Month: April 2022

Fuss, Andreas; Koch, Volker published an article about the compound: 2-Bromo-5-chloropyridin-3-ol( cas:127561-70-0,SMILESS:OC1=CC(Cl)=CN=C1Br ).Related Products of 127561-70-0. Aromatic heterocyclic compounds can be classified according to the number of heteroatoms or the size of the ring. The authors also want to convey more information about this compound (cas:127561-70-0) through the article.

The nucleophilic addition of 3-hydroxypyridine to F2C:CFCF3 gave 73% 3-[(1,1,2,3,3,3-pentafluoropropyl)oxy]pyridine. The preparation of other 3-[(fluoroalkyl)oxy]pyridines from polyfluoroalkenes and hydroxpyridine derivatives is described.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Formula: C7H7NO2. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 6-Methylnicotinic acid, is researched, Molecular C7H7NO2, CAS is 3222-47-7, about Discovery of quinolone derivatives as antimycobacterial agents. Author is Liu, Kun-Lin; Teng, Fei; Xiong, Lu; Li, Xiao; Gao, Chao; Yu, Luo-Ting.

In this report, a compound library was screened and identified compound I with antituberculosis activity and a minimal inhibitory concentration (MIC) against M. tuberculosis of 20μg mL-1. Structure optimization and the structure-activity relationship of 1 as the lead compound enabled the design and synthesis of a series of quinolone derivatives, e.g, II. These compounds were evaluated in vitro for anti-tubercular activity against the M. tuberculosis H37Rv strain. Among them, compounds III [n = 1; R = 3′,5′-dimethoxy-[1,1′-biphenyl], 4-(trifluoromethyl)phenyl, 6-(trifluoromethyl)pyridin-3-yl (IV)] exhibited MIC values in the range of 1.2-3μg mL-1 and showed excellent activity against the tested MDR-TB strain (MIC: 3, 2.9 and 0.9μg mL-1, resp.). All three compounds III were non-toxic toward A549 and Vero cells (>100 and >50μg mL-1, resp.). In addition, an antibacterial spectrum test carried out using compound (IV) showed that this compound specifically inhibits M. tuberculosis. These can serve as a new starting point for the development of anti-TB agents with therapeutic potential.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Tian, Jinlong; Sun, Nannan; Yu, Mingcheng; Gu, Xianfeng; Xie, Qiong; Shao, Liming; Liu, Jin; Liu, Li; Wang, Yonghui published the article 《Discovery of N-indanyl benzamides as potent RORγt inverse agonists》. Keywords: indanylbenzamide ROR gammat inverse agonist Th17 autoimmune disease drug; Autoimmune diseases; Binding modes; N-indanyl benzamides; RORγt inverse agonists; Th17 cells.They researched the compound: 6-Methylnicotinic acid( cas:3222-47-7 ).Application of 3222-47-7. Aromatic heterocyclic compounds can be divided into two categories: single heterocyclic and fused heterocyclic. In addition, there is a lot of other information about this compound (cas:3222-47-7) here.

The retinoic acid receptor-related orphan receptor-gamma-t (RORγt) is a promising therapeutic target for treatment of Th17 cell-mediated autoimmune diseases. Based on a scaffold hopping/conformational restriction strategy, a series of N-indanyl benzamides as novel RORγt inverse agonists was discovered. Exploration of structure-activity relationship on the piperazine ring, benzoyl moiety and cyclopentyl moiety of N-indanyl benzamides 2a and 2d led to identification of potent RORγt inverse agonists. Compound 5c with (S)-enantiomer was found having an IC50 of 153.7 nM in Fluorescence Resonance Energy Transfer (FRET) assay, and an IC50 of 47.1 nM in mouse Th17 cell differentiation assay, which represents a promising starting point for developing potent small mol. RORγt inverse agonists. Binding modes of the two enantiomers 5c and 5d in RORγt ligand binding domain were also discussed.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

The preparation of ester heterocycles mostly uses heteroatoms as nucleophilic sites, which are achieved by intramolecular substitution or addition reactions. Compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone( cas:86404-63-9 ) is researched.Product Details of 86404-63-9.Wang, Yan; Damu, Guri L. V.; Lv, Jing-Song; Geng, Rong-Xia; Yang, Da-Cheng; Zhou, Cheng-He published the article 《Design, synthesis and evaluation of clinafloxacin triazole hybrids as a new type of antibacterial and antifungal agents》 about this compound( cas:86404-63-9 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: clinafloxacin triazole hybrid preparation antibacterial antifungal. Let’s learn more about this compound (cas:86404-63-9).

A series of clinafloxacin triazole hybrids as a new type of antibacterial and antifungal agents were synthesized for the first time and screened for their antimicrobial efficacy against four Gram-pos. bacteria, four Gram-neg. bacteria, and two fungi by two fold serial dilution technique. The bioactive assay indicated that most of the target compounds displayed broad antimicrobial spectrum and good antibacterial and antifungal activities with low MIC values ranging from 0.25 to 2 μg/mL against all the tested strains which exhibited comparable or even better efficiency in comparison with the reference drugs Chloramphenicol, Clinafloxacin, and Fluconazole, resp. Notably, some synthesized clinafloxacin triazoles showed stronger efficacy against methicillin-resistant Staphylococcus aureus than their parent Clinafloxacin.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 188781-36-4. Aromatic heterocyclic compounds can also be classified according to the number of heteroatoms contained in the heterocycle: single heteroatom, two heteroatoms, three heteroatoms and four heteroatoms. Compound: 5-Chloro-6-methylpyrazine-2-carboxylic acid, is researched, Molecular C6H5ClN2O2, CAS is 188781-36-4, about Corrigendum: MPX-004 and MPX-007: new pharmacological tools to study the physiology of NMDA receptors containing the GluN2A subunit [Erratum to document cited in CA168:122429]. Author is The PLOS ONE Staff.

There is an error in affiliation 1 for authors Robert A. Volkmann, Christopher M. Fanger, David R. Anderson, Frank S. Menniti. Affiliation 1 should be: Mnemosyne Pharmaceuticals, Inc. (now Luc Therapeutics) 400 Technol. Square, Cambridge, MA 02139, United States of America

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 86404-63-9. Aromatic compounds can be divided into two categories: single heterocycles and fused heterocycles. Compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, is researched, Molecular C10H7F2N3O, CAS is 86404-63-9, about Design, synthesis, and biological evaluation of novel triazole derivatives as inhibitors of cytochrome P450 14α-demethylase. Author is Chai, Xiaoyun; Zhang, Jun; Hu, Honggang; Yu, Shichong; Sun, Qingyan; Dan, Zhigang; Jiang, Yuanying; Wu, Qiuye.

Based on the results of computational docking to the active site of the cytochrome P 450 14α-demethylase (CYP51), a series of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols I (R = H, 2-F, 2,4-Cl2, 4-MeO2C, PhO2C, etc.) as analogs of fluconazole were designed, synthesized, and evaluated as antifungal agents. The MIC80 values indicate that compounds I (R = H, 2-F, 4-Me, etc.) exhibited higher activity against nearly all fungi tested except Aspergillus fumigatus than fluconazole, while I (R = COOR1, R1 = Me, Et, iso-Pr, COOAr, etc.; Ar = Ph, 3-O2NC6H4, 4-ClC6H4, 2-MeO2CC6H4, etc.) showed no activity or only moderate activity against all fungi tested. Noticeably, the MIC value of I (R = H, 2-F, 4-Cl) is 64 times lower than that of fluconazole against Microsporum gypseum in vitro. And I (R = H, 2-F, CO2Et) showed 128 times higher activity (with the MIC80 value of 0.0039 μg/mL) than that of fluconazole against Candida albicans and also showed higher activity than that of the other pos. controls. Computational docking experiments indicated that the inhibition of CYP51 involves a coordination bond with iron of the heme group, the hydrophilic H-bonding region, the hydrophobic region, and the narrow hydrophobic cleft. In addition, the activity of the compounds would be enhanced when the side chains were shorter.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

SDS of cas: 86404-63-9. The reaction of aromatic heterocyclic molecules with protons is called protonation. Aromatic heterocycles are more basic than benzene due to the participation of heteroatoms. Compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, is researched, Molecular C10H7F2N3O, CAS is 86404-63-9, about 7-Fluoro-2-(prop-2-en-1-ylsulfanyl)-3-(1H-1,2,4-triazol-1-yl)-4H-thiochromen-4-one. Author is Liu, Dong Liang; Xiao, Tao; Li, Yang; Yu, Guang Yan; Li, Chen.

The asym. unit of the title compound, C14H10FN3OS2, contains two independent mols. which differ in the relative orientations of the triazole and allylsulfanyl groups with respect to the planar thiochromen-4-one frameworks. The N-N-C-C torsion angles are 128.2(5) and -120.9(5)°, while the C-S-C-S torsion angles are -17.4(4) and 16.4(4)°. In the crystal, intermol. C-H···O and C-H···N hydrogen bonds link the mols. in a stacked arrangement along the a axis.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 4-(4-Bromophenyl)-5-methylthiazol-2-amine, is researched, Molecular C10H9BrN2S, CAS is 65705-44-4, about Unique Sulfur-Aromatic Interactions Contribute to the Binding of Potent Imidazothiazole Indoleamine 2,3-Dioxygenase Inhibitors.Related Products of 65705-44-4.

Indoleamine 2,3-dioxygenase (IDO1) inhibitors are speculated to be useful in cancer immunotherapy, but a phase III clin. trial of the most advanced IDO1 inhibitor, epacadostat, did not meet its primary endpoint and was abandoned. In previous work we identified the novel IDO1 inhibitor N-(4-chlorophenyl)-2-((5-phenylthiazolo[2,3-c][1,2,4]triazol-3-yl)thio)acetamide 1 through high-throughput screening (HTS). Herein, we report a structure-activity relationship (SAR) study of this compound, which resulted in the potent IDO1 inhibitor 1-(4-cyanophenyl)-3-(3-(cyclopropylethynyl)imidazo[2,1-b]thiazol-5-yl)thiourea 47 (hIDO IC50 = 16.4 nM). X-ray co-crystal structural anal. revealed that the basis for this high potency is a unique sulfur-aromatic interaction network formed by the thiourea moiety of 47 with the F163 and F226. This finding is expected to inspire new approaches towards the discovery of potent IDO1 inhibitors in the future.

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1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Heterocyclic compounds can be divided into two categories: alicyclic heterocycles and aromatic heterocycles. Compounds whose heterocycles in the molecular skeleton cannot reflect aromaticity are called alicyclic heterocyclic compounds. Compound: 86404-63-9, is researched, Molecular C10H7F2N3O, about Novel antifungal 2-aryl-1-(1H-1,2,4-triazol-1-yl)butan-2-ol derivatives with high activity against Aspergillus fumigatus, the main research direction is aryltriazolylbutanol preparation fungicide; triazolylbutanol aryl preparation fungicide; voriconazole preparation fungicide.Related Products of 86404-63-9.

Replacement of one triazole ring of fluconazole with 4-pyridinyl leads to an increase in activity against Aspergillus fumigatus. Introduction of an α-Me group has a marked addnl. beneficial effect. Investigation of pyridinyl and pyrimidinyl analogs resulted in the identification of compound I (UK-109,496, voriconazole) which has excellent potency against a broad range of fungal pathogens including A. fumigatus and Candida krusei.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Recommanded Product: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone. The fused heterocycle is formed by combining a benzene ring with a single heterocycle, or two or more single heterocycles. Compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, is researched, Molecular C10H7F2N3O, CAS is 86404-63-9, about Novel triazole alcohol antifungals derived from fluconazole: design, synthesis, and biological activity. Author is Hashemi, Seyedeh Mahdieh; Badali, Hamid; Faramarzi, Mohammad Ali; Samadi, Nasrin; Afsarian, Mohammad Hosein; Irannejad, Hamid; Emami, Saeed.

A series of new triazole alc. antifungals were designed by replacing one of the triazolyl moiety from fluconazole with a distinct 4-amino-3-mercapto-1,2,4-triazole motif, which is found in some antimicrobial agents. The antimicrobial susceptibility testing of target compounds demonstrated that the direct analogs of fluconazole (difluorophenethyl-triazoles) were less active against fungi, while compound 10h containing dichloro substitutions on both Ph rings of the mol. had potent activity against yeasts including Candida albicans (four strains) and Cryptococcus neoformans (MICs = 2-8 μg/mL). Also, compound 10h was active against Candida parapsilosis, Epidermophyton floccosum, and Trichophyton mentagrophytes, while it showed no activity against Gram-pos. and Gram-neg. bacteria. Finally, a mol. docking study suggested that compound 10h interacts suitably with lanosterol 14α-demethylase, which is the key enzyme in ergosterol biosynthesis.

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Reference:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics