Month: October 2022

Frey, Felice; Sandakly, Jawdat; Ghannam, Mirna; Doueiry, Caren; Hugosson, Fredrik; Berlandi, Johannes; Ismail, Joy N.; Gayden, Tenzin; Hasselblatt, Martin; Jabado, Nada; Shirinian, Margret published an article in 2022, the title of the article was Drosophila tet is required for maintaining glial homeostasis in developing and adult fly brains.SDS of cas: 443-72-1 And the article contains the following content:

Ten-eleven translocation (TET) proteins are crucial epigenetic regulators highly conserved in multicellular organisms. TETs’ enzymic function in demethylating 5-Me cytosine in DNA is required for proper development and TETs are frequently mutated in cancer. Recently, Drosophila melanogaster Tet (dTet) was shown to be highly expressed in developing fly brains and discovered to play an important role in brain and muscle development as well as fly behavior. Furthermore, dTet was shown to have different substrate specificity compared with mammals. However, the exact role dTet plays in glial cells and how ectopic TET expression in glial cells contributes to tumorigenesis and glioma is still not clear. Here, we report a novel role for dTet specifically in glial cell organization and number We show that loss of dTet affects the organization of a specific glia population in the optic lobe, the “optic chiasm” glia. Addnl., we find irregularities in axon patterns in the ventral nerve cord (VNC) both, in the midline and longitudinal axons. These morphol. glia and axonal defects were accompanied by locomotor defects in developing larvae escalating to immobility in adult flies. Furthermore, glia homeostasis was disturbed in dTet-deficient brains manifesting in gain of glial cell numbers and increased proliferation. Finally, we establish a Drosophila model to understand the impact of human TET3 in glia and find that ectopic expression of hTET3 in dTet-expressing cells causes glia expansion in larval brains and affects sleep/rest behavior and the circadian clock in adult flies. The experimental process involved the reaction of N-Methyl-7H-purin-6-amine(cas: 443-72-1).SDS of cas: 443-72-1

The Article related to drosophila melanogaster tet glial homeostasis fly brain development, 6ma dna demethylation, drosophila ten-eleven translocation (tet), drosophila brain, brain tumor, human tet drosophila model, optic chiasm glia and other aspects.SDS of cas: 443-72-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On March 31, 2011, Buckman, Brad; Nicholas, John B.; Beigelman, Leonid; Serebryany, Vladimir; Stoycheva, Antitsa Dimitrova; Thrailkill, Timothy; Seiwert, Scott D. published a patent.Recommanded Product: 4-Bromo-1H-benzo[d]imidazol-2(3H)-one The title of the patent was Preparation of macrocyclic peptides, especially proline-containing peptides, as inhibitors of hepatitis C virus replication for treating hepatitis C infection and liver fibrosis. And the patent contained the following:

The invention is related to the preparation of title compounds, e.g., I [R1 = COOBu-t, (un)substituted (hetero)aryl, etc.; R2 = (un)substituted 1-alkylbenzimidazol-2-yloxy, 2-(4-isopropylthiazol-2-yl)-7-methoxy-8-methylquinazolin-4-yloxy, 5-aryl-2H-tetrazol-2-yl, etc.; R3 = OH, NHSO2R3a, NHSO2OR3a; NHSO2NR3bR3c; R3a = (un)substituted alkyl, aryl, cycloalkyl, etc.; R3b, R3c = independently H, (un)substituted alkyl, C6 or C10 aryl, etc.; or NR3bR3c = (un)substituted 3-6 membered heterocyclyl bonded to the parent structure through a N ; with provisos], pharmaceutical acceptable salts and prodrugs and their compositions containing them as inhibitors of hepatitis C virus replication. The invention is also related to methods of treating a hepatitis C virus infection and methods of treating liver fibrosis. Thus, II·HCl was prepared by a multi-step synthesis and displayed an EC50 between 10 and 100 nM and an IC50 < 10 nM in an NS3-NS4 inhibitory activity assay. The experimental process involved the reaction of 4-Bromo-1H-benzo[d]imidazol-2(3H)-one(cas: 40644-16-4).Recommanded Product: 4-Bromo-1H-benzo[d]imidazol-2(3H)-one

The Article related to cyclic peptide preparation hepatitis c virus replication inhibitor, ns3 ns4a protease inhibitor hcv infection fibrosis macrocycle preparation, proline peptide peptidomimetic preparation inhibitor hcv replication and other aspects.Recommanded Product: 4-Bromo-1H-benzo[d]imidazol-2(3H)-one

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

Floresta, Giuseppe; Fallica, Antonino Nicolo; Patamia, Vincenzo; Sorrenti, Valeria; Greish, Khaled; Rescifina, Antonio; Pittala, Valeria published an article in 2021, the title of the article was From Far West to East: Joining the Molecular Architecture of Imidazole-like Ligands in HO-1 Complexes.Safety of N-(3-Aminopropyl)-imidazole And the article contains the following content:

HO-1 overexpression has been reported in several cases/types of human malignancies. Unfortunately, poor clin. outcomes are reported in most of these cases, and the inhibition of HO-1 is considered a valuable and proven anticancer approach. To identify novel hit compounds suitable as HO-1 inhibitors, a fragment-based approach where ligand joining experiments were used was reported. The two most important parts of the classical structure of the HO-1 inhibitors were used as a starting point, and 1000 novel compounds were generated and then virtually evaluated by structure and ligand-based approaches. The joining experiments led to a novel series of indole-based compds I (R1 = Me, OMe, PhCH2O; R2 = H, OMe; R3 = Me, OMe, PhCH2). A synthetic pathway for eight selected mols. I was designed, and the compounds were synthesized. The biol. activity revealed that some mols. I reach the micromolar activity, whereas mol. I (R1 = PhCH2O; R2 = H; R3 = Me) inhibits the HO-1 with an IC50 of 1.03μM. This study suggested that joining approach was successful, and a novel hit compound I was generated. These results are ongoing for further development. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Safety of N-(3-Aminopropyl)-imidazole

The Article related to imidazolyl indole carboxamide preparation sar heme oxygenase inhibitor docking, ho-1 inhibitors, fragment growing, fragment-based ligand design, heme oxygenase, imidazole, ligand joining, structure-based drug design and other aspects.Safety of N-(3-Aminopropyl)-imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On January 1, 2017, Talsi, Evgenii P.; Bryliakov, Konstantin P. published an article.Category: imidazoles-derivatives The title of the article was Ti-Salan catalyzed asymmetric sulfoxidation of pyridylmethylthiobenzimidazoles to optically pure proton pump inhibitors. And the article contained the following:

The asym. sulfoxidation of two pyridylmethylthiobenzimidazoles to anti-ulcer drugs of the PPI family (S)-omeprazole and (R)-lansoprazole with hydrogen peroxide, mediated by a series of chiral titanium(IV) salan complexes was reported. High sulfoxide yields (up to >95%) and enantioselectivities (up to 94% ee) were achieved. The introduction of electron-withdrawing substituents leaded to less active and less enantioselective catalysts. Like for the previously reported Ti-salalen catalyzed sulfoxidations, the temperature dependence of the sulfoxidation enantioselectivity in the presence of Ti-salan complexes was nonmonotonic, demonstrating isoinversion behavior with decreasing temperature The oxidation was likely rate-limited by the formation of the active (presumably peroxotitanium(IV)) species, followed by a faster oxygen transfer to the substrate. The experimental process involved the reaction of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole(cas: 73590-85-9).Category: imidazoles-derivatives

The Article related to titanium salan complex catalyst preparation, pyridylmethylthiobenzimidazole titanium salan complex catalyst sulfoxidation, pyridylmethyl benzimidazolyl sulfoxide preparation chemoselective enantioselective green chem and other aspects.Category: imidazoles-derivatives

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On July 29, 2020, Darwish, Ghinwa H.; Asselin, Jeremie; Tran, Michael V.; Gupta, Rupsa; Kim, Hyungki; Boudreau, Denis; Algar, W. Russ published an article.Synthetic Route of 5036-48-6 The title of the article was Fully Self-Assembled Silica Nanoparticle-Semiconductor Quantum Dot Supra-Nanoparticles and Immunoconjugates for Enhanced Cellular Imaging by Microscopy and Smartphone Camera. And the article contained the following:

There is a growing need for brighter luminescent materials to improve the detection and imaging of biomarkers. Relevant contexts include low-abundance biomarkers and technol.-limited applications, where an example of the latter is the emerging use of smartphones and other nonoptimal but low-cost and portable devices for point-of-care diagnostics. One approach to achieving brighter luminescent materials is incorporating multiple copies of a luminescent material into a larger supra-nanoparticle (supra-NP) assembly. Here, the authors present a facile method for the preparation and immunoconjugation of supra-NP assemblies (SiO2@QDs) that comprised many quantum dots (QDs) around a central silica nanoparticle (SiO2 NP). The assembly was entirely driven by spontaneous affinity interactions between the constituent materials, which included imidazoline-functionalized silica nanoparticles, ligand-coated QDs, imidazole-functionalized dextran, and tetrameric antibody complexes (TACs). The phys. and optical properties of the SiO2@QDs were characterized at both the ensemble and single-particle levels. Notably, the optical properties of the QDs were preserved upon assembly into supra-NPs, and single SiO2@QDs were approx. an order of magnitude brighter than single QDs and nonblinking. In proof-of-concept applications, including selective immunolabeling of breast cancer cells, the SiO2@QDs provided higher sensitivity and superior signal-to-background ratios whether using research-grade fluorescence microscopy or smartphone-based imaging. Overall, the SiO2@QDs are promising materials for enhanced bioanal. and imaging. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Synthetic Route of 5036-48-6

The Article related to silica nanoparticle semiconductor quantum dot immunoconjugate cell imaging smartphone, cellular imaging, immunolabeling, quantum dots, self-assembly, silica nanoparticles, smartphone device, tetrameric antibody complex and other aspects.Synthetic Route of 5036-48-6

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On February 15, 2020, Wang, Yixuan; Zhou, Rui; Quan, Yanni; Chen, Shumin; Shi, Xingpeng; Li, Yanping; Cen, Shan published an article.Safety of N-(3-Aminopropyl)-imidazole The title of the article was Design, synthesis, and evaluation of novel 4-amino-2-(4-benzylpiperazin-1-yl)methylbenzonitrile compounds as Zika inhibitors. And the article contained the following:

The prevalence of Zika virus (ZIKV) has become widespread in recent years. ZIKV infection is associated with severe congenital CNS malformations in both newborns and adults. However, neither vaccines nor therapeutics are available to control ZIKV infection until now. The authors started by hit screening the authors’ inhouse small mol. library, then designed, synthesized, and evaluated a new class of 1,4-bibenzyl-substituted piperazine derivatives for their cytopathic effect (CPE) protection effect in a ZIKV-infected Vero E6 cellular assay. A preliminary structure-activity relation study identified five novel 4-amino-2-(4-benzylpiperazin-1-yl)methylbenzonitrile analogs with obvious CPE reduction effects against ZIKV at micromolar concentrations Moreover, 2-((4-(2-chlorobenzyl)piperazin-1-yl)methyl)-4-((2(dimethylamino)ethyl)(methyl)amino)benzonitrile exerted a significant antiviral effect on both Zika RNA replication and virus protein expression in a dose-dependent manner at low micromolar concentrations This study demonstrated the potential of a novel 4-amino-2-(4-benzylpiperazin-1-yl)methylbenzonitrile scaffold for the development of anti-ZIKV candidates. The experimental process involved the reaction of N-(3-Aminopropyl)-imidazole(cas: 5036-48-6).Safety of N-(3-Aminopropyl)-imidazole

The Article related to aminobenzylpiperazinylmethylbenzonitrile preparation zika inhibitor, 4-amino-2-(4-benzylpiperazin-1-yl)methylbenzonitrile, antiviral, cytopathic effect, structure-activity relationship, synthesis, zika virus inhibitors and other aspects.Safety of N-(3-Aminopropyl)-imidazole

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On March 13, 1979, Clark, Robert L.; Pessolano, Arsenio A.; Shen, Tsung-Ying published a patent.Quality Control of 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one The title of the patent was Imidazopyridin-2-ones and pharmaceutical compositions and methods of treatment. And the patent contained the following:

Imidazopyridines I [R = H, C2-6 alkenyl, C1-7 alkyl (substituted with C3-6 cycloalkyl, C1-5 alkoxy, or OH), C4-7 cycloalkyl; R1, R2, R4 = H, 5- or 6-F, 5- or 6-Cl, 5- or 6-C1-5 alkoxycarbonylamino; R1R2 = OCR5R6O (R5, R6 = H, alkyl)] were prepared by several methods. Also prepared were 3-heterocyclyl analogs of I and 2-thiono analogs of I. I and their analogs were analgesics, antipyretics, and antiinflammatory agents (no data). Thus, refluxing 2-chloro-3-nitropyridine with 3,4-(OCH2O)C6H3NH2 in NaOAc-AcOH 5 h gave nitropyridine II (R7 = NO2) which was hydrogenated over Pd/C in MeOH and the diamine II (R7 = NH2) cyclized with COCl2 overnight at room temperature to give I (R = R4 = H, R1R2 = 3,4-OCH2O), which was converted into a variety of I (R = alkyl, alkenyl, acyl, R1R2 = OCH2O, R4 = H). The experimental process involved the reaction of 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one(cas: 41010-50-8).Quality Control of 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one

The Article related to analgesic imidazopyridinone preparation, antipyretic imidazopyridinone preparation, antiinflammatory imidazopyridinone preparation, imidazopyridinone pharmaceutical preparation, aminoanilinopyridine cyclization phosgene and other aspects.Quality Control of 3-Phenyl-1H-imidazo[4,5-b]pyridin-2(3H)-one

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On March 31, 2009, Jiang, Biao; Zhao, Xiao-Long; Dong, Jia-Jia; Wang, Wan-Jun published an article.Formula: C17H19N3O2S The title of the article was Catalytic asymmetric oxidation of heteroaromatic sulfides with tert-butyl hydroperoxide catalyzed by a titanium complex with a new chiral 1,2-diphenylethane-1,2-diol ligand. And the article contained the following:

Heteroaromatic sulfoxides, especially 1H-benzimidazolyl pyridinylmethyl sulfoxides, usually used as the blockbuster gastric proton pump inhibitors (PPIs), have been prepared highly enantioselectivity by catalytic asym. oxidation of sulfides attached to nitrogen-containing heterocycles with tert-Bu hydroperoxide in the presence of a chiral titanium complex, formed in situ from Ti(iPrO)4, chiral 1,2-diphenylethane-1,2-diol and water. The chiral sulfoxides were obtained in high yield (97%) with excellent enantiomeric excess (up to 98%). The experimental process involved the reaction of 5-Methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridyl)methyl]thio]benzimidazole(cas: 73590-85-9).Formula: C17H19N3O2S

The Article related to benzimidazolyl pyridinylmethyl benzyl sulfide tertbutyl hydroperoxide titanium, chiral diphenylethane diol asym oxidation sulfoxide stereoselective preparation, asym oxidation catalyst titanium chiral diphenylethane diol and other aspects.Formula: C17H19N3O2S

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On August 18, 2008, Sun, Jiangtao; Yang, Minghua; Dai, Zhenya; Zhu, Chengjian; Hu, Hongwen published an article.Electric Literature of 73590-85-9 The title of the article was Synthesis of optically active 2,5-dialkylcyclohexane-1,4-diols and their application in the asymmetric oxidation of sulfides. And the article contained the following:

A simple and efficient approach to obtain optically pure 1,4-diols was established. The asym. oxidation of sulfides to sulfoxides with cumyl hydroperoxide in moderate yields and moderate to high enantioselectivities (≤84%) catalyzed by chiral Ti/1,4-diols complexes was achieved. An ee of 76% was obtained in the asym. synthesis of esomeprazole. 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 alkylcyclohexanediol resolution chiral ligand titanium catalyzed asym oxidation, sulfide asym oxidation titanium catalyst, thioether asym oxidation titanium catalyst, sulfoxide asym synthesis, esomeprazole asym synthesis and other aspects.Electric Literature of 73590-85-9

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem

On January 31, 2022, Li, Zhenwei; Xu, Qingqing; Ning, Huangfu; Chen, Xiaomin; Zhu, Jianhua published an article.Application of 443-72-1 The title of the article was Mettl3 promotes oxLDL-mediated inflammation through activating STAT1 signaling. And the article contained the following:

Atherosclerosis (AS) is the main cause of cerebrovascular diseases, and macrophages act important roles during the AS pathol. process through regulating inflammation. Modification of the novel N(6)-methyladenine (m6A) RNA is reported to be associated with AS, but its role in AS is largely unknown. The aim of this study was to investigate the role and mechanism of m6A modification in inflammation triggered by oxidized low-d. lipoprotein (oxLDL) in macrophages during AS. RAW264.7 macrophage cells were stimulated with 40μg/mL ox-LDL, Dot blot, Immunoprecipitation, western blot, Rip and chip experiments were used in our study. We found oxLDL stimulation significantly promoted m6A modification level of mRNA in macrophages and knockdown of Methyltransferase-Like Protein 3 (Mettl3) inhibited oxLDL-induced m6A modification and inflammatory response. Mettl3 promoted oxLDL-induced inflammatory response in macrophages through regulating m6A modification of Signal transducer and activator of transcription 1 (STAT1) mRNA, thereby affecting STAT1 expression and activation. Moreover, oxLDL stimulation enhanced the interaction between Mettl3 and STAT1 protein, promoting STAT1 transcriptional regulation of inflammatory factor expression in macrophages eventually. These results indicate that Mettl3 promotes oxLDL-triggered inflammation through interacting with STAT1 protein and mRNA in RAW264.7 macrophages, suggesting that Mettl3 may be as a potential target for the clin. treatment of AS. The experimental process involved the reaction of N-Methyl-7H-purin-6-amine(cas: 443-72-1).Application of 443-72-1

The Article related to mettl3 oxidized low density lipoprotein stat1 signaling inflammation atherosclerosis, n6-methyladenosine, atherosclerosis, inflammation, methyltransferase-like protein 3, signal transducer and activator of transcription 1 and other aspects.Application of 443-72-1

Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem