T. Uno, K. Iuch, Y. Kawahata
Jul 1, 1987
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0
Influential Citations
7
Citations
Quality indicators
Journal
Journal of Heterocyclic Chemistry
Abstract
Two optically active isomers of 1-ethyl-6,8-difluoro-1,4-dihydro-7-(3-hydroxypyrrolidin-1-yl)-4-oxoquinoline-3-carboxylic acid (10) were prepared. One of the isomer, 7-[(3S)-hydroxypyrrolidin-1-yl] derivative 8, was about 4 times more potent in vitro than the other, 7-[(3R)-hydroxypyrrolidin-1-yl] derivative 4, and approximately two times more active than the racemate, 7-[(3RS)-hydroxypyrrolidine-1-yl] derivative 10. Optical active 8 was the most active in in vivo, followed by 10, and 4 was the least active compound. But, they were more potent than CI-934 12 and norfloxacin. From the results, (3S)-hydroxypyrrolidinyl group was found to be one of the beneficial group for PCA-anti-bacterial agent.