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.
Full text not available from this repository. (Request a copy)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 |
|---|---|
| Publication: | Synthetic Communications |
| Publisher: | Taylor & Francis Inc |
| 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.ac.in/id/eprint/5713 |
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