Design, synthesis & evaluation of condensed 2H-4-arylaminopyrimidines as novel antifungal agents

被引：23

作者：

Jain, Kishor S. ^{[1
]}

Khedkar, Vijay M. ^{[2
]}

Arya, Nikhilesh ^{[1
]}

Rane, Prasad V. ^{[3
]}

Chaskar, Pratip K. ^{[4
]}

Coutinho, Evans C. ^{[2
]}

机构：

[1] Sinhgad Inst Pharmaceut Sci, Dept Pharmaceut Chem, Pune 410401, Maharashtra, India

[2] Bombay Coll Pharm, Dept Pharmaceut Chem, Bombay 400098, Maharashtra, India

[3] RJSPMs Coll Pharm, Dept Pharmaceut Chem, Pune 412105, Maharashtra, India

[4] Vivekanand Educ Soc Coll Pharm, Dept Pharmaceut Chem, Bombay 400074, Maharashtra, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2014年 / 77卷

关键词：

Antifungal activity; Condensed pyrimidines; Docking; Lanosterol; 14-alpha-demethylase; MWI; SAR;

D O I：

10.1016/j.ejmech.2014.02.066

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 P-450 family, lanosterol 14 alpha-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. (c) 2014 Elsevier Masson SAS. All rights reserved.

引用

页码：166 / 175

页数：10

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