مرکز اطلاعات علمی Scientific Information Database (SID) - Trusted Source for Research and Academic Resources

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Information Journal Paper

Title

DESIGN, SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF NOVEL 2- [2- (2-CHLOROPHENOXY) PHENYL] -1, 3, 4-OXADIAZOLE DERIVATIVES AS BENZODIAZEPINE RECEPTOR AGONISTS

Pages

  83-90

Abstract

 New derivatives of 2- [2- (2-Chlorophenoxy) phenyl] -1, 3, 4-oxadiazole as candidates for agonistic effect on BENZODIAZEPINE RECEPTORS were synthesized. CONFORMATIONAL ANALYSIS and superimposition of energy minima conformers of the novel compounds on estazolam, a known benzodiazepine agonist, revealed that the main proposed benzodiazepine pharmacophores were well matched. In pharmacological evaluation, ANTICONVULSANT activity of the compounds determined by pentylenetetrazole-induced lethal convulsion and maximal electroshock tests. The results showed that the introduction of an amino substituent in position 5 of 1, 3, 4- oxadiazole ring generates compound 6 that has a considerable effect. Compound 8 with a hydroxyl substituent on position 5 of 1, 3, 4-oxadiazole ring showed a relatively mildANTICONVULSANT activity, which was significantly weaker than that of diazepam and compound 6. ANTICONVULSANT effects of active compounds were antagonized by flumazenil, an antagonist of BENZODIAZEPINE RECEPTORS, indicating the involvement of BENZODIAZEPINE RECEPTORS in these effects.

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    APA: Copy

    FAIZI, MEHRDAD, SHEIKHHA, MAJID, AHANGAR, NEMATOLLAH, TABATABAEI GHOMI, H., SHAFAGHI, BIJAN, SHAFIEE, ABBAS, & TABATABAI, SAYYED ABBAS. (2012). DESIGN, SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF NOVEL 2- [2- (2-CHLOROPHENOXY) PHENYL] -1, 3, 4-OXADIAZOLE DERIVATIVES AS BENZODIAZEPINE RECEPTOR AGONISTS. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), 11(1), 83-90. SID. https://sid.ir/paper/287925/en

    Vancouver: Copy

    FAIZI MEHRDAD, SHEIKHHA MAJID, AHANGAR NEMATOLLAH, TABATABAEI GHOMI H., SHAFAGHI BIJAN, SHAFIEE ABBAS, TABATABAI SAYYED ABBAS. DESIGN, SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF NOVEL 2- [2- (2-CHLOROPHENOXY) PHENYL] -1, 3, 4-OXADIAZOLE DERIVATIVES AS BENZODIAZEPINE RECEPTOR AGONISTS. IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR)[Internet]. 2012;11(1):83-90. Available from: https://sid.ir/paper/287925/en

    IEEE: Copy

    MEHRDAD FAIZI, MAJID SHEIKHHA, NEMATOLLAH AHANGAR, H. TABATABAEI GHOMI, BIJAN SHAFAGHI, ABBAS SHAFIEE, and SAYYED ABBAS TABATABAI, “DESIGN, SYNTHESIS AND PHARMACOLOGICAL EVALUATION OF NOVEL 2- [2- (2-CHLOROPHENOXY) PHENYL] -1, 3, 4-OXADIAZOLE DERIVATIVES AS BENZODIAZEPINE RECEPTOR AGONISTS,” IRANIAN JOURNAL OF PHARMACEUTICAL RESEARCH (IJPR), vol. 11, no. 1, pp. 83–90, 2012, [Online]. Available: https://sid.ir/paper/287925/en

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