51. Synthesis and biological evaluation of some pyrazole derivatives as anti-malarial agents
- Author
-
Alaa El-Din A. Bekhit, Ariaya Hymete, Henok Asfaw, and Adnan A. Bekhit
- Subjects
Male ,Models, Molecular ,Plasmodium falciparum ,Pharmaceutical Science ,Pharmacology ,Pyrazole ,Chloroquine Phosphate ,Acute toxicity ,In vitro ,chemistry.chemical_compound ,Antimalarials ,Mice ,Structure-Activity Relationship ,chemistry ,Biochemistry ,Docking (molecular) ,In vivo ,Chloroquine ,Drug Discovery ,medicine ,Structure–activity relationship ,Animals ,Pyrazoles ,medicine.drug - Abstract
Novel series of pyrazole derivatives were synthesized and tested for their in vivo anti-malarial activity using mice infected with chloroquine sensitive P. berghei at a dose level of 50 µmol/kg. The most active compounds were further tested in vitro against chloroquine resistant (RKL9) strain of P. falciparum. The in vivo anti-malarial activity study indicated that compounds 2a, 2b, 8a and 8b had mean percent suppression of 85%, 83%, 95% and 97%, respectively at equimolar dose level of the standard drug chloroquine diphosphate. Moreover, compounds 2a, 2b, 8a and 8b showed in vitro IC(50) values lower (p
- Published
- 2011