title: Synthesis and biological evaluation of pyrimidine analogs of antimycobacterial purines.
abstract: 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).
authors.affiliation: Department of Chemistry, University of Oslo, Blindern, N-0315 Oslo, Norway.
authors.forename: Matthew L
authors.initials: ML
authors.lastname: Read
authors.forename: Morten
authors.initials: M
authors.lastname: Braendvang
authors.forename: Pedro O
authors.initials: PO
authors.lastname: Miranda
authors.forename: Lise-Lotte
authors.initials: LL
authors.lastname: Gundersen
mesh_terms: 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
chemical_list: D000900:Anti-Bacterial Agents; D011687:Purines; D011743:Pyrimidines