Combinatorial approach to lead optimization of a novel hexapeptide with antifungal activity

被引：16

作者：

Kundu, B ^{[1
]}

Rastogi, SK

Batra, S

Raghuwanshi, SK

Shukla, PK

机构：

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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(00)00343-7

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Three sets of sublibraries of an antifungal lead peptide His-D-Trp-D-Phe-Phe-D-Phe-Lys-NH2 (I) have been prepared by introducing variations at positions 1, 4 and 6. They were screened for their antifungal activity against C. albicans and C. neoformans in order to quantify inhibition at each step of the hexapeptide sublibrary iteration. The studies led to the identification of Arg-D-Trp-D-Phe-Ile-D-Phe-His-NH2 as a novel hexapeptide with potent antifungal activity against both C. albicans and C. neoformans. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：1779 / 1781

页数：3

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