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 class of inhibitors of this enzyme. The design, synthesis, and biological activity of these compounds are reported.
Hubschwerlen
C
C
Pharma Division, Preclinical Research, F. Hoffmann-La Roche Ltd., Basal, Switzerland.
Pflieger
P
P
Specklin
J L
JL
Gubernator
K
K
Gmünder
H
H
Angehrn
P
P
Kompis
I
I
D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000138:chemical synthesis; D011744:Pyrimidinones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
D001562:Benzimidazoles; D004791:Enzyme Inhibitors; D011744:Pyrimidinones; D059005:Topoisomerase II Inhibitors