PYRIMIDO[1,6-A]BENZIMIDAZOLES - A NEW CLASS OF DNA GYRASE INHIBITORS

被引:59
作者
HUBSCHWERLEN, C [1 ]
PFLIEGER, P [1 ]
SPECKLIN, JL [1 ]
GUBERNATOR, K [1 ]
GMUNDER, H [1 ]
ANGEHRN, P [1 ]
KOMPIS, I [1 ]
机构
[1] F HOFFMANN LA ROCHE LTD, PRECLIN RES, DIV PHARMA, CH-4002 BASEL, SWITZERLAND
关键词
D O I
10.1021/jm00086a006
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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-a]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.
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页码:1385 / 1392
页数:8
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