The synthesis and antibacterial activities of quinolones containing five- and six-membered heterocyclic substituents at the 7-position
- 1 April 1990
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 33 (4), 1246-1252
- https://doi.org/10.1021/jm00166a025
Abstract
A series of 6-fluoro-7-substituted-1-ethyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids were prepared. The substituents at the 7-position included five- and six-membered heterocyclic rings such as oxazoline and oxazine as well as five-membered heteroaromatic rings such as oxazoles and imidazoles. The structure-activity relationships (SAR) of these compounds indicated that oxazole substituent containing a 2-methyl group had the greatest in vitro potency. The compounds showed greater in vitro antibacterial activity against Gram-positive organisms than against Gram-negative organisms.This publication has 6 references indexed in Scilit:
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