Abstract：
:A series of quinolone and naphthyridine antibacterial agents possessing as the C7-heterocycle bicyclic 2,5-diazabicyclo[n.2.m]alkanes, where n = 2, 3 and m = 1, 2, and a series including 4-aminopiperidine and 3-amino-8-azabicyclo[3.2.1]octanes have been prepared and evaluated in vitro and in vivo for antibacterial activity against a variety of Gram-negative and Gram-positive organisms. These compounds were also tested against the target enzyme bacterial DNA gyrase. All the examples investigated are nearly equipotent with the parent 7-piperazinyl analogues. Only endo-7-(3-amino-8-azabicyclo[3.2.1]oct-8-yl)-1-cyclopropyl-6,8-difluoro- 1,4- dihydro-4-oxo-3-quinolinecarboxylic acid displays activity that surpasses that of the piperazine parent.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Kiely JS,Hutt MP,Culbertson TP,Bucsh RA,Worth DF,Lesheski LE,Gogliotti RD,Sesnie JC,Solomon M,Mich TFdoi
10.1021/jm00106a029subject
Has Abstractpub_date
1991-02-01 00:00:00pages
656-63issue
2eissn
0022-2623issn
1520-4804journal_volume
34pub_type
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