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Design, synthesis, preliminary pharmacological evaluation, and docking studies of pyrazoline derivatives

Nirupam Das, Biswajit Dash, Meenakshi Dhanawat, and Sushant Kumar Shrivastava

Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, 221 005 Varanasi, India

 

E-mail: skshrivastava.phe@itbhu.ac.in

Abstract: Ten derivatives of N1 substituted/unsubstituted 5-(4-chlorophenyl)-3-(2-thienyl) pyrazoline were synthesised from chalcone-like intermediate and substituted phenyl hydrazines, hydrazine hydrate, and semi/thiosemicarbazide. The chemical structure of compounds was confirmed by means of IR, 1H NMR, mass spectroscopy, and elemental analysis. The antidepressant and anticonvulsant activities were investigated by Porsolt’s behavioural despair test (forced swimming) and maximum electroshock seizure test, respectively. Rota-Rod test was performed to assess any probable changes in motor coordination induced by the test compounds. Four compounds (IId, IIg, IIi, and IIj) exhibited good activity profile against depression and docking studies confirmed their consensual interaction with monoamine oxidase A. In addition, compounds IIc and IIe showed protection against MES-induced seizures.

Keywords: yrazoline – antidepressant – anticonvulsant – docking

Full paper is available at www.springerlink.com.

DOI: 10.2478/s11696-011-0106-2

 

Chemical Papers 66 (1) 67–74 (2012)

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