Abstract

Synthesis of Some Substituted Pyrazole Derivatives and their Evaluation as Antiprotozoal Agents

Author(s): M. Verma, V. Gupta, R. K. Nema and U. Misra

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. The synthesis of pyrazoles moiety substituted with anilines at the fifth position of the ring as anti-protozoal lead moiety have been reported. All the compounds were screened for the anti-protozoal activity. The compounds (3a), 3- amino-5-phenylamino-4H-pyrazole-4-carboxylic acid ethyl ester and (3c) 3-amino-5-(-4-methoxyphenylamino)- 4H-pyrazole-4-carboxylic acid ethyl ester showed better antimalarial as well as antileishmanial activity with IC50 value of 0.132 7mol/L and 0.150 7mol/L against P. falciparum and IC50 value of 0.132 7mol/L and 0.168 7mol/L against Leishmania donovani. These results open up new avenues in designing novel anti-protozoal drugs as dual inhibitor with utilization of pyrazole template as part of the pharmacophore.


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