Synthesis, Antimycobacterial, Antifungal and Photosynthesis-Inhibiting Activity of Chlorinated N-phenylpyrazine-2-carboxamides †
作者:Martin Dolezal、Jan Zitko、Zdenek Osicka、Jiri Kunes、Marcela Vejsova、Vladimir Buchta、Jiri Dohnal、Josef Jampilek、Katarina Kralova
DOI:10.3390/molecules15128567
日期:——
prepared compounds were characterized and evaluated for their antimycobacterial and antifungal activity, and for their ability to inhibit photosynthetic electron transport (PET). 6-Chloro-N-(4-chlorophenyl)pyrazine-2-carboxamide manifested the highest activity against Mycobacterium tuberculosis strain H37Rv (65% inhibition at 6.25 μg/mL). The highest antifungal effect against Trichophyton mentagrophytes
通过取代吡嗪羧酸的氯化物与环取代(氯)苯胺的缩合,合成了一系列具有 -CONH- 连接基团连接吡嗪和苯环的 16 种吡嗪酰胺类似物。对制备的化合物进行表征并评估其抗分枝杆菌和抗真菌活性,以及抑制光合电子传递 (PET) 的能力。6-Chloro-N-(4-chlorophenyl)pyrazine-2-carboxamide 对结核分枝杆菌菌株 H37Rv 表现出最高的活性(6.25 μg/mL 时抑制率为 65%)。6-氯-5-叔丁基-N-(3,4-二氯苯基)吡嗪-2-甲酰胺对须癣毛癣菌(测试的最敏感的真菌菌株)具有最高的抗真菌作用(MIC=62.5 μmol/L) . 6-氯-5-叔丁基-N-(4-氯苯基)吡嗪-2-甲酰胺在菠菜叶绿体 (Spinacia oleracea L.) 叶绿体中表现出最高的 PET 抑制作用 (IC50=43.0 μmol/L)。对于所有化合物,讨论了所