Synthesis and hemostatic and antimicrobial activities of the sodium salts of N-acyl-5-bromo(3,5-dibromo)anthranilic acids

Abstract

Acylation of 5-bromo(3,5-dibromo)anthranilic acids with the corresponding anhydrides yielded 10 N-acyl-5-bromo(3,5-dibromo)anthranilic acids. The resulting compounds were reacted with 10% sodium hydroxide to convert them to the corresponding sodium salts. The hemostatic and antimicrobial activities against Staphylococcus aureus and Escherichia coli of the resulting compounds were studied. Compound IV, containing a phenyl residue in the acyl fragment, was found to have marked hemostatic activity (18.2%) and weak antimicrobial activity. The minimum inhibitory concentration for this compound was 500 μg/ml against S. aureus and E. coli. The other sodium salts were significantly less active.