Synthesis and biological activity of new 2-nitroimidazole derivatives.
In an earlier paper we described the synthesis and the antitrichomonas activity of 2-nitro-alpha,alpha,1-trimethyl-1H-imidazole-5-methanol (2). Starting from this compound, several derivatives have been synthesized. Among these, the phenyl carbonate 8 has been shown to possess activity equal to that of 2 and to be less toxic. This compound therefore is interesting in comparison with some antitrichomonas agents currently in use clinically. Before undertaking an in-depth investigation, compound 8 was subjected to some studies to see whether it has any effects on the central nervous system (CNS). Preliminary results show that, at therapeutic doses, it might induce unwanted CNS effects to a lesser degree than metronidazole.
D000818:Animals; D000994:Antitrichomonal Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D003016:Clostridium perfringens / Q000187:drug effects; D004347:Drug Interactions; D006591:Hexobarbital / Q000494:pharmacology; D008297:Male; D051379:Mice; D008826:Microbial Sensitivity Tests; D009174:Mycoplasma / Q000187:drug effects; D009593:Nitroimidazoles / Q000138:chemical synthesis* / Q000494:pharmacology / Q000627:therapeutic use; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors; D012890:Sleep / Q000187:drug effects; D013211:Staphylococcus aureus / Q000187:drug effects; D013297:Streptococcus pyogenes / Q000187:drug effects; D013331:Strychnine / Q000037:antagonists & inhibitors; D014245:Trichomonas Infections / Q000188:drug therapy; D014246:Trichomonas vaginalis / Q000187:drug effects
D000994:Antitrichomonal Agents; D009593:Nitroimidazoles; D006591:Hexobarbital; D013331:Strychnine; D010433:Pentylenetetrazole