SYNTHESIS AND BETA-LACTAMASE INHIBITORY EVALUATION OF NOVEL 6-ALPHA-HALO-2-BETA-CHLOROMETHYL-2-ALPHA-METHYLPENAM-3-ALPHA-CARBOXYLIC ACIDS AND THEIR SULFONES AND 6-ALPHA-HALO-2-BETA-MERCAPTOBENZOTHIAZOLYLMETHYL-2-ALPHA-METHYLPENAM-3-ALPHA-CARBOXYLIC ACIDS

被引：14

作者：

DANELON, GO

MATA, EG

MASCARETTI, OA

GIRARDINI, J

MARRO, M

ROVERI, OA

机构：

[1] UNIV NACL ROSARIO,CONICET,INST QUIM ORGAN SINTESIS,RA-2000 ROSARIO,ARGENTINA

[2] UNIV NACL ROSARIO,FAC CIENCIAS BIOQUIM & FARMACEUT,DEPT QUIM BIOL,CATEDRA BIOFIS,RA-2000 ROSARIO,ARGENTINA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 17期

关键词：

D O I：

10.1016/0960-894X(95)00348-W

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and the inhibitory activity against beta-lactamase 1 from Bacillus cercus is described Tor a new series of 6 alpha-bromo, chloro or fluoro-2 beta-chloromethyl-2 alpha-methylpenam-3 alpha-carboxylic acids (5a-c) and their corresponding sulfones 6a-c and 6 alpha-bromo, chloro or fluoro-2 beta-mercaptobenzothiazolylmethyl-2 alpha- methylpenam-3 alpha-carboxylic acids (8a-c). Among the novel compounds, the highest activity was expressed by 6 alpha-chloro-2 beta-chloromethyl-2 alpha-methylpenam-3 alpha-carboxylic acid 1,1-dioxide (6b).

引用

页码：2037 / 2040

页数：4

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