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ID: ALA3232951
Journal: Eur J Med Chem
Title: Design, synthesis & evaluation of condensed 2H-4-arylaminopyrimidines as novel antifungal agents.
Authors: Jain KS, Khedkar VM, Arya N, Rane PV, Chaskar PK, Coutinho EC.
Abstract: A small, focussed library of condensed 2H-4-arylaminopyrimidines, with 3-diversity points, based on an initial design by molecular docking study of this scaffold at the active site of the fungal enzyme of cytochrome P450 family, lanosterol 14α-demethylase (CYP51) was synthesized through a one-pot green chemical synthetic protocol. The screening of the synthesised compounds for antifungal activity against Candida albicans, Aspergillus fumigatus &Aspergillus niger revealed activity in many of the compounds as comparable to that of fluconazole. Based on the antifungal activity and physicochemical property data of these derivatives, a meaningful SAR has been proposed.
CiteXplore: 24631896