Kumar, Sanjay ; Kumar, Gyanendra ; Kapoor, Mili ; Surolia, Avadhesha ; Surolia, Namita (2006) Synthesis and evaluation of substituted pyrazoles: potential antimalarials targeting the enoyl-ACP reductase of Plasmodium falciparum Synthetic Communications, 36 (2). pp. 215-226. ISSN 0039-7911
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Official URL: http://www.tandfonline.com/doi/abs/10.1080/0039791...
Related URL: http://dx.doi.org/10.1080/00397910500334561
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 μM and 50 μM, 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: | Article |
|---|---|
| Source: | Copyright of this article belongs to Taylor and Francis Group. |
| Keywords: | Antimalarials; Fatty Acid Synthesis; Inhibitor; Substituted Pyrazol |
| ID Code: | 56475 |
| Deposited On: | 24 Aug 2011 11:32 |
| Last Modified: | 03 Oct 2011 14:06 |
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