Month: November 2022

On November 30, 1993, Basu, Ashis K.; Wood, Michael L.; Niedernhofer, Laura J.; Ramos, Leilani A.; Essigmann, John M. published an article.Reference of Imidazo[1,2-c]pyrimidin-5(6H)-one The title of the article was Mutagenic and genotoxic effects of three vinyl chloride-induced DNA lesions: 1,N6-ethenoadenine, 3,N4-ethenocytosine, and 4-amino-5-(imidazol-2-yl)imidazole. And the article contained the following:

The mutagenic and genotoxic properties of 1,N6-ethenoadenine (εAde), 3,N4-ethenocytosine (εCyt), and 4-amino-5-(imidazol-2-yl)imidazole (β) were investigated in vivo. The former two modified bases are known DNA adducts formed by the human carcinogen vinyl chloride; β is formed by pyrimidine ring-opening of εAde. Chem. synthesized deoxyhexanucleotides containing εAde and β, d[GCT(εA)GC], and d[GCT(β)GC], resp., were described previously [(1987) Biochem. 26, 5626-5635]. εCyt was inserted into an oligonucleotide, d[GCTAG(εC)], by a mild enzymic synthetic procedure, which avoided exposure of the base to alk. conditions. 3,N4-etheno-2′-deoxycytidine 3′,5′-bisphosphate coupled with reasonable efficiency (30-40%) to the 3′-nucleoside of an acceptor pentamer, d(GCTAG), in a reaction catalyzed by T4 RNA ligase in the presence of ATP. Each of the three modified hexanucleotides and an unmodified control were inserted into a six-base gap positioned at a known site in the genome of bacteriophage M13-NheI. A nick was placed in the DNA strand opposite that containing the single DNA lesions, enabling the formation of singly adducted single-stranded genomes by denaturation. After transfection of the adducted phage DNAs into Escherichia coli, each of the adducts was found to be genotoxic. The most toxic lesion was β, which reduced survival of the genome by 97%. εCyt and εAde reduced survival by 90% and 65%, resp. An examination of the surviving phage populations revealed that each of the three adducts was mutagenic. The least mutagenic lesion was εAde (0.1% of the survivors were mutant), which showed primarily A → G transitions. The εAde rearrangement product, β, was also found to induce mutations but at a 20-fold higher frequency (∼2%). In this case, however, mutagenesis was random, possibly because the hydrogen-bonding face of this lesion has been obliterated. εCyt induced mutations at a frequency of 1.5-2%; its mutations were mainly C → T transitions, although targeted C → A and -1 deletions were also detected. The possible resp. roles of these three DNA lesions in the mutagenic and carcinogenic activities of vinyl chloride and related haloalkanes are discussed. The experimental process involved the reaction of Imidazo[1,2-c]pyrimidin-5(6H)-one(cas: 55662-66-3).Reference of Imidazo[1,2-c]pyrimidin-5(6H)-one

The Article related to mutation genotoxicity vinyl chloride dna damage, ethenoadenine ethenocytosine aminoimidazolylimidazole dna genotoxicity, Toxicology: Carcinogens, Mutagens, and Teratogens and other aspects.Reference of Imidazo[1,2-c]pyrimidin-5(6H)-one

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On January 31, 1989, Eberle, Gertrud; Barbin, Alain; Laib, Reinhold J.; Ciroussel, Francoise; Thomale, Juergen; Bartsch, Helmut; Rajewsky, Manfred F. published an article.Safety of Imidazo[1,2-c]pyrimidin-5(6H)-one The title of the article was 1,N6-etheno-2′-deoxyadenosine and 3,N4-etheno-2′-deoxycytidine detected by monoclonal antibodies in lung and liver DNA of rats exposed to vinyl chloride. And the article contained the following:

1,N6-Etheno-2′-deoxyadenosine (εdAdo) and 3,N4-etheno-2′-deoxycytidine (εdCyd) are formed in vitro by reaction of DNA with the electrophilic metabolites of vinyl chloride (VC), chloroethylene oxide and chloroacetaldehyde. To detect and quantitate these DNA adducts in vivo, a series of specific monoclonal antibodies (Mab) were raised. Among those, Mab EM-A-1 and Mab EM-C-1, resp., were used for detection of εdAdo and εdCyd by competitive RIA, following preseparation of the etheno adducts from DNA hydrolyzates by HPLC. At 50% inhibition of tracer-antibody binding, both Mab had a detection limit of 187 fmol and antibody affinity constants (K) of 2 × 109 L/mol. The levels of εdAdo and εdCyd were quantitated in the DNA of lung and liver tissue of young rats exposed to 2000 ppm of VC for 10 days. The εdAdo/2′-deoxyadenosine and εdCyd/2′-deoxycytidine molar ratios were 1.3 × 10-7 and 3.3 × 10-7, resp., in lung DNA, and 5.0 × 10-8 and 1.6 × 10-7 in liver DNA. When hydrolyzates of 3 mg of DNA were analyzed by RIA at 25% inhibition of tracer-antibody binding, εdAdo and εdCyd were not detected in liver DNA from untreated rats above the limiting εdAdo/2′-deoxyadenosine and εdCyd/2′-deoxycytidine molar ratios of 2.2 × 10-8 and 3.1 × 10-8, resp. The experimental process involved the reaction of Imidazo[1,2-c]pyrimidin-5(6H)-one(cas: 55662-66-3).Safety of Imidazo[1,2-c]pyrimidin-5(6H)-one

The Article related to vinyl chloride ethenodeoxyadenosine ethenodeoxycytidine dna, lung dna adduct vinyl chloride, liver dna adduct vinyl chloride, Toxicology: Carcinogens, Mutagens, and Teratogens and other aspects.Safety of Imidazo[1,2-c]pyrimidin-5(6H)-one

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On October 14, 2021, Liu, Tao; Zhou, Shubao; Wang, Shaomeng; Zhang, Meng; Xu, Fuming; Zhou, Haibin; Aguilar, Angelo; Huang, Liyue published a patent.Safety of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one The title of the patent was Preparation of piperidine derivatives as menin inhibitors and methods of use for treating cancer. And the patent contained the following:

The present disclosure provides compounds represented by Formula (I): or a pharmaceutically acceptable salt thereof, wherein Ra, Rb, Rc, Rd, L1, R2 B, Q and E are as defined as set forth in the specification. The present disclosure also provides compounds of Formula (I) for use to treat cancer or any other disease, condition, or disorder that is responsive to inhibition of menin. :. The disclosure provides compounds represented by formula I, or a pharmaceutically acceptable salt thereof. The disclosure also provides compounds of formula I for use to treat cancer or any other disease, condition, or disorder that is responsive to inhibition of menin. Compounds of formula I wherein n is 0, 1 and 2; each Ra and each Rb are independently H and C1-4 alkyl; Rc is H and halo; each R4 is independently halo; Q is NHCO2R; R is C1-4 alkyl, C1-4 haloalkyl and CD3; B is imidazolylmethyl, pyrazolylmethyl, CH2OH, etc.; E is (un)substituted sulfonylphenyl, (un)substituted Ph, (un)substituted pyrimidinyl, etc.; L1 is CH2; and pharmaceutically acceptable salt thereof, are claimed. Example compound II was prepared by a multistep procedure (procedure given). The invention compounds were evaluated for their menin inhibitory activity. From the assay, it was determined that compound II exhibited IC50 values of less than 50 nM. The experimental process involved the reaction of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one(cas: 40644-16-4).Safety of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one

The Article related to piperidine preparation menin inhibitor treatment cancer, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Safety of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On February 15, 2021, Shahid, Salman; Baron, Gino V.; Denayer, Joeri F. M.; Martens, Johan A.; Wee, Lik H.; Vankelecom, Ivo F. J. published an article.COA of Formula: C6H11N3 The title of the article was Hierarchical ZIF-8 composite membranes: Enhancing gas separation performance by exploiting molecular dynamics in hierarchical hybrid materials. And the article contained the following:

Mixed matrix membranes (MMM) incorporating metal-organic framework (MOF) fillers have gained increasing attention in addressing environmental and sustainability challenges. Hierarchical materials combining pore sizes of different length scales are expected to facilitate mol. diffusion and mass transfer for the optimization of catalysis and separation processes. Herein, a novel preparation method for hierarchical ZIF-8 (H-ZIF-8) particles is presented for the synthesis of polyimide (PI)-based MMMs with good compatibility between filler and polymer. Gas permeability measurements of polyimide-Matrimid/H-ZIF-8 MMMs showed 4-fold improvements in permeability of both CO2 and CH4 coupled with a marked increase in selectivity and plasticization resistance for MMM with 30 wt% H-ZIF-8 loading. Gas transport anal. in these MMMs revealed that the enhanced gas separation performance of the MMMs can be related to the imidazolate modification of the PI structure and the hierarchical structure of H-ZIF-8, as confirmed by N2, Ar, mercury porosimetry, SEM, TEM anal. CO2 permeability for all MMMs increases with increasing CO2 concentration and by decreasing temperature The proof of concept, as demonstrated in this study, could be extended for the preparation of other hierarchical ZIFs and related MMMs. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).COA of Formula: C6H11N3

The Article related to hierarchical zif8 composite membrane gas separation mol dynamic, Plastics Fabrication and Uses: Plastic Product Uses and other aspects.COA of Formula: C6H11N3

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On May 31, 2019, Makino, Kosho; Hasegawa, Yumi; Inoue, Takahide; Araki, Koji; Tabata, Hidetsugu; Oshitari, Tetsuta; Ito, Kiyomi; Natsugari, Hideaki; Takahashi, Hideyo published an article.Safety of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole The title of the article was Chemoselective Demethylation of Methoxypyridine. And the article contained the following:

A chemoselective demethylation method for various methoxypyridine derivatives I (R = 3-OMe, 4-CH2=CHCH2O, 4-C6H5CH2O, etc.; X = H, 5-Cl, 4-Me, etc.; Y = CH, N) has been developed. Treatment of 4-methoxypyridine with L-selectride in THF for 2 h at reflux temperature afforded 4-hydroxypyridine in good yield; and no reaction to anisole is occurred. The utility of this method was demonstrated by the efficient synthesis of the metabolic substances of the antiulcer agent omeprazole. Chemoselective demethylation at the site of 3,5-dimethyl-4-methoxypyridine in the presence of 4-methoxybenzimidazole was achieved. The experimental process involved the reaction of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole(cas: 73590-85-9).Safety of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole

The Article related to hydroxypyridine preparation chemoselective, alkoxy pyridine demethylation, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Safety of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On September 1, 2020, Xu, Zhaozan; Tang, Hongying; Li, Nanwen published an article.Application In Synthesis of N-(3-Aminopropyl)-imidazole The title of the article was Enhanced proton/iron permselectivity of sulfonated poly(ether ether ketone) membrane functionalized with basic pendant groups during electrodialysis. And the article contained the following:

High permselectivity of cation exchange membrane for H+ and divalent metallic ions is essential for waste acid recovery by electrodialysis. Basic tertiary amine and imidazole groups were introduced into sulfonated poly(ether ether ketone) (SPEEK) membrane via a facile and controllable reaction, named as TA-x and IM-x (x was the basic group content), to construct acid-base pairs and reduce the swelling degree of membranes. 1H NMR confirmed the chem. structure of the as-obtained materials and protonation of tertiary amine and imidazole groups. As expected, all TA-x and IM-x membranes showed lower Fe2+ fluxes than pristine SPEEK membrane during electrodialysis because of their lower swelling degree and the electrostatic repulsion of protonated tertiary amine and imidazole groups. Remarkably, their H+ fluxes were kept similar to that of pristine SPEEK membrane. Therefore, the H+/Fe2+ permselectivity of membrane was improved considerably. Among them, IM-30 membrane showed the highest H+/Fe2+ permselectivity of 65.4, which was over three times that of pristine SPEEK membrane (19.1). Therefore, the introduction of basic groups into cation exchange membrane could reduce the swelling degree of membrane and improve the permselectivity between H+ and divalent metallic ions. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Application In Synthesis of N-(3-Aminopropyl)-imidazole

The Article related to sulfonated peek electrodialysis proton permselective membrane waste acid reclamation, Plastics Fabrication and Uses: Plastic Product Uses and other aspects.Application In Synthesis of N-(3-Aminopropyl)-imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On May 31, 2020, Nazir, Ahsan; Yu, Haojie; Wang, Li; Liu, Jinhua; Li, Songbiao; Ul Amin, Bilal; Naveed, Kaleem-ur-Rahman; Ullah Khan, Rizwan; Khan, Amin; Usman, Muhammad; Elshaarani, Tarig; Uddin, Alim Md. published an article.Name: N-(3-Aminopropyl)-imidazole The title of the article was Electromagnetic interference shielding effectiveness of ferrocene-based polyimidazole/carbon material composites. And the article contained the following:

Ferrocene-based polyimidazole (PPIFc) composites containing multiwalled carbon nanotube (MWCNT), reduced graphene oxide (RGO), and carbon black (CB) were prepared by chem. oxidative polymerization, resp. The prepared PPIFc/MWCNT, PPIFc/RGO, and PPIFc/CB composites were characterized by scanning electron microscope, transmission electron microscope, Fourier transform IR, X-ray diffraction, XPS, and thermogravimetric anal. The elec. conductive property of the PPIFc/MWCNT, PPIFc/RGO, and PPIFc/CB composites was tested by a four-probe method. The electromagnetic interference (EMI) shielding properties of the composites were measured by a coaxial method in the 1 to 4.5 GHz. These PPIFc/MWCNT, PPIFc/RGO, and PPIFc/CB composites showed good EMI shielding performance and total shielding effectiveness (SET) for PPIFc/CB was -11.2 dB, PPIFc/RGO was -13.1 dB, and PPIFc/MWCNT was -25.4 dB by using 50 wt% of the composite in the paraffin wax. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Name: N-(3-Aminopropyl)-imidazole

The Article related to ferrocene based polyimidazole mwcnt graphene oxide carbon black composite, electromagnetic interference shielding oxidative polymerization, Plastics Fabrication and Uses: Plastic Product Uses and other aspects.Name: N-(3-Aminopropyl)-imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Bollenbach, Maud; Nemska, Simona; Wagner, Patrick; Camelin, Guillaume; Daubeuf, Francois; Obrecht, Adeline; Villa, Pascal; Rognan, Didier; Bihel, Frederic; Bourguignon, Jean-Jacques; Schmitt, Martine; Frossard, Nelly published an article in 2021, the title of the article was Design, synthesis and biological evaluation of arylpyridin-2-yl guanidine derivatives and cyclic mimetics as novel MSK1 inhibitors. An application in an asthma model.Category: imidazoles-derivatives And the article contains the following content:

In order to identify new MSK1 inhibitors, a screening of a library of low mol. weight compounds was performed, and the results highlighted the I [R = phenyl] ( IC50~18μM) as a starting hit for structure-activity relationship study. Derivatives, homologues and rigid mimetics of I [R = Ph, 2-furanyl, 3-pyridine, etc.] were designed, and all synthesized compounds were evaluated for their inhibitory activity towards MSK1. Among them, the non-cytotoxic 2-aminobenzimidazole was the most potent at inhibiting significantly: (i) MSK1 activity, (ii) the release of IL-6 in inflammatory conditions in vitro (IC50~2μM) and (iii) the inflammatory cell recruitment to the airways in a mouse model of asthma. The experimental process involved the reaction of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one(cas: 40644-16-4).Category: imidazoles-derivatives

The Article related to arylpyridinyl guanidine preparation msk1 inhibitor antiasthmatic cytotoxicity sar, msk1, pyridine-2-yl guanidine, asthma, inflammation, kinase inhibitors, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On June 30, 2016, Koppala, Srinivasarao; Ranga Reddy, V.; Anireddy, Jaya Shree published an article.Electric Literature of 73590-85-9 The title of the article was Development and validation of a novel stability-indicating RP-HPLC method for the simultaneous determination of related substances of ketoprofen and omeprazole in combined capsule dosage form. And the article contained the following:

A novel, simple, sensitive, selective and reproducible stability-indicating high performance liquid chromatog. method was developed for the quant. determination of degradation products and process-related impurities of ketoprofen (KET) and omeprazole (OMZ) in combined oral solid dosage form. Chromatog. separation was achieved on a Phenomenex Luna C18 (2) column (150 × 4.6 mm, 5 μm) under gradient elution by using a binary mixture of potassium dihydrogen phosphate buffer and acetonitrile at a flow rate of 0.8 mL/min. Chromatogram was monitored at 233 nm for KET impurities and at 305 nm for OMZ impurities using a dual wavelength UV detector. Resolution for KET and OMZ and 14 impurities was found to be >1.5 for any pair of components. Typical retention behaviors of impurities at various pH values were depicted graphically. To prove the stability-indicating power of the method, the drug product was subjected to hydrolytic, oxidative, photolytic, humidity and thermal stress conditions as per ICH. The developed method was validated according to the current ICH guidelines for specificity, limit of detection, limit of quantification, linearity, accuracy, precision, ruggedness and robustness. The experimental process involved the reaction of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole(cas: 73590-85-9).Electric Literature of 73590-85-9

The Article related to ketoprofen omeprazole capsule rp hplc, Pharmaceutical Analysis: Synthetic Organic Compounds and other aspects.Electric Literature of 73590-85-9

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Liu, Hong; Li, Yuan; Chen, Yan; Zhao, Haipeng published an article in 2015, the title of the article was Main component self-comparison with calibration factor method for determination of related substances in Omeprazole Enteric Capsules.Product Details of 73590-85-9 And the article contains the following content:

Objective: To establish the main component self-comparison with calibration factor method to determine the contents of related substances in Omeprazole Enteric Capsules. Methods: An Agilent HC-C8 column (4.6 mm × 250 mm, 5 μm) was adopted with the mobile phase composed of 0.01 mol·L-1 disodium hydrogen phosphate (adjusted to pH 7.6 with phosphoric acid) and acetonitrile in the ratio of 75:25 pumped at a flow rate of 1.0 mL·min-1. The detection was carried out at 280 nm and a column temperature of 35°C. The injection volume was 20 μL. The slope of linear equation was used to determine the correction factor between impurities A, B, C, D and omeprazole. The relative retention time was used to determine the position of impurities. Results: The relative retention time between impurities A, B, C, D and omeprazole was 0.27, 0.31, 0.41 and 0.79, resp. The correction factor of impurities A, B, C, D was 1.20, 0.58, 0.57 and 1.04, resp. The content of impurity D was 0.022% in three batches of samples. Other impurities were not detected. Conclusion: The method is simple, efficient and accurate for analyzing the related substances in Omeprazole Enteric Capsules. The experimental process involved the reaction of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole(cas: 73590-85-9).Product Details of 73590-85-9

The Article related to omeprazole enteric capsule related substance, Pharmaceutical Analysis: Synthetic Organic Compounds and other aspects.Product Details of 73590-85-9

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem