Synthesis of novel substituted 1,3-diaryl propenone derivatives and their antimalarial activity in vitro.
The synthesis of novel 1,3-diaryl propenone derivatives and their antimalarial activity in vitro against asexual blood stages of human malaria parasite, Plasmodium falciparum, are described. Chalcone derivatives were prepared via Claisen-Schmidt condensation of substituted aldehydes with substituted methyl ketones. Antiplasmodial IC(50) (half maximal inhibitory concentration) activity of these compounds ranged between 1.5 and 12.3 microg/ml. The chloro-series, 1,2,4-triazole substituted chalcone was found to be the most effective in inhibiting the growth of P. falciparum in vitro while pyrrole and benzotriazole substituted chalcones showed relatively less inhibitory activity. This is the first report on antiplasmodial activity of chalcones with azoles on acetophenone ring.
Mishra
Nidhi
N
Chemical Biology Laboratory, Department of Chemistry, University of Delhi, Delhi, India.
Arora
Preeti
P
Kumar
Brajesh
B
Mishra
Lokesh C
LC
Bhattacharya
Amit
A
Awasthi
Satish K
SK
Bhasin
Virendra K
VK
D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D003959:Diamines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D066298:In Vitro Techniques; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D010963:Plasmodium falciparum / Q000187:drug effects
D000962:Antimalarials; D003959:Diamines; C009475:trimethylenediamine