期刊
CHEMICAL BIOLOGY & DRUG DESIGN
卷 78, 期 5, 页码 844-852出版社
WILEY-BLACKWELL
DOI: 10.1111/j.1747-0285.2011.01211.x
关键词
(arylalkyl)azoles; 1,2,4-triazole; 1H-imidazole; anticonvulsant; drug-likeness; thiazole
资金
- Research Council of Mazandaran University of Medical Sciences, Sari, Iran
A series of novel thiazole incorporated (arylalkyl)azoles were synthesized and screened for their anticonvulsant properties using maximal electroshock and pentylenetetrazole models in mice. Among target compounds, 1-[(2-(4-chlorophenyl)thiazol-4-yl)methyl]-1H-imidazole (compound 4b), 1-[(2-phenylthiazol-4-yl)methyl]-1H-1,2,4-triazole (8a), and its 4-chlorophenyl analog (compound 8b) were able to display noticeable anticonvulsant activity in both pentylenetetrazole and maximal electroshock tests with percentage protection range of 33-100%. A computational study was carried out for prediction of pharmacokinetics properties and drug-likeness. The structure-activity relationship and in silico drug relevant properties (molecular weight, topological polar surface area, clog P, hydrogen bond donors, hydrogen bond acceptors, and log BB) confirmed that the compounds were within the range set by Lipinski's rule-of-five, and possessing favorable physicochemical properties for acting as CNS-drugs, making them potentially promising agents for epilepsy therapy.
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