Journal of Chemical and Pharmaceutical Research (ISSN : 0975-7384)

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Original Articles: 2011 Vol: 3 Issue: 2

Studies on synthesis of some new amino acid derivatives of Cefadroxil and their antimicrobial evaluation

Abstract

A series of new semi-synthetic cefadroxil antibiotic derivatives (II-XX) carrying N-tosyl-, phthalylaminoacyl- or dipeptidyl units attached to α-amino group of 7-phenylglycinamido acyl moiety was synthesized. Furthermore, amino acid and their corresponding ester derivatives (XXI-XXVII) at 4-C carboxylic acid group of the cephem nucleus of cefadroxil were also obtained. The structures of the synthesized compounds were assigned on the bases of elemental analysis, IR, 1HNMR, and mass spectroscopy. The synthesized cefadroxil derivatives were screened for antibacterial and antifungal activities and some of them showed potent activities but were somewhat less active than cefadroxil against a wide variety of Gram-positive and Gram-negative bacteria and selected fungi.