Category: Triazoles

Reference of 4-(4-Bromophenyl)-5-methylthiazol-2-amine. 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: 4-(4-Bromophenyl)-5-methylthiazol-2-amine, is researched, Molecular C10H9BrN2S, CAS is 65705-44-4, about Sequencing [4+1]-Cycloaddition and Aza-Michael Addition Reactions: A Diastereoselective Cascade for the Rapid Access of Pyrido[2′,1′:2,3]/Thiazolo[2′,3′:2,3]imidazo[1,5-a]quinolone Scaffolds as Potential Antibacterial and Anticancer Motifs. Author is Srinivasulu, Vunnam; Khanfar, Monther; Omar, Hany A.; ElAwady, Raafat; Sieburth, Scott McN; Sebastian, Anusha; Zaher, Dana M.; Al-Marzooq, Farah; Hersi, Fatema; Al-Tel, Taleb H..

The design and synthesis of a quality compound library containing a small number of skeletally diverse scaffolds, whose members rapidly deliver new chem. probes active against multiple phenotypes, is paramount in drug discovery. In this context, an efficient one-pot strategy for the synthesis of a mini library of sp3 enriched hexahydropyrido[2′,1′:2,3]imidazo[1,5-a]quinolinium and hexahydrothiazolo[2′,3′:2,3] imidazo[1,5-a]quinolinium architectures, is described. This new one-pot method features a combination of Sc(OTf)3-catalyzed [4+1]-cycloaddition with aza-Michael addition reactions.The cascade results in a rapid and diastereoselective formation of these scaffolds via desymmetrization of the oxidative-dearomatization products of phenols. Phenotypic screening of the mini library against multidrug resistant bacteria and a panel of cancer cell lines identified potential antibacterial and anticancer lead drug candidates.Further investigation of the anticancer leads, indicated their activity as tubulin-polymerization inhibitors, representing a promising approach for cancer therapy.

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

The reaction of an aromatic heterocycle with a proton is called a protonation. One of articles about this theory is 《1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanol》. Authors are Kesternich, Victor; Nelson-Gonzalez, Ronald; Perez-Fehrmann, Marcia; Cardenas, Alejandro; Brito, Ivan.The article about the compound:1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanonecas:86404-63-9,SMILESS:FC1=CC=C(C(CN2N=CN=C2)=O)C(F)=C1).Related Products of 86404-63-9. Through the article, more information about this compound (cas:86404-63-9) is conveyed.

In the title compound, C10H9F2N3O, the dihedral angle between the mean planes of the triazole and benzene rings is 20.6 (2)°. In the crystal, mols. are linked by strong O-H··· N hydrogen bonds into chains with graph-set notation C(9) along [100]. Weak C-H···N and C-H···F interactions are also observed Crystallog. data are given.

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

Formula: C10H7F2N3O. 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 Studies on synthesis, structure and biological activities of novel triazole compounds containing thioamide. Author is Xu, Liang-Zhong; Li, Wei-Hua; Li, Kai; Qin, Yong-Qi; Li, Chun-Li; Hou, Bao-Rong.

Four novel triazole compounds containing thioamide group were designed and synthesized by using triazole, Ph isothiocyanate and aryl Et ketones as starting materials. The desired intermediates were thus derivatives of α-(1H-1,2,4-triazol-1-yl)methyl ketones. Their structures were confirmed by elemental anal., 1H NMR, IR and MS spectra. The crystal structure of 1-[1-[(anilino)thiocarbonyl]-1-(4-fluorobenzoyl)methyl]-1,2,4-triazole [also, i.e., α-(fluorobenzoyl)-N-phenyl-1,2,4-triazole-1-ethanethioamide] has been determined by X-ray diffraction anal. The preliminary bioassays have shown that the title compounds exhibit certain antifungal activity.

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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: 127561-70-0, is researched, Molecular C5H3BrClNO, about Chemistry of 3-hydroxypyridine. Part 3. Synthesis of substituted 3-[fluoro(chloro)alkoxy]pyridines from halo- or amino-3-hydroxypyridines, the main research direction is fluoroalkene nucleophilic addition hydroxypyridine; pyridine fluoroalkyloxy.Related Products of 127561-70-0.

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

So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Zou, Yan; Zhao, Qingjie; Liao, Jun; Hu, Honggang; Yu, Shichong; Chai, Xiaoyun; Xu, Mingjuan; Wu, Qiuye researched the compound: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone( cas:86404-63-9 ).SDS of cas: 86404-63-9.They published the article 《New triazole derivatives as antifungal agents: Synthesis via click reaction, in vitro evaluation and molecular docking studies》 about this compound( cas:86404-63-9 ) in Bioorganic & Medicinal Chemistry Letters. Keywords: triazolylpropanol difluorophenyl fluconazole derivative preparation antifungal. We’ll tell you more about this compound (cas:86404-63-9).

A series of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-substituted-2-propanols, which are analogs of fluconazole, have been designed and synthesized via Cu(I)-catalyzed azide-alkyne cycloaddition on the basis of computational docking experiments to the active site of the cytochrome P 450 14α-demethylase (CYP51). The in vitro antifungal activities of all the target compounds were evaluated against eight human pathogenic fungi. 4-Methylbenzyl-substituted compound I showed the best antifungal activities.

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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: 1-(2,4-Difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)ethanone, is researched, Molecular C10H7F2N3O, CAS is 86404-63-9, about Synthesis of Schiff base having a heterocyclic moiety along with its cyclized derivatives and study of their antifungal activities.Electric Literature of C10H7F2N3O.

Synthesis of Schiff’s base 1-[(2,4-difluorophenyl)-2-(1H-1,2,4-triazol-1-yl)]ethanone thiosemicarbazone (I) prepared by condensation of 1-(2,4-difluorophenyl)-2-[1(H)-1,2,4-triazol-1-yl]ethanone with thiosemicarbazide is discussed. Further, I was cyclized using acetic anhydride to form triazolyl thiadiazoline II [R = C(O)CH3] and finally hydrolyzed using hydrazine hydrate to form thiadiazoline II [R = H]. All the synthesized compounds were tested for anti-fungal activity and most of the compounds were potent than the starting material as well as the known antifungal compound Fluconazole.

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