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Morita-Baylis-Hillman 加合物:生物活性和潜力发现新的更便宜的药物。

Morita-Baylis-Hillman adducts: biological activities and potentialities to the discovery of new cheaper drugs.

机构信息

Laboratório de Síntese Orgânica Medicinal da Paraíba (LASOM-PB), Departamento de Química, Universidade Federal da Paraíba, Campus I, João Pessoa PB 58059-900, Brazil.

出版信息

Bioorg Med Chem. 2012 Jul 1;20(13):3954-71. doi: 10.1016/j.bmc.2012.04.061. Epub 2012 May 9.

Abstract

This review aims to present by the first time the Morita-Baylis-Hillman adducts (MBHA) as a new class of bioactive compounds and highlight its potentialities to the discovery of new cheaper and efficient drugs. Now, most these compounds can be prepared fast and on a single synthetic step (one-pot reaction) in high yields and using ecofriendly synthetic protocols. We highlight here the aromatic MBHA, which have shown diverse biological activities as anti-Leishmania chagasi and Leishmania amazonensis (parasites that cause cutaneous and visceral leishmaniasis), anti-Trypanosoma cruzi (parasite that cause Chagas disease), anti-Plasmodium falciparum and Plasmodium berghei (parasites that cause malaria), lethal against Biomphalaria glabrata (the snail transmitter of schistosomiasis), antibacterial, antifungal, herbicide and actives against some human tumor cell lines. Understanding of the biological mechanisms of action of this new class of molecules is still in the infancy stage. However, we report here which has been described to date on the possibilities of biological mechanisms of action, and we present new analyzes based on literature in this area. The academic and industrial interest in selecting green and cheaper experiments to the drugs development has been the prime mover of the growth on the subject.

摘要

本次综述首次介绍了 Morita-Baylis-Hillman 加合物(MBHA)作为一类新的生物活性化合物,并强调了其在发现新型廉价、高效药物方面的潜力。现在,这些化合物大多数可以通过快速、单步(一锅反应)、高产率和使用环保的合成方案进行制备。我们在这里重点介绍芳香族 MBHA,它们表现出多种生物活性,如抗恰加斯锥虫(引起恰加斯病的寄生虫)、抗疟原虫 falciparum 和疟原虫 berghei(引起疟疾的寄生虫)、致死性抗巴西血吸虫(血吸虫病的传播蜗牛)、抗菌、抗真菌、除草剂以及对一些人肿瘤细胞系的活性。对这一类新分子的作用机制的理解仍处于起步阶段。然而,我们在这里报告了迄今为止关于作用机制的生物学可能性的描述,并根据该领域的文献提出了新的分析。学术界和工业界对选择绿色、廉价的实验来进行药物开发的兴趣是该领域增长的主要动力。

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