期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 15, 期 22, 页码 5030-5034出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2005.08.040
关键词
antidepressant activity; 1,3,5-triphenyl pyrazolines; 3-(2 ''-naphthalen-1 ''-yl)-1,5-diphenyl-2-pyrazolines; forced-swimming test
Five new 1,3,5-triphenyl-2-pyrazolines were synthesised by reacting 1,3-diphenyl-2-propene-1-one with phenyl hydrazine hydrochloride and another five new 3-(2-hydroxy naphthalen-1-yl)-1,5-diphenyl-2-pyrazolines were synthesised by reacting 1-(2'-hydroxynaphthyl)-3- henyl-2-propene-1-one with phenyl hydrazine hydrochloride. The structures of the compounds were proved by means of their IR, H-1 NMR spectroscopic data, and microanalyses. The antidepressant activity of these compounds was evaluated by the 'Porsolt behavioural despairtest' on Swiss-Webster mice. 1-Phenyl-3-(2-hydroxyphenyl)-5-(4'-dimethylaminophenyl)-2-pyrazoline, 5-(4'-dimethylaminophenyl)-1, 3-diphenyl-2-pyrazo line, 1-phenyl-3-(2-hydroxynaphthalen-1-yl)-5-(3',4',5'-trimethoxyphenyl)-2-pyrazoline, 1-phenyl-3-(4-methylphenyl)-5-(4-dimethylaminophenyl)-2-pyrazoline and 1-phenyl-3-(4-bromophenyl)-5-(4'dimethyl amino phenyl)-2-pyrazo line reduced immobility times 25.63-59.25% at 100 mg/kg dose level. In addition, it was found that the compounds possessing electron-releasing groups such as dimethyl amino, methoxy and hydroxyl substituents, on both the aromatic rings at positions 3 and 5 of pyrazolines, considerably enhanced the antidepressant activity when compared to the pyrazolines having no substituents on the phenyl rings. (c) 2005 Elsevier Ltd. All rights reserved.
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