Der Pharma Chemica
Journal for Medicinal Chemistry, Pharmaceutical Chemistry, Pharmaceutical Sciences and Computational Chemistry

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Abstract

Synthesis, computational studies and pharmacological evaluation of some acetamides as serotonin antagonists

Author(s): Sushil Kumar, Prateek Pandey, Yogita Srivastava, Asheesh Kumar

New acetamides (4a-c) linked with coumarin fragment were synthesized by chloroacetylation of some aminothiazoles and further treating with 7-hydroxy-4-methylcoumarin in the presence of anhydrous potassium carbonate in acetonitrile. The target compounds (4a-c) were evaluated for antiserotonergic activity by 5-HTP induced head twitches behavior in mice. The physicochemical similarity of the target compounds with respect to clozapine was assessed by calculating from a set of physiochemical properties using software programs. Compound 4b demonstrated good similarity values with respect to the standard drug and has shown antiserotonergic activity


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