São Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, SP, Brazil.
Med Chem. 2020;16(1):24-38. doi: 10.2174/1573406415666190620141109.
More than 10 million people around the world are afflicted by Neglected Tropical Diseases, such as Chagas Disease, Human African Trypanosomiasis, and Leishmania. These diseases mostly occur in undeveloped countries that suffer from a lack of economic incentive, research, and policy for new compound development. Sulfonamide moieties are effective scaffolds present in several compounds that are determinants to treat various diseases, principally neglected tropical diseases. This review article examines the contribution of these scaffolds in medicinal chemistry in the last five years, focusing on three trypanosomatid parasites: Trypanosoma cruzi, Trypanosoma brucei, and Leishmania ssp. We also present perspectives for their use in drug designs in an effort to contribute to new drug development. In addition, we consider the physicochemical parameters, whose molecules all presented according to Lipinski's rule. The correlation between the selective index and LogP was evaluated, showing that sulfonamide derivatives can act differently against each trypanosomatid parasite. Moreover, the approaches of novel drugs and technologies are very important for the eventual drug discovery against trypanosomatid diseases.
全世界有超过 1000 万人患有被忽视的热带病，如恰加斯病、非洲人类锥虫病和利什曼病。这些疾病主要发生在经济激励、研究和新化合物开发政策缺乏的欠发达国家。磺胺部分是几种化合物中的有效支架，这些化合物是治疗各种疾病的决定因素，主要是被忽视的热带病。本文综述了这些支架在过去五年中在药物化学中的贡献，重点关注三种锥虫寄生虫：克氏锥虫、布氏锥虫和利什曼原虫。我们还提出了将它们用于药物设计的观点，以有助于新药物的开发。此外，我们还考虑了根据 Lipinski 规则呈现的所有分子的物理化学参数。评估了选择性指数与 LogP 之间的相关性，表明磺胺衍生物对每种锥虫寄生虫的作用不同。此外，新型药物和技术的方法对于最终发现针对锥虫疾病的药物非常重要。
