Synthesis of cephems bearing olefinic sulfoxide side chains as potential β-lactamase inhibitors
✍ Scribed by Vittorio Farina; Sheila I. Hauck; Raymond A. Firestone
- Publisher
- Elsevier Science
- Year
- 1996
- Tongue
- English
- Weight
- 266 KB
- Volume
- 6
- Category
- Article
- ISSN
- 0960-894X
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✦ Synopsis
Several cephems bearing vinyl sulfoxide and suffone moieties at C-3 were prepared by the Stille coupling of a 3-trifloxy cephem with stannanes. The sulfoxides were designed to be suicide lactamase inhibitors. None of the cephems described in this study functioned as an enzyme inhibitor, but two derivatives displayed interesting biological activity against Methycillin -resistant S. Aureus.
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This paper describes the synthesis of a series of 6-azabicyclo[3 .2.0]hept-2-ene compounds and subsequent results obtained from biological testing, for anti-microbial potency and fi-lactamase inhibition activity . It was determined that a number of compounds possessed some J3-lactamase inhibition ef