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International Journal of Pharmaceutical Chemistry and Analysis


DESIGN, SYNTHESIS AND NEUROPHARMACOLOGICAL EVALUATION OF THIOPHENE INCORPORATED ISOXAZOLE DERIVATIVES AS ANTIDEPRESSANT AND ANTIANXIETY AGENTS


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Author Details: Jagdish Kumar, Mymoona Akhtar, Chanda Ranjan, Gita Chawla

Volume : 2

Issue : 2

Online ISSN : 2394-2797

Print ISSN : 2394-2789

Article First Page : 74

Article End Page : 83


Abstract

A series of 5-substituted phenyl-3-(thiophen-2-yl)-4, 5-dihydro-1, 2-oxazoles (2a-l) was synthesized by reacting appropriate chalcones of 2-acetyl thiophene with hydroxylamine hydrochloride in the presence of dry pyridine. The newly synthesized compounds were characterized by IR, 1HNMR, 13CNMR and mass spectral data. All the compounds were evaluated for their antidepressant and antianxiety activities in mice by forced swimming test and elevated plus maze method respectively. Test compounds and imipramine were administered intraperitoneally in antidepressant study at dose of 10 mg/kg. Similarly to study antianxiety activity, test compounds at the dose of 10 mg/kg and diazepam at the dose of 2 mg/kg were administered intraperitoneally. However, preliminary antidepressant screening of compounds (2a-l) revealed that none of the compounds showed antidepressant activity except for compound 2k which moderately (P<0.05) reduced the duration of immobility time. This compound was also tested in-vitro for its MAO inhibitory effect. Compound 2f showed highest antianxiety activity compared to diazepam and did not show neurotoxicity in rotarod test. The compounds were also studied for pharmacokinetic parameters and was observed that compound 2f displayed good ADME properties.


Keywords: Thiophene, isoxazole, antianxiety and antidepressant.