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040 _aAIKTC-KRRC
_cAIKTC-KRRC
100 _99997
_aKerzare, Deweshri Rajendrakumar
245 _aSynthesis, Characterization, Antidepressant Activity and Docking Studies of Some Novel Indole Bearing Azetidinone Derivatives
250 _aVol.52(1), Jan-Mar
260 _aKarnataka
_bIndian journal of pharmaceutical education and research
_c2018
300 _a110-121p.
520 _aContext: In general, indole bearing azetidinone derivatives are exhibiting various biological activities. The evaluation of pharmacological potential of the indole bearing azetidinone derivatives as antidepressant agent has been relatively less explored. To get insight of the intermolecular interactions, the molecular docking studies are performed at active site of MAO-A enzyme. Aim: In this study, an attempt has been made to generate new molecular template by linking two pharmacophores (indole and azetidinone), which are likely to exhibit antidepressant-like action in animal models. Methods: The derivatives was synthesized by conventional reactions and characterized by various spectrometric methods. The derivatives were evaluated for antidepressant activity by using forced swim test. Molecular docking studies of the synthesized derivatives with MAO-A enzyme were carried on Vlife MDS Molecular Modelling software, version 4.3.1. by using k-nearest neighbour genetic algorithm method. Results: All the final structures were assigned on the basis of IR, 1H NMR, mass spectra and elemental analyses. The antidepressant evaluation exhibited final derivatives 26 and 36 as promising molecules with percentage decrease in immobility duration 66.82 and 65.61 respectively. Molecular docking studies are also in agreement with pharmacological evaluation with potent compounds exhibiting dock score -2.8474. Conclusion: It can be concluded that these compounds may have enough potential to be developed as antidepressant agent. It can be further studied for their structure-activity relationship (SAR) studies and developed into potential lead molecules. So our research can make a great impact on those medicinal chemists who work on the development of MAO-A inhibitors.
650 0 _94639
_aPHARMACEUTICS
700 _99998
_aMenghani, Sunil Sugnomal
773 0 _x0019-5464
_dBengluru Association of Pharmaceutical Teachers of India (APTI)
_tIndian journal of pharmaceutical education and research
856 _uhttps://www.ijper.org/sites/default/files/IndJPhaEdRes_52_1_110.pdf
_yClick here
942 _2ddc
_cAR