SYNTHESIS OF SELECTED ANTIMICROBIAL AGENTS

Abstract

In this investigation, the synthesis of thirteen final semisynthetic cephalosporins via substitution of 7-amino-3-desacetoxycephalosporanic acid with different coumarin residues at its 7-position, designed to possess antimicrobial activity, has been achieved. Among these final compounds, eleven of them are new, and the other two are abstracted in the chemical abstracts with no details on its chemical structure and microbiological activity. The rationale behined the synthetic schemes applied is discussed. The basis, on which these molecules were designed is given. The structures of the prepared compounds were confirmed using various chemical and spectroscopic tools. In this study, synthesis, structural verification and quantitative antimicrobial activities of the following final compouds is reported. Known Finals : 1. 7-(3-Coumarinoyl) amino-3-desacetoxycephalosporanic acid. (I) 2. 7-(3-Coumarinyl acetyl) amino-3-desacetoxycephalosporanic acid.(IV) Novel Finals: 1. 7-(7-Methoxy-4-Coumainoy) amino-3-desacetoxycephalosporanic acid.(II) 2. 7-(7-Hydroxy-4-coumarinyl acetyl) amino-3-desacetoxycephalosporanic acid.(III) 3. 7-(4-Methyl-6-coumarinyloxy acetyl) amino-3-desacetoxycephalo• sporanic acid.(V)