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Journal of Antimicrobial Chemotherapy (2001) 47, 451-454
© 2001 The British Society for Antimicrobial Chemotherapy

Brief report

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

William J. Suling,* and Joseph A. Maddry

Drug Discovery Division, Southern Research Institute, 2000 Ninth Avenue South, Birmingham, AL 35205, USA

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 <=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.

* Corresponding author. Tel: +1-205-581-2558; Fax: +1-205-581-2877; E-mail: suling{at}sri.org


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