Synthesis, Characterization, Molecular docking and Anti-anxiety Evaluation of Some Novel Phenothiazine Derivatives

Abstract

The phenothiazine derivatives 1-(10H-phenothiazin-10-yl)-2-(4-(1-(phenylimino)ethyl)phenoxy)ethan-1-one (4a-4j) are produced from 2-(4-acetylphenoxy)-1-(10H-phenothiazin-10-yl)ethan-1-one (3) and after that, condensing them with various carbonyl compounds. Acetonitrile was used as solvent. The purity of the analogues and reaction progress were identified through their retention factor value and melting point. Characterization of the prepared analogues was completed via performing their Infra-red, proton-nuclear magnetic resonance spectroscopy with their elemental analysis. The set of molecular docking parameters of the compounds were assessed to check to their potentiality. Autodock Vina 1.2.0 was used to dock the derivatives and the docking score of all the synthesized derivatives ranges from -8.7 to -10.2. Investigation of anti-anxiety activity on albino wistar rat, was executed for all the prepared phenothiazine analogues. EPM model was approached for performing anti-anxiety study, taking Diazepam as standard drug. The compounds 2-(4-(1-((3-nitrophenyl) imino)ethyl)phenoxy)-1-(10H-phenothiazin-10-yl)ethan-1-one (4e) and 2-(4-(1-((3,4-dinitrophenyl)imino)ethyl)phenoxy)-1-(10H-phenothiazin-10-yl)ethan-1-one (4g) were showed maximum potency among all the prepared derivatives as compared to Diazepam.