QUINOLINECARBOXYLIC ACIDS .3. SYNTHESIS AND ANTIBACTERIAL EVALUATION OF 2-SUBSTITUTED-7-OXO-2,3-DIHYDRO-7H-PYRIDO[1,2,3-DE][1,4]BENZOTHIAZINE-6-CARBOXYLIC ACIDS RELATED TO RUFLOXACIN

被引：19
|
作者：
CECCHETTI, V
FRAVOLINI, A
PAGELLA, PG
SAVINO, A
TABARRINI, O
机构：
[1] UNIV PERUGIA,IST CHIM FARMACEUT & TECN FARMACEUT,I-06123 PERUGIA,ITALY
[2] MEDIOLANUM FARMACEUT,I-20143 MILAN,ITALY
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 1993年 / 36卷 / 22期
关键词：
D O I：
10.1021/jm00074a028
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of 2-substituted-7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzothiazine-6-carboxylic acids has been prepared and evaluated for in vitro antibacterial activity. These derivatives were less active than corresponding desmethylated analogues. Among these derivatives, the most active compound 22a was selected for preliminary pharmacokinetics in rats. The pharmacokinetic data indicated that 22a was rapidly absorbed and induced lasting plasma and urinary levels. In comparison with rufloxacin, it was excreted in low quantity in urine; a significant amount of desmethylated piperazinyl urinary metabolite was observed.
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页码：3449 / 3454
页数：6
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