Synthesis and pharmacological activity of 1,4-benzodiazepine derivatives.
2-Aminobenzamides (3a-g) were prepared starting with isatoic anhydride. These compounds reacted with chloroacetic acid to give (4a-g), which were cyclized by dicyclohexylcorbodiimide to afford (5a-g). The preliminary pharmacological screening revealed that some of the new 2H-1,4-benzodiazepin-3,5(1H,4H)-dione derivatives (5) exhibited CNS-depressant and anticonvulsant activities.
Osman
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Organic Chemistry Department, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
el-Gendy
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AA
Omar
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RH
Wagdy
L
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Omar
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AH
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000494:pharmacology*; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000494:pharmacology*; D002492:Central Nervous System Depressants / Q000138:chemical synthesis* / Q000494:pharmacology*; D003292:Convulsants / Q000494:pharmacology; D005260:Female; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D008297:Male; D051379:Mice; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors / Q000494:pharmacology; D012890:Sleep / Q000187:drug effects; D013055:Spectrophotometry, Infrared
D000927:Anticonvulsants; D002492:Central Nervous System Depressants; D003292:Convulsants; D007202:Indicators and Reagents; D001569:Benzodiazepines; D010433:Pentylenetetrazole