High selective leishmanicidal activity of 3-hydroxy-2-methylene-3-(4-bromophenyl)propanenitrile and analogous compounds

被引：42

作者：

de Souza, R. O. M. A.

Pereira, V. L. P.

Muzitano, M. F.

Falcao, C. A. B.

Rossi-Bergmann, B. ^{[1
]}

Filho, E. B. A.

Vasconcellos, M. L. A. A.

机构：

[1] Univ Fed Rio de Janeiro, Inst Biofis Carlos Chagas Filho, Rio De Janeiro, Brazil

[2] Univ Fed Paraiba, Dept Quim, BR-58059900 Joao Pessoa, Paraiba, Brazil

[3] Univ Fed Rio de Janeiro, BR-21941590 Rio De Janeiro, Brazil

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2007年 / 42卷 / 01期

关键词：

leishmanicide; Leishmania amazonensis; Baylis-Hillman adducts;

D O I：

10.1016/j.ejmech.2006.07.013

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

Sixteen not new aromatic compounds were prepared by one-pot reaction i.e. through Baylis-Hillman reaction and were the first time evaluated against promastigote Leishmania amazonensis and infected mammalian cells. Most of the compounds were selectively more active against amastigotes than the reference drug sodium stibogluconate (Pentostam, IC50 = 44.7 mu M). We found that 3-hydroxy-2-methylene-3-(4-broinophenyl)propanenitrile (13) was the most active (IC50 = 12.5 mu M) and safer compound (0.0 (0.9); % macrophage LDH release), being the lead compound. (c) 2006 Elsevier Masson SAS. All rights reserved.

引用

页码：99 / 102

页数：4

共 21 条

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