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KMID : 0370019920060000085
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Chung-Ang Journal of Pharmacal Sciences
1992 Volume.6 No. 0 p.85 ~ p.95
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Syntheses and Antimicrobial Activities of N-Diethylcarbamoylpiperazino quinolones
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Abstract
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As a series of development of antimicrobial substances, six N-diethylcarbamoylpiperazino quinolones were prepared and evaluated for their antimicrobial activities. Treatment of 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7-(1-piperazinyl)quinoline-3-carboxylic acid [Norfloxacin], 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7-(1-piperazinyl)-1, 8-naphthridine-3-carboxylic acid [Enoxacin]and 8-dihydro-5-oxo-2-(1-piperazinyl) pyrido-[2,3-d]pyrimidine-6-carboxylic acid [Pipemidic acid] with diethylcarbamoyl chloride afforded three N-diethylcarbamoyl piperazino quinolone carboxylic acid([1]-[3]). Their privaloyloxymethyl esters of N-diethylcarbamoylpiperazinoquinolone carboxylic acids were obtained by the reaction of N-diethylcarbamoyl quinolones with pivaloyloxymethyl chloride in the presence of potassium carbonate and potasium iodide([4]-[6]). The compounds synthesixed were evaluated for their antimicrobial activities in vitro against Esche-richia coli ATCC-25922, Staphylococcus aureus ATCC 29213, Proteus vulgaris 78615. Pseudomonas ae-ruginosa 98765-IP_2, Klebsiella pneumoniae and Salmonella tompson ATCC 10256.
The results obtained were as follow :
1. The most active compound, [1], 1-ethyl-1,4-dihydro-4-oxo-7-[4-N-diethylcarbamoyl-1-piperazinyl)-3-quinoline carboxylic acid exhibited the growth inhibitory activity at a concentration of 0.25㎍/ml against E. coli, 1.0㎍/ml against S.aureus, 32.0㎍/ml against P. vulgaris, 4.0㎍/ml against Ps. aeruginosa, 1.0㎍/ml against K. pneumoniae, 4.0㎍/ml against s. tompson.
2. Most synthesized N-diethylcarbamoyl piperazino quinolones showed more potent antimicrobial activities than those shown by their pivaloyloxymethyl esters.
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