Department of Pharmaceutical Chemistry, R.C. Patel Institute of Pharmaceutical, Education and Research, Maharashtra, India.
Arch Pharm (Weinheim). 2011 May;344(5):292-300. doi: 10.1002/ardp.201000096. Epub 2011 Feb 2.
Some (E/Z)-aminocarbonyl arylvinylbenzamides (B1-B15) were synthesized, evaluated for anti-inflammatory activity and ulcerogenic tendency, and their effect on gastro-intestinal motility in the rats was studied. These benzamides comprising of aliphatic unsaturated region situated between two amide linkages were synthesized by nucleophilic ring opening of appropriate azlactones (AZ1-AZ4) by suitable amines. The characterization of newly synthesized benzamides was performed by IR, (1)H- and (13)C-NMR, mass and elemental analysis. Amongst the tested compounds, benzamide B1, B2, B4, B5, and B13 were able to produce comparable or superior anti-inflammatory activity at 10 and 20 mg/kg p.o. dose with respect to standard diclofenac in carrageenan induced rat paw edema model with lessened propensity to cause gastro-intestinal hypermotility and were found to have nil tendencies to generate gastric ulcers.
一些（E/Z）-氨甲酰基芳基乙烯基苯甲酰胺（B1-B15）被合成，评估其抗炎活性和溃疡倾向，并研究它们对大鼠胃肠动力的影响。这些苯甲酰胺由位于两个酰胺键之间的脂族不饱和区域组成，通过合适的胺对适当的氮丙啶（AZ1-AZ4）进行亲核开环合成。新合成的苯甲酰胺的特性通过 IR、（1）H 和（13）C-NMR、质谱和元素分析进行表征。在所测试的化合物中，苯甲酰胺 B1、B2、B4、B5 和 B13 在角叉菜胶诱导的大鼠足肿胀模型中，以 10 和 20mg/kg po 剂量与标准双氯芬酸钠相比，能够产生相当或更好的抗炎活性，并且引起胃肠高动力的倾向较小，并且发现它们没有产生胃溃疡的趋势。
