxides, lead sequestering agents, and β-enamino acid derivatives.Product Details of 530-62-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

In 2022,Hokmabadi, Fahimeh; Zadmard, Reza; Akbarzadeh, Ali; Tafakori, Vida; Jalali, Mohammad Reza; Ahmadian, Gholamreza published an article in Royal Society Open Science. The title of the article was 《Synthesis of a new chitosan-p-tert-butylcalix[4]arene polymer as adsorbent for toxic mercury ion》.COA of Formula: C7H6N4O The author mentioned the following in the article:

In this paper, we have synthesized a novel chitosan-p-tert-butylcalix[4]arene polymer (CCP) as a highly efficient adsorbent for mercury ion (Hg2+) removal from water. In fact, a lower rim diamine derivative of p-tert-butylcalix[4]arene has been cross-linked with chitosan chain by carbonyl diimidazole (CDI) as the linker. CDI forms a urea linkage between calix[4]arene diamine derivative and amine groups of the chitosan polymeric chain. The structure and properties of the new polymer were characterized by Fourier transform IR spectroscopy, X-ray diffraction and scanning electron microscope. Also, the adsorption capacity of CCP was studied towards Hg2+ in aqueous medium by inductively coupled plasma-optical emission spectrometry. Interestingly, the results showed a considerable adsorption capacity for CCP in comparison with chitosan. Therefore, CCP can be introduced as a promising adsorbent for the elimination of Hg2+ from wastewaters. Moreover, because of the conformity of adsorption kinetic with pseudo-second-order kinetic models, it can be concluded that chem. adsorption has an important role between functional groups on CCP polymer and Hg2+ ions. In addition, according to Freundlich isotherm, the CCP surface was heterogeneous with different functional groups. The experimental part of the paper was very detailed, including the reaction process of Di(1H-imidazol-1-yl)methanone(cas: 530-62-1COA of Formula: C7H6N4O)

Di(1H-imidazol-1-yl)methanone(cas: 530-62-1) is a coupling agent in the synthesis of dipolar polyamides for nonlinear optical applications and polypeptides. It also used to make β-keto sulfones and sulfoxides, lead sequestering agents, and β-enamino acid derivatives.COA of Formula: C7H6N4O

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Ma, Zonghui; Jiang, Ling; Li, Bingyan; Liang, Dailin; Feng, Yu; Liu, Li; Jiang, Cheng published an article in 2021. The article was titled 《Discovery of benzimidazole derivatives as potent and selective aldehyde dehydrogenase 1A1 (ALDH1A1) inhibitors with glucose consumption improving activity》, and you may find the article in Bioorganic & Medicinal Chemistry.HPLC of Formula: 4857-06-1 The information in the text is summarized as follows:

Aldehyde dehydrogenase 1A1 (ALDH1A1) plays vital physiol. and toxicol. functions in many areas, such as CNS, inflammation, metabolic disorders, and cancers. Overexpression of ALDH1A1 has been disclosed to play an important role in obesity, diabetes and other diseases, indicating the potential need for the identification and development of small mol. ALDH1A1 inhibitors. Herein, a series of benzimidazole derivatives was designed, synthesized and evaluated. Among them, compounds 21, 27, 29, 61 and 65 exhibited excellent inhibitory activity against ALDH1A1 with IC50 values in the low micromolar range and high selectivity over ALDH1A2, ALDH1A3, ALDH2 and ALDH3A1. Moreover, an in vitro study demonstrated that all five compounds effectively improved glucose consumption in HepG2 cells, of which, 61 and 65 at 10 μM produced nearly equal glucose consumption with pos. control Metformin (Met) at 1 mM. Furthermore, 61 and 65 showed desirable metabolic stability in human liver microsomes. All these results suggest that 61 and 65 are suitable for further studies. In the experiment, the researchers used 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1HPLC of Formula: 4857-06-1)

2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1) is an analog of benzimidazole that has been synthesized by Langmuir adsorption isotherm. It is a white crystalline solid that can be dissolved in water and hydrochloric acid. 2-Chloro-1H-benzo[d]imidazole inhibits the growth of herpes simplex virus by acting as a competitive inhibitor for the viral enzyme thymidine kinase, which catalyzes the conversion of thymine to thymidine.HPLC of Formula: 4857-06-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Yadav, Priyanka; Kakati, Praachi; Singh, Preeti; Awasthi, Satish K. published their research in Applied Catalysis, A: General in 2021. The article was titled 《Application of sulfonic acid fabricated cobalt ferrite nanoparticles as effective magnetic nanocatalyst for green and facile synthesis of benzimidazoles》.Product Details of 934-32-7 The article contains the following contents:

This work represents the design and synthesis of efficient sulfonated cobalt ferrite solid acid catalyst. The synthesized solid acid green catalyst was characterized using various techniques viz. FT-IR, powder XRD, SEM, TEM and VSM. The obtained catalyst was used to synthesize biol. significant 2-substituted benzimidazole derivatives I (R = Ph, H, NH2, pyridin-3-yl) by condensation between o-phenylenediamine with various aromatic, aliphatic and heterocyclic aldehydes RCHO. High yield (up to 98%), short reaction time (10-25 min), mild reaction condition, wide functional group tolerance, easy work-up procedure and excellent values of green chem. metrices such as lower E factor (0.126), high RME value (88.83%), carbon efficiency (100%) and high atom economy (AE) value (90.65%), are some salient features of the present catalytic system. Moreover, the catalyst recovery by simply using an external magnet and catalyst reusability up to 7 times without any significant loss in catalytic efficiency are some addnl. remarkable features of the current protocol. In addition to this study using 1H-Benzo[d]imidazol-2-amine, there are many other studies that have used 1H-Benzo[d]imidazol-2-amine(cas: 934-32-7Product Details of 934-32-7) was used in this study.

1H-Benzo[d]imidazol-2-amine(cas: 934-32-7) can be used in the hydrolysis of a choline carbonate. It was also used in the synthesis of imidazo[1,2-a]benzimidazoles.Product Details of 934-32-7

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Prasoona, Gumpula; Kishore, Baireddy; Brahmeshwari, Gavaji published their research in Letters in Organic Chemistry in 2021. The article was titled 《Synthesis and Antimicrobial Evaluation of Benzimidazolyl Pyrimido[4,5-b]Quinolinones》.HPLC of Formula: 934-32-7 The article contains the following contents:

The reaction of 2-amino benzimidazoles with Et cyanoacetate afforded N-(1H-benzo[d]imidazol-2-yl)-2-cyanoacetamides I (R = H, Cl, NO2, Me, etc.). Compounds I on Knoevenagel condensation with o-nitro benzaldehydes produced (E)-N-(1H-benzo[d]imidazol-2-yl)-2-cyano-3-(2-nitrophenol) acylamides II (R1 = H, Cl, OMe). Compounds II were converted to 2-amino-N-(1H-benzo[d]imidazol-2-yl) quinoline-3-carboxamides III on treatment with stannous chloride by reductive cyclization. The target compounds viz., 3-(1H-benzo[d]imidazol-2-yl)-2-methylpyrimido[4,5-b]quinolin-4(3H)-ones IV were obtained by N-acetylation followed by cyclodehydration of compounds III in situ by treatment with acetic anhydride. 3-(1H-Benzo[d]imidazol-2-yl)-2-methylpyrimido[4,5-b]quinolin-4(3H)-ones IV have been synthesized from com. available materials in excellent yields. The title compounds IV are evaluated for in vitro antimicrobial activity. Compounds IV (R = Me; R1 = H), IV (R = OMe; R1 = H) and IV (R = H; R1 = OMe) have shown more antimicrobial activity than that of standard drugs. The structures of all the newly synthesized compounds I, II, III & IV are confirmed on the basis of spectral data. Antimicrobial studies of compounds IV have revealed that compounds IV (R = Me; R1 = H) and IV (R = OMe; R1 = H) have more efficient activity when compared to the standard drugs. In the experimental materials used by the author, we found 1H-Benzo[d]imidazol-2-amine(cas: 934-32-7HPLC of Formula: 934-32-7)

1H-Benzo[d]imidazol-2-amine(cas: 934-32-7) can be used in the hydrolysis of a choline carbonate. It was also used in the synthesis of imidazo[1,2-a]benzimidazoles.HPLC of Formula: 934-32-7

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

《Improved Coverage of Mouse Myelomeningocele With a Mussel Inspired Reverse Thermal Gel》 was written by Bardill, James R.; Park, Daewon; Marwan, Ahmed I.. Safety of Di(1H-imidazol-1-yl)methanone And the article was included in Journal of Surgical Research in 2020. The article conveys some information:

Myelomeningocele (MMC) is an open neural tube defect of the spinal column. Our laboratory previously introduced a reverse thermal gel (RTG) as the first in situ forming patch for in utero MMC application. To overcome the challenges of anchoring the RTG in the wet amniotic environment to improve MMC coverage, we modified the RTG to mimic the underwater adhesive properties of mussels. We have separated this study into three sep. hypotheses-based components:Based on mussel inspired chem., modification of the RTG with dopamine will increase the underwater adhesive properties to improve RTG anchoring ability in a wet environment. Methods: The dopamine-modified RTG (DRTG) was synthesized using carbonyldiimidazole chem. and characterized with proton NMR, Fourier transform IR spectroscopy, and UV-visible spectroscopy. Rheol. and underwater adhesive tests measured mech. properties. Results: DRTG synthesis was confirmed with proton NMR, Fourier transform IR spectroscopy, and UV-visible spectroscopy. Rheol. demonstrated increased elasticity. Underwater adhesion testing revealed DRTG has similar wet adhesive strength to Tisseel fibrin sealant.The DRTG will support in vitro skin cell growth and will be safe for injection in a mouse animal model. Methods: Biocompatibility testing included 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay, DRTG-fibroblast and keratinocyte cultures, and s.c. injections to quantify macrophages stained with immunohistochem. Results: 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and DRTG cell cultures revealed no cytotoxicity and demonstrated the growth of fibroblasts and keratinocytes. S.c. injections cause a macrophage response that decreases after 4 wk.In utero injection of novel DRTG into a mouse MMC model will be effective with improved patch coverage of the MMC defect. Methods: MMC coverage by DRTG was assessed using in utero mouse injections in the Grainy head-like 3 (Grhl3) mouse model. Results: In utero Grhl3 mouse injections demonstrate statistically significant (P = 0.012) improved MMC coverage of DRTG compared with previous RTG coverage with no significant macrophage response.The DRTG demonstrates increased elasticity, cellular scaffolding properties, and improved MMC coverage in the Grhl3 mouse model. Future studies will be translated to the preclin. ovine model to evaluate this novel gel. In addition to this study using Di(1H-imidazol-1-yl)methanone, there are many other studies that have used Di(1H-imidazol-1-yl)methanone(cas: 530-62-1Safety of Di(1H-imidazol-1-yl)methanone) was used in this study.

Di(1H-imidazol-1-yl)methanone(cas: 530-62-1) is a coupling agent in the synthesis of dipolar polyamides for nonlinear optical applications and polypeptides. It also used to make β-keto sulfones and sulfoxides, lead sequestering agents, and β-enamino acid derivatives.Safety of Di(1H-imidazol-1-yl)methanone

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

《A study of plasma electrolytic oxidation coatings doped with 2-ainobenzimidazole loaded halloysite nanotubes on AZ31 magnesium alloy》 was written by Wu, Wen-Xin; Lin, Hsin-Chih. HPLC of Formula: 934-32-7 And the article was included in Purazuma Oyo to Fukugo Kino Zairyo in 2020. The article conveys some information:

Plasma electrolytic oxidation (PEO) coatings with actively protective functionality by incorporating 2-aminobenzimidazole (2-ABI) loaded halloysite nanotubes (HNTs) was presented. The coatings were characterized by SEM and EDX. Corrosion behavior was evaluated by EIS measurement. With the SEM and EDX anal., the existence of HNT or 2ABI-loaded HNT was confirmed. EIS complex spectra showed the enhanced corrosion resistance of 2-ABI-HNT PEO coating, suggesting 2-ABI has good potential as corrosion inhibitor for Mg alloys.1H-Benzo[d]imidazol-2-amine(cas: 934-32-7HPLC of Formula: 934-32-7) was used in this study.

1H-Benzo[d]imidazol-2-amine(cas: 934-32-7) can be used in the hydrolysis of a choline carbonate. It was also used in the synthesis of imidazo[1,2-a]benzimidazoles.HPLC of Formula: 934-32-7

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

In 2019,Bioorganic & Medicinal Chemistry included an article by Chino, Ayaka; Honda, Shugo; Morita, Masataka; Yonezawa, Koichi; Hamaguchi, Wataru; Amano, Yasushi; Moriguchi, Hiroyuki; Yamazaki, Mayako; Aota, Masaki; Tomishima, Masaki; Masuda, Naoyuki. Name: 2-Chloro-1H-benzo[d]imidazole. The article was titled 《Synthesis, SAR study, and biological evaluation of novel 2,3-dihydro-1H-imidazo[1,2-a]benzimidazole derivatives as phosphodiesterase 10A inhibitors》. The information in the text is summarized as follows:

Phosphodiesterase 10A (PDE10A) inhibitors were designed and synthesized based on the dihydro-imidazobenzimidazole scaffold. Compound I showed moderate inhibitory activity and good permeability but unfavorable high P-glycoprotein (P-gp) liability for brain penetration. An optimization study to improve both the P-gp efflux ratio and PDE10A inhibitory activity was performed. As a result, compound II was identified with improved P-gp liability and high PDE10A inhibitory activity. Compound II also showed satisfactory brain penetration, suppressed phencyclidine-induced hyperlocomotion and improved MK-801-induced working memory deficit. In addition to this study using 2-Chloro-1H-benzo[d]imidazole, there are many other studies that have used 2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1Name: 2-Chloro-1H-benzo[d]imidazole) was used in this study.

2-Chloro-1H-benzo[d]imidazole(cas: 4857-06-1) binds to monoclonal antibodies, inhibiting their binding to their corresponding antigens. This activity may be due to its ability to bind covalently with amino groups on proteins and other molecules.Name: 2-Chloro-1H-benzo[d]imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem