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  • Title: Design and synthesis of new 2-substituted-5-(2-benzylthiophenyl)-1,3,4-oxadiazoles as benzodiazepine receptor agonists.
    Author: Zarghi A, Faizi M, Shafaghi B, Ahadian A, Khojastehpoor HR, Zanganeh V, Tabatabai SA, Shafiee A.
    Journal: Bioorg Med Chem Lett; 2005 Jun 15; 15(12):3126-9. PubMed ID: 15876530.
    Abstract:
    A series of new 2-substituted-5-(2-benzylthiophenyl)-1,3,4-oxadiazoles was designed and synthesized as anticonvulsant agents. Conformational analysis and superimposition of energy minima conformers of the designed molecules on estazolam, a known benzodiazepine receptor agonist, revealed that the main proposed benzodiazepine pharmacophores were well matched. Electroshock and pentylenetetrazole-induced lethal convulsion tests showed that the introduction of an amino group in position 2 of 1,3,4-oxadiazole ring and a fluoro substituent at para position of benzylthio moiety had the best anticonvulsant activity. It seems this effect is mediated through benzodiazepine receptors mechanism.
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