title: Pyrimido[1,6-a]benzimidazoles: a new class of DNA gyrase inhibitors.
abstract: 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.
authors.affiliation: Pharma Division, Preclinical Research, F. Hoffmann-La Roche Ltd., Basal, Switzerland.
authors.forename: C
authors.initials: C
authors.lastname: Hubschwerlen
authors.forename: P
authors.initials: P
authors.lastname: Pflieger
authors.forename: J L
authors.initials: JL
authors.lastname: Specklin
authors.forename: K
authors.initials: K
authors.lastname: Gubernator
authors.forename: H
authors.initials: H
authors.lastname: Gmünder
authors.forename: P
authors.initials: P
authors.lastname: Angehrn
authors.forename: I
authors.initials: I
authors.lastname: Kompis
mesh_terms: 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
chemical_list: D001562:Benzimidazoles; D004791:Enzyme Inhibitors; D011744:Pyrimidinones; D059005:Topoisomerase II Inhibitors