摘要 : Some pyrazinamide derivatives (2a-2e, 2a '-2e ', and 2a ''-2e '') were synthesized and evaluated as antimycobacterial agents against Mycobacterium tuberculosis H37Rv strain. These derivatives were designed by structural modificati... 展开 Some pyrazinamide derivatives (2a-2e, 2a '-2e ', and 2a ''-2e '') were synthesized and evaluated as antimycobacterial agents against Mycobacterium tuberculosis H37Rv strain. These derivatives were designed by structural modification of pyrazinamide with alkyl chains and six-membered hetereocylic rings, respectively. The title compounds were synthesized using pyrazinamide as the starting material for haloakylation (1a-1c), and then halo-alkylpyrazinamides were reacted with appropriate heterocyclic rings. The structures of compounds were confirmed by H-1 NMR, C-13 NMR, mass spectroscopy, and elemental analysis. The activity of pyrazinamide derivatives was assayed using microplate alamar blue assay (MABA) and characterized by minimum inhibitory concentrations (MICs). Results showed that the obtained pyrazinamide derivatives exhibited high inhibitory effect on M. tuberculosis. The antimycobacterial activity of compounds 2b ', 2d ', and 2e ' was the best among all compounds tested, and their MIC values were about 6.25 m mu/mL. These compounds have ethylene chain between pyrazinamide moiety and six-membered hetereocylic rings. 收起