Synthesis of some substituted pyrazole derivatives as antiprotozoal agents

Abstract

Compounds incorporating a pyrazole moiety have attracted a great deal of research owing to its therapeutic utility of the templates as useful drug molecule scaffolding. We report the synthesis of Pyrazoles moiety substituted with anilines at the fifth position of the ring as anti-protozoal lead moiety. All the compounds were screened for the anti-protozoal activity. The compounds 3a, 3-Amino-5phenylamino-4H-pyrazole-4-carboxylic acid ethyl ester and 3c 3-Amino-5-(-4- methoxy-phenyl amino)-4H-pyrazole-4-carboxylic acid ethyl ester showed better antimalarial as well as anti-leishmanial activity with IC50 value of 0.132ìmol/l and 0.150ìmol/l against P.falciparum and IC50 value of
0.132ìmol/l and 0.168 ìmol/l against Leishmaniasis donovani. The result opens up new avenues in designing novel anti-protozoal drugs as dual inhibitor with utilization of pyrazole template as part of the pharmacophore.