Pyrimido[1,6-a]benzimidazoles: a new class of DNA gyrase inhibitors

Pyrimido[1,6-a]benzimidazoles: a new class of DNA gyrase inhibitors

Substituted 4-quinolone- (1, A = CH) and 1,8-naphthyrid-4-one- (1, A = N) 3-carboxylic acids are currently the only classes of clinically useful antibacterial agents exerting their activity by inhibiting the subunit A of DNA gyrase. Pyrimido[1,6-alpha]benzimidazoles 11 have been found to be a new cl...

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Veröffentlicht in:Journal of medicinal chemistry 1992-04, Vol.35 (8), p.1385-1392
Hauptverfasser: Hubschwerlen, C, Pflieger, P, Specklin, J L, Gubernator, K, Gmünder, H, Angehrn, P, Kompis, I
Format: Artikel
Sprache:eng
Schlagworte:
Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Enzyme Inhibitors - chemical synthesis
Pyrimidinones - chemical synthesis
Pyrimidinones - chemistry
Pyrimidinones - pharmacology
Structure-Activity Relationship
Topoisomerase II Inhibitors
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Zusammenfassung:Substituted 4-quinolone- (1, A = CH) and 1,8-naphthyrid-4-one- (1, A = N) 3-carboxylic acids are currently the only classes of clinically useful antibacterial agents exerting their activity by inhibiting the subunit A of DNA gyrase. Pyrimido[1,6-alpha]benzimidazoles 11 have been found to be a new class of inhibitors of this enzyme. The design, synthesis, and biological activity of these compounds are reported.
ISSN:0022-2623
DOI:10.1021/jm00086a006