Chemotherapeutic nitroheterocycles. 18. 2-(5-Nitro-2-imidazolylmethylene)-1-indanones, -1-tetralones, and -acetophenones substituted by aminoalkoxy groups.
2-(5-Nitro-2-imidazolylmethylene)-1-indanones, -1-tetralones, and -acetophenones substituted by aminoalkoxy groups and related compounds (41-69, table ii) were synthesized and their antimicrobial activities were evaluated (table iii). Some of these compounds (e.g. 47, 52, and 59) suprisingly exhibited a broad antibacterial spectrum including Proteus species and Pseudomonas aeruginosa. Extraordinary antitrichomonal activities could also be observed in vitro (MIC of compound 59, 0.0004 pg/ml) and six of the title compounds (48, 49, 52, 58, 64, 66) displayed in vivo activity in mice against Trichomonas vaginalis comparable to that of metronidazole (70).
D000098:Acetophenones / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D000994:Antitrichomonal Agents / Q000494:pharmacology / Q000627:therapeutic use; D004748:Entamoeba histolytica / Q000187:drug effects; D013293:Enterococcus faecalis / Q000187:drug effects; D007189:Indans / Q000138:chemical synthesis* / Q000494:pharmacology; D007192:Indenes / Q000138:chemical synthesis*; D007711:Klebsiella pneumoniae / Q000187:drug effects; D051379:Mice; D008826:Microbial Sensitivity Tests; D009281:Naphthalenes / Q000138:chemical synthesis* / Q000494:pharmacology; D009593:Nitroimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011513:Proteus mirabilis / Q000187:drug effects; D011514:Proteus vulgaris; D013210:Staphylococcus / Q000187:drug effects; D014245:Trichomonas Infections / Q000188:drug therapy; D014246:Trichomonas vaginalis / Q000187:drug effects
D000098:Acetophenones; D000900:Anti-Bacterial Agents; D000994:Antitrichomonal Agents; D007189:Indans; D007192:Indenes; D009281:Naphthalenes; D009593:Nitroimidazoles