克鲁兹锥虫
化学
喹啉酮
喹唑啉
药品
苯硝唑
硝呋替莫
杀锥虫剂
组合化学
恰加斯病
药理学
医学
病毒学
寄生虫寄主
计算机科学
万维网
作者
Mariela Bollini,Ana M. Bruno,María E. Niño,Juan J. Casal,Leandro D. Sasiambarrena,Damián A.G. Valdez,Leandro Battini,Vanesa Puente,Marı́a Elisa Lombardo
出处
期刊:Medicinal Chemistry
日期:2018-10-08
卷期号:15 (3): 265-276
被引量:8
标识
DOI:10.2174/1573406414666181005145042
摘要
Chagas disease affects about 7 million people worldwide. Only two drugs are currently available for the treatment for this parasite disease, namely, benznidazol (Bzn) and nifurtimox (Nfx). Both drugs have limited curative power in the chronic phase of the disease. Therefore, continuous research is an urgent need so as to discover novel therapeutic alternatives.The development of safer and more efficient therapeutic anti-T. cruzi drugs continues to be a major goal in trypanocidal chemotherapy.Synthesis, 2D-QSAR and drug-like physicochemical properties of a set of quinazolinone and quinazoline derivatives were studied as trypanocidal agents. All compounds were screened in vitro against Trypanosoma cruzi (Tulahuen strain, Tul 2 stock) epimastigotes and bloodstream trypomastigotes.Out of 34 compounds synthesized and tested, six compounds (5a, 5b, 9b, 9h, 13f and 13p) displayed significant activity against both epimastigotes and tripomastigotes, without exerting toxicity on Vero cells.The antiprotozoal activity of these quinazolinone and quinazoline derivatives represents an interesting starting point for a medicinal chemistry program aiming at the development of novel chemotherapies for Chagas disease.
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