title: Synthesis of novel substituted 1,3-diaryl propenone derivatives and their antimalarial activity in vitro.
abstract: 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.
authors.affiliation: Chemical Biology Laboratory, Department of Chemistry, University of Delhi, Delhi, India.
authors.forename: Nidhi
authors.initials: N
authors.lastname: Mishra
authors.forename: Preeti
authors.initials: P
authors.lastname: Arora
authors.forename: Brajesh
authors.initials: B
authors.lastname: Kumar
authors.forename: Lokesh C
authors.initials: LC
authors.lastname: Mishra
authors.forename: Amit
authors.initials: A
authors.lastname: Bhattacharya
authors.forename: Satish K
authors.initials: SK
authors.lastname: Awasthi
authors.forename: Virendra K
authors.initials: VK
authors.lastname: Bhasin
mesh_terms: 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
chemical_list: D000962:Antimalarials; D003959:Diamines; C009475:trimethylenediamine