Synthesis, antimalarial and antitubercular activity of acetylenic chalcones

被引：150

作者：

Hans, Renate H. ^{[1
]}

Guantai, Eric M. ^{[1
]}

Lategan, Carmen ^{[2
]}

Smith, Peter J. ^{[2
]}

Wan, Baojie ^{[3
]}

Franzblau, Scott G. ^{[3
]}

Gut, Jiri ^{[4
]}

Rosenthal, Philip J. ^{[4
]}

Chibale, Kelly ^{[1
,5
]}

机构：

[1] Univ Cape Town, Dept Chem, ZA-7701 Rondebosch, South Africa

[2] Univ Cape Town, Div Pharmacol, ZA-7925 Observatory, South Africa

[3] Univ Illinois, Coll Pharm, Inst TB Res, Chicago, IL 60612 USA

[4] Univ Calif San Francisco, San Francisco Gen Hosp, Dept Med, San Francisco, CA 94143 USA

[5] Univ Cape Town, Inst Infect Dis & Mol Med, ZA-7701 Rondebosch, South Africa

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 03期

基金：

新加坡国家研究基金会;

关键词：

Chalcones; Falcipain-2; P; falciparum; M; tuberculosis; MYCOBACTERIUM-TUBERCULOSIS; PLASMODIUM-FALCIPARUM; LICOCHALCONE-A; AGENTS; DERIVATIVES; DESIGN; INHIBITORS; GROWTH; ROOTS; ASSAY;

D O I：

10.1016/j.bmcl.2009.12.062

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of acetylenic chalcones were evaluated for antimalarial and antitubercular activity. The antimalarial data for this series suggests that growth inhibition of the W2 strain of Plasmodium falciparum can be imparted by the introduction of a methoxy group ortho to the acetylenic group. Most compounds were more active against non-replicating than replicating cultures of Mycobacterium tuberculosis H(37)Rv, an unusual pattern with respect to existing anti-TB agents. (c) 2009 Elsevier Ltd. All rights reserved.

引用

页码：942 / 944

页数：3

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