A series of isoxazole and triazole derivatives, with interesting bioactive scaffolds, were examined for their in vitro antibacterial, antifungal, and antiprotozoal activities. These compounds exhibited antitrypanosomal activity comparable to difluoromethylornithine (DMFO), a drug used in the treatment of human African trypanosomiasis. Isoxazole analogs 1, 3, and 4, and triazole derivatives 16, 17, 28, 37, 40, and 42 showed the highest antitrypanosomal activity with IC₅₀ values of 17.89, 1.82, 10.38, 10.26, 11.77, 9.29, 3.93, 2.11, and 0.93 µM, respectively. Compounds 40 and 42 showed the most potent activity against Leishmania donovani amastigotes with IC₅₀ values of 18.28 and 10.54 µM, respectively. Compound 42 showed the most potent activity against Leishmania donovani macrophage internalized amastigotes with an IC₅₀ value of 8.32 µM. Conjugate triazoles 40–43 displayed potential antimalarial activity against chloroquine-resistant W2 and chloroquine-sensitive D6 Plasmodium falciparum strains (IC₅₀ value range from 0.58 to 8.36 µM). Compound 37 showed antibacterial activity against Staphylococcus aureus, MRSA, and Mycobacterium intracellulare with IC₅₀ values of 15.53, 14.22, and 47.45 µM, respectively. None of the compounds exhibited antifungal activity.

中文翻译：

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评价三唑和异恶唑衍生物作为潜在的抗感染药。

研究了一系列具有有趣生物活性支架的异恶唑和三唑衍生物的体外抗菌，抗真菌和原生动物活性。这些化合物显示出与二氟甲基鸟氨酸（DMFO）相当的抗锥虫活性，DMFO是一种用于治疗人类非洲锥虫病的药物。异恶唑类似物1，3，和4，和三唑衍生物16，17，28，37，40，和42显示出最高的抗锥体虫活性，IC _50个的17.89值，1.82，10.38，10.26，11.77，9.29，3.93，2.11，和0.93 µM。化合物40和42表现出最强的抗倒钩利什曼原虫活性，IC ₅₀值分别为18.28和10.54 µM。化合物42对Leishmania donovani巨噬细胞内化的变形虫表现出最强的活性，IC ₅₀值为8.32 µM。共轭三唑40 – 43对耐氯喹的W2和对氯喹敏感的D6恶性疟原虫菌株具有潜在的抗疟活性（IC ₅₀值范围从0.58至8.36 µM）。化合物37显示出对以下细菌的抗菌活性金黄色葡萄球菌，MRSA和细胞内分枝杆菌的IC ₅₀值分别为15.53、14.22和47.45 µM。这些化合物均未显示出抗真菌活性。