IN-VITRO ANTIMYCOBACTERIAL ACTIVITIES OF PYRAZINAMIDE ANALOGS

We synthesized various pyrazine derivatives and pyrazinamide analogs a nd assayed their antimycobacterial activities in vitro in order to fin d new drugs which are more active against Mycobacterium tuberculosis t han pyrazinamide and also active against Mycobacterium avium and Mycob acterium intracellulare. Of the drugs synthesized, four drugs, namely, pyrazine thiocarboxamide, N-hydroxymethyl pyrazine thiocarboxamide, p yrazinoic acid n-octyl ester, and pyrazinoic acid pivaloyloxymethyl es ter, were not only bacteriostatic but also bacteriocidal against these three species of mycobacteria in vitro under conditions in which pyra zinamide showed no or little activity. In conclusion, these four drugs are possible candidates for new antimycobacterial agents, and animal experiments are now under way.