Syntheses of novel antimycobacterial combinatorial libraries of structurally diverse substituted pyrimidines by three-component solid-phase reactions

被引：58

作者：

Kumar, A

Sinha, S

Chauhan, PMS ^{[1
]}

机构：

[1] Cent Drug Res Inst, Div Med Chem, Lucknow 226001, Uttar Pradesh, India

[2] Cent Drug Res Inst, Div Biochem, Lucknow 226001, Uttar Pradesh, India

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(01)00829-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new pyrimidine based scaffold has been developed by three-component solid-phase syntheses. The utility of scaffolds was demonstrated by synthesizing libraries of 80 substituted pyrimidines 12(a-p), 13(a p), 14(a p), 15(la-p), 16(a-p). Among 80 compounds screened, six compounds, 12i, 13c, 14d, 14e, 14o, and 15d showed in vitro activity against Mycobacterium tuberculosis (MABA) at a concentration of 50 and 25 mug/mL. (C) 2002 Elsevier Science Ltd. All rights reserved.

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页码：667 / 669

页数：3

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