SYNTHESIS OF SOME NEW PRODRUGS OF SULPHONAMIDES AND STUDIES ON THEIR ANTIMICROBIAL AND ANTI-INFLAMMATORY ACTION

Khan M.S.Y,Husain A,Hasan S.M,Akhter M

doi:10.3797/scipharm.aut-02-26

Abstract

Various amide-based prodrugs of sulphonamides have been synthesised by condensing appropriate sulphonamide moiety with different β-aroyl propionic acids. All the compounds have been evaluated for their antimicrobial and anti-inflammatory activities. Their structures were established on the basis of elemental analysis, 1H NMR and Mass spectral data. Some of these compounds were found to have significant activity

Highlights

The sulphonamides are one of the least expensive chemotherapeutic agents and this factor largely accounts for their greater extent of use in developing countries
They are used in urinary tract infections, meningitis, streptococcal pharyngitis, baciliary dysentery, trachoma, chancroid, malaria, toxoplasmosis, nocardiasis and conjunctivitis'"
YKhan et al.: choice for all forms of leprosy. They are generally taken orally in higher doses which cause nausea, vomiting and epigastric pain4.'. p-Aroyl propionic acids are well known antiinflammatory drugs and some of them are available in the market ' . ~th,ey owe their activity to in-vivo metabolism to the corresponding phenyl acetic acid and have been reported to have comparatively more gastrointestinal side effects as compared to other NSAIDS'-~.In view of these facts, it was considered worthwhile to study various amide-based prodrugs of sulphonamides with P-aroyl propionic acids in order to improve their efficacy and to decrease the side effects

Summary

Introduction

The sulphonamides are one of the least expensive chemotherapeutic agents and this factor largely accounts for their greater extent of use in developing countries. They are used in urinary tract infections, meningitis, streptococcal pharyngitis, baciliary dysentery, trachoma, chancroid, malaria, toxoplasmosis, nocardiasis and conjunctivitis'". Different P-aroyl propionic acids were condensed with appropriate sulphonamides and their structures were established on the basis of elemental analysis, 'H NMR and Mass spectral data. These compounds were evaluated for their anti-inflammatory and antimicrobial activity

Results and Discussion

Compd Ar

Mass spectral

Antibacterial Activity