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
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container_end_page 1392
container_issue 8
container_start_page 1385
container_title Journal of medicinal chemistry
container_volume 35
creator Hubschwerlen, C
Pflieger, P
Specklin, J L
Gubernator, K
Gmünder, H
Angehrn, P
Kompis, I
description 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.
doi_str_mv 10.1021/jm00086a006
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subjects Benzimidazoles - chemical synthesis
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Enzyme Inhibitors - chemical synthesis
Pyrimidinones - chemical synthesis
Pyrimidinones - chemistry
Pyrimidinones - pharmacology
Structure-Activity Relationship
Topoisomerase II Inhibitors
title Pyrimido[1,6-a]benzimidazoles: a new class of DNA gyrase inhibitors
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