title: 6-Oxo and 6-thio purine analogs as antimycobacterial agents.
abstract: 6-Oxo and 6-thio analogs of purine were prepared based on the initial activity screening of a small, diverse purine library against Mycobacterium tuberculosis (Mtb). Certain 6-oxo and 6-thio-substituted purine analogs described herein showed moderate to good inhibitory activity. N(9)-substitution apparently enhances the anti-mycobacterial activity in the purine series described herein. Several 2-amino and 2-chloro purine analogs were also synthesized that showed moderate inhibitory activity against Mtb.
authors: Drug Discovery Division, Southern Research Institute, 2000 9th Avenue South, Birmingham, AL 35205, USA. pathaka@southernresearch.org
authors: Ashish K
authors: AK
authors: Pathak
authors: Vibha
authors: V
authors: Pathak
authors: Lainne E
authors: LE
authors: Seitz
authors: William J
authors: WJ
authors: Suling
authors: Robert C
authors: RC
authors: Reynolds
mesh_terms: D000818:Animals; D000995:Antitubercular Agents / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D006801:Humans; D051379:Mice; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects*; D011687:Purines / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use* / Q000633:toxicity; D013438:Sulfhydryl Compounds / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use / Q000633:toxicity; D014376:Tuberculosis / Q000188:drug therapy*; D014709:Vero Cells
chemical_list: D000995:Antitubercular Agents; D011687:Purines; D013438:Sulfhydryl Compounds