Design and synthesis of novel triazole antifungal derivatives based on the active site of fungal lanosterol 14a-demethylase (CYP51)

Autor:	Zhi Gang Dan, Jun Zhang, Honggang Hu, Qiu Ye Wu, Shi Chong Yu, Qing Yan Sun, Xiao Yun Chai
Rok vydání:	2009
Předmět:	biology Stereochemistry Lanosterol Triazole Active site General Chemistry biology.organism_classification In vitro Aspergillus fumigatus chemistry.chemical_compound chemistry biology.protein medicine Proton NMR Demethylase Fluconazole medicine.drug
Zdroj:	Chinese Chemical Letters. 20:935-938
ISSN:	1001-8417
DOI:	10.1016/j.cclet.2009.03.027
Popis:	A series of 1-(1H-1,2,4-triazole-1-yl)-2-(2,4-difluorophenyl)-3-(N-isoproyl-N-substituted-amino)-2-propanols have been designed and synthesized on the basis of the active site of lanosterol 14a-demethylase (CYP51). Their structures were confirmed by MS and 1H NMR. In vitro antifungal activities of these synthesized compounds were evaluated against eight human pathogenic fungi. The results showed that all title compounds exhibited activity against fungi tested to some extent. Compounds 3c, 3d, 7a, 7b and 7c exhibited more potent antifungal activities against nearly all fungi tested except Aspergillus fumigatus than fluconazole.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_________::1b4d7a512f3f5b95b09e684bdf4fb1cb https://doi.org/10.1016/j.cclet.2009.03.027 Zobrazit plný text záznamu Full Text from ScienceDirect