Design, synthesis and biological evaluation of novel bicyclic β-lactams as potential antimalarials

[Display omitted] A series of bicyclic N-substituted and unsubstituted β-lactams were synthesized and evaluated as targeted potential antimalarials. The compounds MNR4 and MNR5 were found to have highest potency against Plasmodium falciparum in vitro.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-03, Vol.15 (5), p.1371-1373
Main Authors: Nivsarkar, Manisha, Thavaselvam, D., Prasanna, S., Sharma, Mamta, Kaushik, M.P.
Format: Article
Language:English
Subjects:
Animals
Antibiotics. Antiinfectious agents. Antiparasitic agents
Antimalarial
Antimalarials - chemical synthesis
Antimalarials - pharmacology
Antiparasitic agents
beta-Lactams - chemical synthesis
beta-Lactams - pharmacology
Bicyclic
Biological and medical sciences
Bridged Bicyclo Compounds - chemical synthesis
Bridged Bicyclo Compounds - pharmacology
Drug Design
Drug Evaluation, Preclinical
Humans
Magnetic Resonance Spectroscopy
Medical sciences
Molecular Structure
Parasitic Sensitivity Tests
Pharmacology. Drug treatments
Plasmodium falciparum
Plasmodium falciparum - drug effects
Plasmodium falciparum - isolation & purification
Structure-Activity Relationship
β-lactam
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Description
Summary:[Display omitted] A series of bicyclic N-substituted and unsubstituted β-lactams were synthesized and evaluated as targeted potential antimalarials. The compounds MNR4 and MNR5 were found to have highest potency against Plasmodium falciparum in vitro.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.01.011