| 1-[(2-Arylthiazol-4-yl)methyl]azoles as a new class of anticonvulsants: Design, synthesis, in vivo screening and in silico drug-like properties. | |
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MedLine Citation:
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PMID: 21827633 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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A series of novel thiazole incorporated (arylalkyl)azoles were synthesized and screened for their anticonvulsant properties using maximal electroshock (MES) and pentylenetetrazole (PTZ) models in mice. Among target compound, 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 PTZ and MES 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 (MW, TPSA, clog P, HBD, HBA 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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Authors:
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Nematollah Ahangar; Adile Ayati; Eskandar Alipour; Arsalan Pashapour; Alireza Foroumadi; Saeed Emami |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-8-9 |
Journal Detail:
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Title: Chemical biology & drug design Volume: - ISSN: 1747-0285 ISO Abbreviation: - Publication Date: 2011 Aug |
Date Detail:
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Created Date: 2011-8-10 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 101262549 Medline TA: Chem Biol Drug Des Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011 John Wiley & Sons A/S. |
Affiliation:
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Department of Toxicology and Pharmacology, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran Department of Chemistry, Islamic Azad University, Tehran-North Branch, Zafar St., Tehran, Iran Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, Iran Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran. |
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