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...

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Bibliographic Details
Published in:Journal of medicinal chemistry 1978-08, Vol.21 (8), p.781-784
Main Authors: Cavalleri, Bruno, Volpe, Giancarlo, Arioli, Vittorio, Pizzocheri, Fabio, Diena, Alberto
Format: Article
Language:English
Subjects:
Animals
Antitrichomonal Agents - chemical synthesis
Antitrichomonal Agents - pharmacology
Antitrichomonal Agents - therapeutic use
Clostridium perfringens - drug effects
Drug Interactions
Hexobarbital - pharmacology
Male
Mice
Microbial Sensitivity Tests
Mycoplasma - drug effects
Nitroimidazoles - chemical synthesis
Nitroimidazoles - pharmacology
Nitroimidazoles - therapeutic use
Pentylenetetrazole - antagonists & inhibitors
Sleep - drug effects
Staphylococcus aureus - drug effects
Streptococcus pyogenes - drug effects
Strychnine - antagonists & inhibitors
Trichomonas Infections - drug therapy
Trichomonas vaginalis - drug effects
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Summary: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.
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00206a012