Novel antileishmanial chalconoids: Synthesis and biological activity of 1- or 3-(6-chloro-2H-chromen-3-yl)propen-1-ones

被引：50

作者：

Nazarian, Zohreh ^{[1
]}

Emami, Saeed ^{[2
,3
]}

Heydari, Samaneh ^{[4
]}

Ardestani, Sussan K. ^{[5
]}

Nakhjiri, Maryam ^{[1
]}

Poorrajab, Fatemeh ^{[5
]}

Shafiee, Abbas ^{[1
]}

Foroumadi, Alireza ^{[1
,4
]}

机构：

[1] Univ Tehran Med Sci, Res Ctr, Fac Pharm & Pharmaceut Sci, Tehran 14174, Iran

[2] Mazandaran Univ Med Sci, Fac Pharm, Dept Med Chem, Sari, Iran

[3] Mazandaran Univ Med Sci, Fac Pharm, Pharmaceut Sci Res Ctr, Sari, Iran

[4] Univ Tehran Med Sci, Drug Design & Dev Res Ctr, Tehran 14174, Iran

[5] Univ Tehran, Inst Biochem & Biophys, Dept Biochem, Tehran, Iran

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 45卷 / 04期

关键词：

Chromene; Chalcones; Leishmania major; Antileishmanial activity; VITRO LEISHMANICIDAL ACTIVITY; VISCERAL LEISHMANIASIS; CUTANEOUS LEISHMANIASIS; DERIVATIVES; MILTEFOSINE; DONOVANI;

D O I：

10.1016/j.ejmech.2009.12.046

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel chalconoids containing a 6-chloro-2H-chromen-3-yl group were prepared through a convenient and efficient synthetic method by using 5-chloro-2-hydroxybenzaldehyde as starting material. The target compounds were evaluated against the promastigote form of Leishmania major using MTT assay. All of the evaluated compounds have shown high in vitro antileishmanial activity at concentrations less than 3.0 mu M. The results of cytotoxicity assessment against mouse peritoneal macrophage cells showed that these compounds display antileishmanial activity at non-cytotoxic concentrations. (C) 2009 Elsevier Masson SAS. All rights reserved.

引用

页码：1424 / 1429

页数：6

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