Synthesis and Pharmacological Evualuation of Newly Derived Heterocyclic Compounds Targeted For Neurological Disoreders

Abstract

Human neurological system is one of the multifaceted and important systems of human body. Due to unchanging life style large number of population are suffering from these chronic neurological disorders such as Alzheimer, Parkinson, epilepsy, schizophrenia and neuropathic pain. To develop of the neuroprotective agents is endless need in mind of medicinal research fertility. Indole and its derivatives exhibit therapeutic potential against neurological disorders through regulating circadian rhythm and immune function. So, this research work has been planned to screen novel indole containing molecule by QSAR studies and later synthesizes potentially active molecules targeting neurological disorders. newlineMarine alkaloids having indole moiety were virtual analyzed on human adenosine receptor A2a by using V life MDS 4.6 and indole nucleus containing marine alkaloids showed excellent binding affinity towards specific receptor. Virtually total 75 molecules from scheme-I and scheme-II screened for QSAR, pharmacophore and molecular docking study by using V life MDS 4.6. From theoretically designed schemes, practically we have synthesised total 45 molecules and its novelty confirmed by using Scifinder database. All the synthesised molecules were characterised and they confirmed by melting point, TLC, 1H-NMR, 13C-NMR, Mass and IR Spectroscopy. Few synthesised molecules were screened for anticonvulsant and antidepressant activity in rat models as per priority of highest docking score. newlineThe screening of anticonvulsant activity carried out in two animal models i.e. maximal electroschock and pentylenetetrazole. Effect of synthesised molecules on duration of hind limb tonic extension (HLTE) considered as a final response and as a determinant for drugs potential in both models of anticonvulsant activity. The antidepressant activity also carried out in two animal models i.e. forced swim test and tail suspension test. Effect of synthesised molecules on duration of immobility in forced swim test and tail suspension test as a final response