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Synthesis and Evaluation of Substituted Pyrazoles: Potential Antimalarials Targeting the Enoyl-Acp Reductase of Plasmodium Falciparum

Kumar, Sanjay and Kumar, Gyanendra and Kapoor, Mili and Surolia, Avadhesha and Surolia, Namita (2006) Synthesis and Evaluation of Substituted Pyrazoles: Potential Antimalarials Targeting the Enoyl-Acp Reductase of Plasmodium Falciparum. In: Synthetic Communications, 36 (2). pp. 215-226.

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Abstract

A series of 1,5- and 1,3-diarylsubstituted pyrazoles were designed, synthesized, and evaluated for their ability to inhibit enoyl-ACP reductase of Plasmodium falciparum. The inhibitory activity of these synthesized compounds was evaluated in a continuous spectrophotometric assay. Of all the compounds analyzed, NAS-81 and NAS-39 inhibited the enzyme with IC50 values of 30 \mu M and 50 \mu M, respectively. The mode of ligand binding was investigated by docking the synthetic inhibitors at the active site of the crystal structure of the enzyme.

Item Type: Journal Article
Additional Information: Copyright for this article belongs to Taylor & Francis Inc.
Keywords: Antimalarials; fatty acid synthesis; inhibitor; substituted pyrazole
Department/Centre: Division of Biological Sciences > Molecular Biophysics Unit
Date Deposited: 27 Feb 2006
Last Modified: 27 Aug 2008 11:47
URI: http://eprints.iisc.ernet.in/id/eprint/5713

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