861215-45-4Relevant academic research and scientific papers
Design and synthesis of new 2-substituted-5-(2-benzylthiophenyl)-1,3,4- oxadiazoles as benzodiazepine receptor agonists
Zarghi, Afshin,Faizi, Mehrdad,Shafaghi, Bijan,Ahadian, Avideh,Khojastehpoor, Hamid R.,Zanganeh, Vahideh,Tabatabai, Sayyed A.,Shafiee, Abbas
, p. 3126 - 3129 (2007/10/03)
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.
