Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry
ISSN: 0975-413X
Abstract
In Vivo Antipsychotics: Synthesis, Spectral, Docking and Pharmacokinetic Properties of New 1-(4-(3,4-dihydroquinolin-2(1H)-one-7-yloxy)butyl)-3-methyl-2,7-diphenyl-1,4-diazepan-5-one Analogs of Aripiprazole
Author(s): Selvarasu Sekar, Srinivasan Pazhamalai, Ganesan Ariharasivakumar, Mannathusamy GopalakrishnanA series of new 1-(4-(3,4-dihydroquinolin-2(1H)-one-7-yloxy)butyl)-3-methyl-2,7-diphenyl-1,4-diazepan-5-one analogs of aripiprazole was synthesized by the replacement of 2,3-dichlorophenyl-4-piperazine/diazepane moiety with 3-methyl-2,7-diphenyl-1,4-diazepan-5-one to explore the influence of structural features. All the synthesized compounds are characterized by elemental analysis, Fourier Transform Infrared (FTIR), Proton Nuclear Magnetic Resonance (1H-NMR), Carbon-13 Nuclear Magnetic Resonance (13C-NMR), Heteronuclear Single Quantum Coherence (HSQC) (2D NMR) and mass spectrometry of compound 4a. All the multi target ligands have been docked against, human A2A adenosine receptor and human β2-adrenergic G-protein-coupled Receptors (GPCRs), both receptor and ligand interaction shows an excellent dock score. Absorption Distribution, Metabolism and Excretion (ADME), properties were also evaluated in the desirable range, finally these compounds have orally drug-likeness property. In this event was done to screening the neuroleptic activity of the synthesized compounds with different anti-psychotic animal models.
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