SYNTHESIS AND BIOLOGICAL EVALUATION OF N1 AND N4 SUBSTITUTED 3, 5- DINITROSULFANILAMIDES DERIVATIVES AS ANTI-LEISHMANIA AGENTS

Abstract

Leishmaniasis is a disease caused by a protozoan parasites belonging to the genus leishmania. The neglected tropical
diseases (NTDs) affect more than one-sixth of the world's population. Current drugs are toxic, expensive, and require
longterm treatment. Thus, identification and development of novel, efficient and safe anti-leishmanial compounds as
drug candidates are important. Quantitative structure activity relationship analysis (QSAR) was carried out to identify
the ideal physicochemical characteristics of potential nitrosulfanilamide analogs. QSAR results show that some derivatives
studied would be useful as prototype molecules for the planning of new derivatives with profile of anti-leishmanial
drugs.In our efforts to identify novel chemical scaffolds for the development of antileishmanial agents, a series of nitro
sulfanilamide compounds was synthesized and tested against the leishmaniasis. Among the synthesized derivatives,
compound 1b showed significant antileishmanial efficacy against L.donavani. The results show that the reported
compounds are promising leads for potential anti-leishmanial drug development.