The series of new 4-substituted picolinohydrazonamides were synthesized (6-25) and evaluated for tuberculostatic activity. Compounds having a hydrophilic cyclic amine such as morpholine and pyrrolidine at the end of the thiosemicarbazide chain, exhibited the highest antimycobacterial activity. The antimycobacterial activity of compounds 6, 11, and 15 (MIC 0.4-0.8 μg/mL) was higher than that of reference drugs. Moreover, derivative 15 exhibited lower activity against other tested microorganism such as bacteria gram-positive, gram-negative or fungi. Thus, this compound is characterized by the selectivity of antimicrobial activity. Antiproliferative study conducted against human dermal fibroblasts (HDF) and mouse melanoma cell line (B16-F10) revealed low cytotoxicity of compound 15. Conducted research allowed to identify compound 15 as leading for further research.

中文翻译：

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4-取代的picolinooazonamides作为一类新的潜在抗结核药。

合成了一系列新的4-取代的吡咯并酰肼酰胺（6-25），并评估了其抑菌活性。在硫代氨基脲链的末端具有亲水环胺的化合物，例如吗啉和吡咯烷，表现出最高的抗分枝杆菌活性。化合物6、11和15（MIC 0.4-0.8μg/ mL）的抗分枝杆菌活性高于参考药物。此外，衍生物15表现出对其他测试微生物如革兰氏阳性，革兰氏阴性或真菌的较低活性。因此，该化合物的特征在于抗微生物活性的选择性。针对人类皮肤成纤维细胞（HDF）和小鼠黑素瘤细胞系（B16-F10）进行的抗增殖研究表明，化合物15的细胞毒性较低。