Alagarsamy Veerachamy, Shankar Durairaj, Solomon Viswas Raja, Sheorey Rajendra Vasant, Parthiban Periyasamy
Medicinal Chemistry Research Laboratory, MNR College of Pharmacy, Sangareddy-502294, India.
Acta Pharm. 2009 Mar;59(1):75-88. doi: 10.2478/v10007-009-0004-0.
A series of novel 3-cyclohexyl-2-substituted hydrazino-quinazolin-4(3H)-ones were synthesized by reacting the amino group of 3-cyclohexyl-2-hydrazino quinazolin-4(3H)-one with a variety of aldehydes and ketones. The starting material, 3-cyclohexyl-2-hydrazino quinazolin-4(3H)-one, was synthesized from cyclohexyl amine. Title compounds were investigated for analgesic, anti-inflammatory and ulcerogenic behavior. The compound 3-cyclohexyl-2-(1-methylbutylidene-hydrazino)-3H-quinazolin-4-one (4c) emerged as the most active compound of the series and is moderately more potent in its analgesic and anti-inflammatory activities compared to the reference standard diclofenac sodium. Interestingly, test compounds showed only mild ulcerogenic potential when compared to acetylsalicylic acid.
通过使3-环己基-2-肼基喹唑啉-4(3H)-酮的氨基与多种醛和酮反应，合成了一系列新型的3-环己基-2-取代肼基喹唑啉-4(3H)-酮。起始原料3-环己基-2-肼基喹唑啉-4(3H)-酮由环己胺合成。对标题化合物的镇痛、抗炎和致溃疡行为进行了研究。化合物3-环己基-2-(1-甲基亚丁基肼基)-3H-喹唑啉-4-酮(4c)是该系列中活性最强的化合物，与参比标准双氯芬酸钠相比，其镇痛和抗炎活性略强。有趣的是，与乙酰水杨酸相比，受试化合物仅显示出轻微的致溃疡潜力。
