Designing novel inhibitors against falcipain-2 of Plasmodium falciparum |
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Authors: | Dharam Pal Pathak Vidushi Sharma Sachin Kumar |
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Affiliation: | 1. Department of Pharmaceutical Chemistry, Delhi Institute of Pharmaceutical Sciences and Research, Sector-3, Pushp Vihar, Delhi 17, India;2. Department of Pharmacology, Delhi Institute of Pharmaceutical Sciences and Research, Sector-3, Pushp Vihar, Delhi 17, India |
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Abstract: | Coumarin containing pyrazoline derivatives have been synthesized and tested as inhibitors of in vitro development of a chloroquine-sensitive (MRC-02) and chloroquine-resistant (RKL-2) strain of Plasmodium falciparum and in vivo Plasmodium berghei malaria. Docking study was also done on cysteine protease falcipain-2 which showed that the binding pose of C-14 molecule and epoxysuccinate, inhibitor of falcipain-2, binds in the similar pattern. The most active antimalarial compound was 3-(1-benzoyl-5-(4-flurophenyl)-4,5-dihydro-1H-pyrazol-3yl)-7-(diethyamino)-2H-chromen-2-one C-14, with an IC50 of 4.21?µg/ml provided complete protection to the infected mice at 24?mg/kg X 4?days respectively. |
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Keywords: | Pyrazoline Coumarin Corresponding author at: Department of Pharmaceutical Chemistry, Delhi Institute of Pharmaceutical Sciences and Research, Sector-3, Pushp Vihar, New Delhi 110017, India. |
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