Synthesis of antimicrobial agents. I. Synthesis and antimicrobial activities of thiazoloquinoline derivatives.

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Abstract
A series of substituted thiazolo[4,5-g]-, [5,4-g]-, [4,5-h]- and [5,4-h]quinoline carboxylic acids was prepared by the following 2 methods for providing new antimicrobial drugs. One of the synthetic methods was conducted through successive steps of condensation of aminobenzothiazole with diethyl ethoxymethylenemalonate, Gould-Jacobs reaction, N-alkylation and hydrolysis. The other is thiazole ring cyclization of o-aminated mercaptoquinoline. These compounds prepared in this work were evaluated for antimicrobial [antibacterial] activities in vitro. 9-Chloro-8-ethyl-5,8-dihydro-5-oxothiazolo-[4,5-g]quinoline-6-carboxylic acid showed the highest activity.

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