New "ofloxacin" type antibacterial agents. Incorporation of the spiro cyclopropyl group at N-1
- 1 October 1988
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 31 (10) , 2004-2008
- https://doi.org/10.1021/jm00118a026
Abstract
The first example incorporating a spiro cyclopropyl group into an "ofloxacin" type of quinolone antibacterial agent has been prepared by potassium fluoride mediated ring closure of the hydroxymethyl cyclopropyl intermediate to give 9''-fluoro-7''-oxo-10''-(1-piperazinyl)spiro[cyclopropane-1,3''(2''H)-[7H]pyrido[1,2,3-de][1,4]benzoxazine]-6''-carboxylic acid. Analogues were made by substitution at C-7 by various complex amines. Evaluation of these compouns for antibacterial activity was carried out. All examples prepared and examined showed in vitro minimum inhibitory values and in vivo mouse protection results to be diminished as compared to the parent, ofloxacin.This publication has 10 references indexed in Scilit:
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