Chemistry of cephalosporin antibiotics. 28. Preparation and biological activity of 3 (substituted) vinyl cephalosporins
3 (Substituted)vinylcephem nuclei have been prepared by the reaction of 3 formylcephem derivatives with stabilized phosphoranes. Appropriate synthetic steps allowed preparation of a series of 3 ethoxycarbonylvinyl and 3 carboxyvinylcephem derivatives bearing a variety of 7 acylamino functions. The phenoxyacetyl and thiopheneacetyl derivatives of the 3 cyanovinylcephem nucleus were also prepared. Although general gram positive activity was comparable to cephalothin in many cases, against penicillin G resistant Staphylococcus aureus, the new cephalosporins were of low effectiveness. The 3 (substituted)vinyl cephalosporins had good activity against a number of gram negative organisms. In some cases, this activity was excellent. The N acetyl analogs had surprisingly good activity relative to N acetyl 7 ACA. The phenylmalonoyl side chain derivatives were shown to have an unusual antibacterial spectrum expansion (relative to previously known cephalosporins) to include activity against Serratia marcescens and Pseudomonas aeruginosa.
Webber,Ott,Vasileff
p. 986 - 992
(2007/10/07)
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