Antitrichomonal activity of mesoionic thiazolo[3,2-a]pyridines.
Screening of mesoionic compounds as potential electron acceptors by analogy with metronidazole led to the finding of in vitro antitrichomonal activity for anhydro-2-phenyl-3-hydroxythiazolo [3,2-a]pyridinium hydroxide (1). In a series of analogues, potent in vitro activity was found to be associated with amino substitution; however, such activity was dependent on specific structural features and not on the reduction potential. The most active compounds showed only poor in vivo activity.
D000818:Animals; D055598:Chemical Phenomena; D002621:Chemistry; D006224:Cricetinae; D005260:Female; D008647:Mesocricetus; D008795:Metronidazole / Q000494:pharmacology / Q000627:therapeutic use; D011725:Pyridines / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D011726:Pyridinium Compounds / Q000138:chemical synthesis / Q000494:pharmacology / Q000627:therapeutic use; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology* / Q000627:therapeutic use; D014244:Trichomonas / Q000187:drug effects*; D014245:Trichomonas Infections / Q000188:drug therapy*
D011725:Pyridines; D011726:Pyridinium Compounds; D013844:Thiazoles; D008795:Metronidazole; C047239:anhydro-2-phenyl-3-hydroxythiazolo(3,2-a)pyridinium