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...

Full description

Saved in:
Bibliographic Details
Published in:European journal of medicinal chemistry 2008-07, Vol.43 (7), p.1530-1535
Main Authors: Mishra, Nidhi, Arora, Preeti, Kumar, Brajesh, Mishra, Lokesh C., Bhattacharya, Amit, Awasthi, Satish K., Bhasin, Virendra K.
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimalarial activity
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Antiparasitic agents
Biological and medical sciences
Chalcones
Diamines - chemical synthesis
Diamines - chemistry
Diamines - pharmacology
In vitro
In Vitro Techniques
Magnetic Resonance Spectroscopy
Mass Spectrometry
Medical sciences
Pharmacology. Drug treatments
Plasmodium falciparum
Plasmodium falciparum - drug effects
Synthesis
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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 μg/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. Two step synthesis protocol was used to prepare chalcones. Chloro-series, 1,2,4-triazole substituted chalcone was found to be the most effective in inhibiting Plasmodium falciparum in vitro. [Display omitted]
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2007.09.014