SYNTHESIS AND BETA-LACTAMASE INHIBITORY EVALUATION OF NOVEL HLOROMETHYL-2-ALPHA-METHYLPENAM-3-ALPHA-CARBOXYLIC ACIDS AND THEIR SULFONES ANDZOLYLMETHYL-2-ALPHA-METHYLPENAM-3-ALPHA-CARBOXYLIC ACIDS

Authors
DANELON GO MATA EG MASCARETTI OA GIRARDINI J MARRO M ROVERI OA
Citation
Go. Danelon et al., SYNTHESIS AND BETA-LACTAMASE INHIBITORY EVALUATION OF NOVEL HLOROMETHYL-2-ALPHA-METHYLPENAM-3-ALPHA-CARBOXYLIC ACIDS AND THEIR SULFONES ANDZOLYLMETHYL-2-ALPHA-METHYLPENAM-3-ALPHA-CARBOXYLIC ACIDS, Bioorganic & medicinal chemistry letters, 5(17), 1995, pp. 2037-2040
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
17
Year of publication
1995
Pages
2037 - 2040
Database
ISI
SICI code
0960-894X(1995)5:17<2037:SABIEO>2.0.ZU;2-5
Abstract
The synthesis and the inhibitory activity against beta-lactamase 1 fro m Bacillus cercus is described Tor a new series of 6 alpha-bromo, chlo ro or fluoro-2 beta-chloromethyl-2 alpha-methylpenam-3 alpha-carboxyli c acids (5a-c) and their corresponding sulfones 6a-c and 6 alpha-bromo , chloro or fluoro-2 beta-mercaptobenzothiazolylmethyl-2 alpha- methyl penam-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).