Antimalarial activity of 3-hydroxyalkyl-2-methylene-propionic acid derivatives

Several Baylis-Hillman adducts and their derivatives were synthesized and evaluated as targeted potential anti-malarials. The compounds 4, 7 and 9 were found to have highest potency against P. falciparum in vitro. The in vivo test result of compound 4 and 9 against P. berghei demonstrated activity a...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 1999-03, Vol.9 (5), p.731-736
Main Authors: Kundu, Mrinal K., Sundar, N., Kumar, Srinivas K., Bhat, Sujata V., Biswas, Sukla, Valecha, Neena
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Antiparasitic agents
Biological and medical sciences
Chloroquine - pharmacology
Drug Evaluation, Preclinical
Drug Resistance
Medical sciences
Pharmacology. Drug treatments
Plasmodium berghei - drug effects
Plasmodium falciparum - drug effects
Propionates - chemical synthesis
Propionates - chemistry
Propionates - pharmacology
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Summary:Several Baylis-Hillman adducts and their derivatives were synthesized and evaluated as targeted potential anti-malarials. The compounds 4, 7 and 9 were found to have highest potency against P. falciparum in vitro. The in vivo test result of compound 4 and 9 against P. berghei demonstrated activity at 80 mg/Kg dose level. Synthesis and evaluation studies of some new anti-malarials is reported.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(99)00057-8