Zhao, Qing-Jie published the artcileDesign, synthesis, and antifungal activities of novel 1H-triazole derivatives based on the structure of the active site of fungal lanosterol 14α-demethylase (CYP51), Related Products of triazoles, the publication is Chemistry & Biodiversity (2007), 4(7), 1472-1479, database is CAplus and MEDLINE.
A series of fluconazole analogs I (R2 = H, R4 = H; R2 = Me, R4 = H; R2 = H, R4 = Me; R2 = F, R4 = H; R2 = H, R4 = F; R2 = Cl, R4 = H; R2 = H, R4 = Cl; R2 = Br, R4 = H; R2 = H, R4 = Br; R2 = H, R4 = CMe3; R2 = F, R4 = F) were prepared and assayed for antifungal activity. They were designed by computational docking experiments to the active site of the cytochrome P 450 14α-sterol demethylase (CYP51), whose crystal structure is known. Preliminary biol. tests showed that most of the target compounds exhibit significant activities against the eight most-common pathogenic fungi. Thereby, the most potent congener, 1-[(4-tert-butylbenzyl)(cyclopropyl)amino]-2-(2,4-difluorophenyl)-3-(1H-1,2,4-triazol-1-yl)propan-2-ol I (R2 = H, R4 = CMe3), was found to exhibit a broad antifungal spectrum, being more active against Candida albicans, Candida tropicalis, Cryptococcus neoformans, Microsporum canis, and Trichophyton rubrum (MIC80<0.125 μg/mL) than the standard clin. drug itraconazole. The observed affinities of the lead mols. towards CYP51 indicate that a cyclopropyl residue enhances binding to the target enzyme. These results may provide some guidance for the development of novel triazole-based antifungal lead structures.
Chemistry & Biodiversity published new progress about 86386-77-8. 86386-77-8 belongs to triazoles, auxiliary class Epoxides,Triazole,Fluoride,Salt,Sulfonic acid,Benzene, name is 1-((2-(2,4-Difluorophenyl)oxiran-2-yl)methyl)-1H-1,2,4-triazole methanesulfonate, and the molecular formula is C13H12BClO3, Related Products of triazoles.
Referemce:
https://en.wikipedia.org/wiki/1,2,3-Triazole,
Triazoles – an overview | ScienceDirect Topics