Abstract: |
Anew series of 2,3-dihydroquinazolin-4(1H)-one derivatives bearing benzamide moiety have been synthesized with a survey of their analgesic and anti-inflammatory activities. In addition, novel 3,4-dihydro-1H-benzo[e][1,2,4]triazepin-5(2H)-one derivatives have been synthesized with a survey of their C.N.S. activities. The study showed that the quinazolinone bearing 4-hydroxybenzamide moiety IVe showed a higher anti-inflammatory activity than diclofenac sodium and celecoxib. The compounds IVc , IVe were the most active as analgesic. Moreover, all of the tested compounds showed lower ulcerogenic index than celecoxib.
Moreover, evaluation of the Central Nervous System activities for quinazolinone derivatives )XIIIa,b,d,f XVIIa,b,d,e,f( and benzotriazepine derivatives (V, VIIb, VIIc, IXc, IXd) revealed that the benzotriazepine derivatives (V, VIIb, VIIc, IXc, IXd)showed higher CNS
depressant activity
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