Synthesis, characterization and evaluation of amide based prodrugs of Norfloxacin

Abstract

A series of new prodrugs (3a-e) of norfloxacin (1) was synthesized using 4-oxo-4-substituted-phenylbutanoic acids (2a-e) as promoiety. An amide-linkage was established between the secondary amino group of 1with the free carboxylic group of 2 following a single-step synthesis. The structure of the synthesized prodrugs was established on the basis of IR, ¹HNMR and mass spectral data. The title compounds (3a-e) were evaluated for in-vitro antibacterial activity against some selected pathogenic bacterial strains. The minimum inhibitory concentration (MIC) results indicated that two compounds (3c & 3d) were excellent in their antibacterial action.