synthesis of phthalimide derivatives and evaluation of their anxiolytic activity
نویسندگان
چکیده
based on the molecular modeling studies on two major families of anxiolytics and sedative hypnotics (benzodiazepines and barbiturates) a series of phthalimide derivatives were prepared from corresponding di-methyl phthalate derivatives in two steps, namely trans-amidification and ring closer of di-methyl phthalate with urea and base catalysed condensation of 4-bromobenzyl chloride and benzoyl chloride with resulting imide. the designed compounds were synthesized with satisfactory yields and chemical structures were confirmed using ir, nmr and mass spectrophotometery. among the compounds that were tested for anxiolytic activity using elevated plus-maze technique, n-benzoyl-phthalimide increased the time spent and the number of entries into the open arms at doses of 0.5 mg/kg (p<0.05).
منابع مشابه
Synthesis and Evaluation of the Anxiolytic Activity of Some Phthalimide Derivatives in Mice Model of Anxiety
The aim of the present study was to synthesis a series of phthalimides based on our previous works and examine their anxiolytic properties. Using a three steps process, phthalimides were prepared from the corresponding di-methyl phthalate derivatives. Phthalic anhydride was nitrated to produce 3-nitrophthalic acid. Ring closer of either 3-nitrophthalic acid or di-methyl phthalate with urea w...
متن کاملSynthesis and Evaluation of the Anxiolytic Activity of Some Phthalimide Derivatives in Mice Model of Anxiety
The aim of the present study was to synthesis a series of phthalimides based on our previous works and examine their anxiolytic properties. Using a three steps process, phthalimides were prepared from the corresponding di-methyl phthalate derivatives. Phthalic anhydride was nitrated to produce 3-nitrophthalic acid. Ring closer of either 3-nitrophthalic acid or di-methyl phthalate with urea w...
متن کاملSynthesis and Evaluation of the Anxiolytic Activity of Some Phthalimide Derivatives in Mice Model of Anxiety
The aim of the present study was to synthesis a series of phthalimides based on our previous works and examine their anxiolytic properties. Using a three steps process, phthalimides were prepared from the corresponding di-methyl phthalate derivatives. Phthalic anhydride was nitrated to produce 3-nitrophthalic acid. Ring closer of either 3-nitrophthalic acid or di-methyl phthalate with urea were...
متن کاملsynthesis and evaluation of the anxiolytic activity of some phthalimide derivatives in mice model of anxiety
the aim of the present study was to synthesis a series of phthalimides based on our previous works and examine their anxiolytic properties. using a three steps process, phthalimides were prepared from the corresponding di-methyl phthalate derivatives. phthalic anhydride was nitrated to produce 3-nitrophthalic acid. ring closer of either 3-nitrophthalic acid or di-methyl phthalate with urea were...
متن کاملSynthesis of New Bis - Phthalimide and Thalidomide Ester Derivatives , and Evaluation of their Cytotoxic Activity
The esterification reaction of trimellitic anhydride chloride TMAC 1 with N-(hydroxymethyl) phthalimide NHMP 2, N-(2-hydroxyethyl) phthalimide NHEP 3 or N-(hydroxymethyl) thalidomide NHMT 4 afforded novel cyclic imide-ester derivatives; phthaloyl-phthalic anhydride methyl ester PPAME 5, phthaloyl-phthalic anhydride ethyl ester PPAEE 6 and thalidomide-phthalic anhydride methyl ester TPAME 7, res...
متن کاملHypolipidemic activity of phthalimide derivatives. 1. N-Substituted phthalimide derivatives.
The general lipid-lowering action of the N-substituted phthalimide derivatives reported herein, as well as the activity of potassium phthalimide, implicates the phthalimide moiety as possessing hypolipidemic activity in rodents. Compounds containing substituents with chain lengths of four carbon or oxygen atoms showed the best hypolipidemic activity in the series tested. Tests involving 1-N-pht...
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عنوان ژورنال:
research in pharmaceutical sciencesجلد ۲، شماره ۱، صفحات ۳۵-۰
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