Semisynthetic cephalosporins. Synthesis and structure-activity relations of analogs with 7-acyl groups derived from 2-(cyanomethylthio) acetic acid or 2-[(2, 2, 2- …

…, JRE Hoover, JV Uri, JR Guarini, L Phillips…

Index: DeMarinis; Boehm; Dunn; Hoover; Uri; Guarini; Phillips; Actor; Weisbach Journal of Medicinal Chemistry, 1977 , vol. 20, # 1 p. 30 - 35

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Citation Number: 11

Abstract

The synthesis and in vitro and in vivo activities of a series of cephalosporins having side chains derived from 2-[(2, 2, 2-trifluoroethyl) thio] acetic acid or 2-(cyanomethy1thio) acetic acid and with acetoxymethyl or 3-heterocyclic thiomethyl substituents at the 3 position are described. In both series, increasing the oxidation state of the side-chain sulfur atom from sulfide to sulfoxide/sulfone decreased the in vitro gram-positive activity, but the effect on ...