Synthesis and anti-mycobacterial evaluation of some pyrazine-2-carboxylic acid hydrazide derivatives.

摘要

A series of pyrazine-2-carboxylic acid hydrazide derivatives were synthesized and screened for their activity against Mycobacterium tuberculosis. The results show that pyrazine-2-carboxylic acid hydrazide-hydrazone derivatives 3a-l were less active than pyrazinamide. In contrast, the N(4)-ethyl-N(1)-pyrazinoyl-thiosemicarbazide 4 showed the highest activity against M. tuberculosis H(37)Rv (IC(90) = 16.87 microg/mL). Details of the structure-activity and structure-cytotoxicity relationships are discussed.