کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1361151 981458 2008 9 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and exploration of novel curcumin analogues as anti-malarial agents
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and exploration of novel curcumin analogues as anti-malarial agents
چکیده انگلیسی

Curcumin, a major yellow pigment and active component of turmeric, has been shown to possess anti-inflammatory and anti-cancer activities. Recent studies have indicated that curcumin inhibits chloroquine-sensitive (CQ-S) and chloroquine-resistant (CQ-R) Plasmodium falciparum growth in culture with an IC50 of ∼3.25 μM (MIC = 13.2 μM) and IC50 4.21 μM (MIC = 14.4 μM), respectively. In order to expand their potential as anti-malarials a series of novel curcumin derivatives were synthesized and evaluated for their ability to inhibit P. falciparum growth in culture. Several curcumin analogues examined show more effective inhibition of P. falciparumgrowth than curcumin. The most potent curcumin compounds 3, 6, and 11 were inhibitory for CQ-S P. falciparum at IC50 of 0.48, 0.87, 0.92 μM and CQ-R P. falciparum at IC50 of 0.45 μM, 0.89, 0.75 μM, respectively. Pyrazole analogue of curcumin (3) exhibited sevenfold higher anti-malarial potency against CQ-S and ninefold higher anti-malarial potency against CQ-R. Curcumin analogues described here represent a novel class of highly selective P. falciparum inhibitors and promising candidates for the design of novel anti-malarial agents.

Novel curcumin analogues were prepared and evaluated for its anti-malarial activity against CQ-S and CQ-R Plasmodium falciparum culture. Compound 3, 6 and 11 were found to be the most potent analogue with IC50 values 0.48, 0.87, and 0.92 μM against CQ-S and 0.45, 0.89, and 0.75 μM against CQ-R.Figure optionsDownload as PowerPoint slide

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 6, 15 March 2008, Pages 2894–2902
نویسندگان
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