Pharmaceutical Sciences Graduate Program (PPGCS), Federal University of Sergipe, São Cristóvão, Sergipe 49100-001, Brazil.
Institute of Chemistry and Biotechnology, Federal University of Alagoas, AC Simões Campus, Lourival Melo Mota Avenue, s/n, 57072-970 Maceió, Brazil.
Bioorg Med Chem Lett. 2022 Nov 1;75:128930. doi: 10.1016/j.bmcl.2022.128930. Epub 2022 Aug 24.
Chagas disease and Human African trypanosomiasis (HAT) are caused by Trypanosoma cruzi, T. brucei rhodesiense or T. b. gambiense parasites, respectively; while Leishmania is caused by parasites from the Leishmania genus. In recent years, many efforts have been addressed to develop inhibitors against these parasites, especially nitro-containing derivatives, which can interfere with essential enzymes from the protozoa. In this review, all anti-trypanosomatidae nitrocompounds reported so far are shown herein, highlighting their activities and SAR analyses, providing all the benefits and problems associated with this ambiguous chemical group. Finally, this review paper will be useful for many research teams around the world, which are searching for novel trypanocidal and leishmanicidal agents.
恰加斯病和非洲人类锥虫病（HAT）分别由克氏锥虫、罗得西亚锥虫或冈比亚锥虫寄生虫引起；而利什曼病是由利什曼原虫属的寄生虫引起的。近年来，人们已经做出了许多努力来开发针对这些寄生虫的抑制剂，特别是含硝基的衍生物，这些衍生物可以干扰原生动物的必需酶。在这篇综述中，本文展示了迄今为止报道的所有抗锥虫硝基化合物，强调了它们的活性和 SAR 分析，提供了与这个模糊的化学基团相关的所有好处和问题。最后，这篇综述文章将对全世界许多研究团队有用，这些团队正在寻找新型的杀锥虫和杀利什曼原虫药物。
