The synthesis and lactamase inhibitory activity of 6-(carboxymethylene)penicillins and 7-(carboxymethylene)cephalosporins
โ Scribed by John D. Buynak; Bolin Geng; Brian Bachmann; Ling Hua
- Book ID
- 103982987
- Publisher
- Elsevier Science
- Year
- 1995
- Tongue
- English
- Weight
- 259 KB
- Volume
- 5
- Category
- Article
- ISSN
- 0960-894X
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โฆ Synopsis
A series of 6-(carboxymethylene)penicillinates and 7-(carboxymethylene)cephalosporanates were synthesized and evaluated as inhibitors of one type A and two type C p-lactamases. Disodium 6-(carboxymethylene)penicillinate sulfone (15) showed broad spectrum activity. A kinetic analysis demonstrated that 15 was a potent, partially irreversible inhibitor of the 13-1actamase derived from Enterobacter cloacae Ix)9.
๐ SIMILAR VOLUMES
Swainsonine (1), an inhibitor of the important glycoprotein-processing enzyme Golgi a-mannosidase II, is a clinical candidate for cancer treatment. Analogs bearing substituents at C-6 and C-7 have been prepared and evaluated as inhibitors of a-mannosidase (jack bean), a closely related enzyme.