Giarolla Jeanine, Ferreira Elizabeth Igne
Av. Prof. Lineu Prestes, 580 - Bloco 13 sup., Cidade Universitaria, Sao Paulo, SP 05508-900, Brasil.
Mini Rev Med Chem. 2015;15(3):220-42. doi: 10.2174/138955751503150312122523.
Neglected tropical diseases (NTD) are a group of 17 diseases transmitted by virus, protozoa, helminthes and bacteria. These illnesses are responsible for millions of deaths per year, affecting mainly the poorest populations in the world. The therapeutic drugs available are obsolete, toxic, have questionable efficacy and there are reports of resistance. Therefore, the discovery of new, safe, effective and affordable active molecules is urgently needed. Considering that, the main purpose of this mini-review is to show the current scenario concerning drug design for neglected disease in Brazil. NTD are a very broad topic. Thus, we selected four infections for discussion: Chagas disease, leishmaniasis, malaria and tuberculosis. According to CNPq (National Counsel of Technological and Scientific Development) directories, there are many Brazilian groups studying these respective diseases. The papers published possess high quality and some of them, the most recent, are briefly discussed here. Medicinal chemistry approaches such as synthesis of novel series of molecules and biological activity evaluation, studies of structure-activity relationships (qualitative and quantitative), molecular modeling calculations and electrochemistry are some of the tools applied in the design of the compounds.
被忽视的热带病(NTD)是一组由病毒、原生动物、蠕虫和细菌传播的17种疾病。这些疾病每年导致数百万人死亡,主要影响世界上最贫困的人群。现有的治疗药物过时、有毒、疗效存疑,且有耐药性报告。因此,迫切需要发现新的、安全、有效且负担得起的活性分子。考虑到这一点,本综述的主要目的是展示巴西被忽视疾病药物设计的现状。被忽视的热带病是一个非常广泛的话题。因此,我们选择了四种感染进行讨论:恰加斯病、利什曼病、疟疾和结核病。根据巴西国家科技发展委员会(CNPq)的名录,有许多巴西研究团队在研究这些各自的疾病。发表的论文质量很高,其中一些最新的论文在此进行简要讨论。药物化学方法如新型分子系列的合成与生物活性评估、构效关系(定性和定量)研究、分子模拟计算和电化学是化合物设计中应用的一些工具。