Synthesis and biological evaluation of pyrimidine analogs of antimycobacterial purines.
Pyrimidine analogs of antimycobacterial 6-aryl-9-benzylpurines have been synthesized and screened for antibacterial activity against Mycobacterium tuberculosis H(37)Rv in vitro. Several active compounds were identified and the best results were observed for 5-formamidopyrimidines. These compounds generally displayed IC(90) values < or =1microg/mL, and they exhibited low toxicity towards mammalian cells. Imidazolylpyrimidines, which may be regarded as fleximer analogs of the parent purines, were also synthesized and one of them was found to be quite a potent inhibitor of M. tuberculosis (IC(90) 14microg/mL).
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Matthew L
ML
Department of Chemistry, University of Oslo, Blindern, N-0315 Oslo, Norway.
Braendvang
Morten
M
Miranda
Pedro O
PO
Gundersen
Lise-Lotte
LL
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011687:Purines / Q000494:pharmacology; D011743:Pyrimidines / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship
D000900:Anti-Bacterial Agents; D011687:Purines; D011743:Pyrimidines