Continuous efforts have been made to discover new drugs for the treatment of Chagas’ disease, human African trypanosomiasis, and leishmaniasis. We have previously reported the synthesis and antileishmanial and antitrypanosomal (Y strain) properties of 2,3-disubstituted quinoxalines. Considering their promising antiparasitic potential, the present study was conducted to expand our search and take advantage of high-throughput assays to investigate the effects of quinoxaline derivatives against Leishmania donovani, Trypanosoma brucei, and Trypanosoma cruzi (Tulahuen strain). These compounds were active against the kinetoplastid parasites that were evaluated. The 2-chloro-3-methylsulfoxylsulfonyl and 2-chloro-3-methylsulfinyl quinoxalines were the most potent, and some of these derivatives were even more active than the reference drugs. Although the 2,3-diaryl-substituted quinoxalines were not active against all of the parasites, they were active against T. brucei and intracellular amastigotes of T. cruzi, without interfering with mammalian cell viability. These compounds presented encouraging results that will guide our future studies on in vivo bioassays towards the mode of action.

人们一直在努力寻找治疗南美锥虫病，人类非洲锥虫病和利什曼病的新药。我们先前已经报道了2,3-二取代喹喔啉的合成，抗衰老和抗锥虫（Y菌株）特性。考虑到它们潜在的抗寄生虫潜力，本研究旨在扩大我们的搜索范围，并利用高通量分析方法研究喹喔啉衍生物对利什曼原虫，诺氏锥虫和克鲁氏锥虫的影响。（图拉胡恩株）。这些化合物对所评估的运动质体寄生虫具有活性。2-氯-3-甲基亚磺酰基磺酰基和2-氯-3-甲基亚磺酰基喹喔啉是最有效的，这些衍生物中的一些甚至比参考药物具有更高的活性。尽管2,3-二芳基取代的喹喔啉对所有寄生虫均无活性，但它们对布鲁氏锥虫和克氏锥虫的胞内变形虫均具有活性，而不会干扰哺乳动物细胞的生存能力。这些化合物提供了令人鼓舞的结果，这些结果将指导我们将来在体内生物测定方面的研究朝着作用方式发展。