1,4-BENZOTHIAZINE-2-CARBOXYLIC ACID 1-OXIDES AS ANALOGS OF ANTIBACTERIAL QUINOLONES

被引:22
作者
CECCHETTI, V [1 ]
FRAVOLINI, A [1 ]
SCHIAFFELLA, F [1 ]
TABARRINI, O [1 ]
ZHOU, WC [1 ]
PAGELLA, PG [1 ]
机构
[1] MEDIOLANUM FARMACEUT,I-20143 MILAN,ITALY
关键词
D O I
10.1002/jhet.5570290215
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The synthesis of 1,4-benzothiazine-2-carboxylic acid 1-oxides as agents which mimic quinolone antibacterial, are described. The key step includes intramolecular cyclization of phenylsulfinyl acrylates 17 and 18 which are prepared in six steps from 11. None of new target compounds showed interesting antibacterial activity in vitro against the tested strains.
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页码:375 / 382
页数:8
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