| Literature DB >> 24231338 |
Parameshwar Makam1, Prasoon Kumar Thakur2, Tharanikkarasu Kannan3.
Abstract
A series of 2-(2-hydrazinyl)thiazole derivatives with a wide range of substitutions at 2-, 4- and 5-positions were synthesized, characterized and evaluated their inhibitory potentials against plasmodium falciparum, NF54, by in vitro blood stage assay. The compounds, ethyl-4-methyl-2-[(E)-2-[1-(pyridin-2-yl)ethylidene]hydrazin-1-yl]-1,3-thiazole-5-carboxylate, 4d, and 1-{4-methyl-2-[(E)-2-[1-(pyridin-2-yl)ethylidene]hydrazin-1-yl]-1,3-thiazol-5-yl}ethan-1-one, 5d showed significant antimalarial activity with IC50 values of 0.725 μM and 0.648 μM respectively. To understand the mechanism, the binding interactions between 2-(2-hydrazinyl)thiazole derivatives and trans-2-enoyl acyl carrier protein reductase of P. falciparum were studied through docking studies. The half maximal inhibitory concentration (IC50) through docking studies for the compounds, 4d and 5d were found to be 22.88 μM and 631.84 μM respectively.Entities:
Keywords: 2-Chlorobenzaldehyde (PubChem CID: 6996); 2-Nitrobenzaldehyde (PubChem CID: 11101); 3-Bromobenzaldehyde (PubChem CID: 76583); 3-Hydroxy-4-methoxybenzaldehyde (PubChem CID: 12127); 4-Chlorobenzaldehyde (PubChem CID: 7726); 4-Hydroxy-3-methoxybenzaldehyde (PubChem CID: 1183); 4-Methoxybenzaldehyde (PubChem CID: 31244); Acetophenone (PubChem CID: 7410); Antimalarial activity; Benzaldehyde (PubChem CID: 240); Enoyl-ACP reductase; In silico analysis; In vitro blood stage assay; Plasmodium falciparum; Thiazole; Thiosemicarbazide (PubChem CID: 2723789)
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Year: 2013 PMID： 24231338 DOI： 10.1016/j.ejps.2013.11.001
Source DB: PubMed Journal: Eur J Pharm Sci ISSN： 0928-0987 Impact factor: 4.384