Antimycobacterial activity of 1-deaza-7,8-dihydropteridine derivatives against Mycobacterium tuberculosis and Mycobacterium avium complex in vitro.

Twenty-five 1-deaza-7,8-dihydropteridine derivatives were screened for antimycobacterial activity against Mycobacterium tuberculosis strain H37Ra and three Mycobacterium avium clinical isolates (serovar 1, 4 or 6). Antibacterial activity was determined with a colorimetric microdilution broth assay. Seventeen of the compounds inhibited growth in the range >1.28 to <or=12.8 mg/L against one or more of the test strains. The presence of an alkoxycarbonyl group on the amino nitrogen at position 2 was not required for activity. Activity was dependent upon the type and location of group substitutions on the 6-phenyl ring and, in some cases, the presence of a 7-alkyl group.