University Institute of Pharmaceutical Sciences, Panjab University, Sector-14, Chandigarh 160014, India.
Eur J Med Chem. 2010 Jun;45(6):2591-6. doi: 10.1016/j.ejmech.2010.02.047. Epub 2010 Feb 25.
A novel mutual prodrug consisting of 4-biphenylacetic acid (BPA) and quercetin tetramethyl ether (QTME) has been synthesized as a gastrosparing NSAID, devoid of ulcerogenic side effects. The physicochemical properties, including aqueous solubility, partition coefficient, chemical stability and enzymatic hydrolysis of synthesized derivative have been studied to assess its prodrug potential. Its antiinflammatory, antiulcer and analgesic activities were also evaluated. The results indicated that BPA-QTME derivative is chemically stable, biolabile and possesses optimum lipophilicity. The synthesized compound also exhibited retention of antiinflammatory activity with reduced ulcerogenicity. Based on these observations, the therapeutic potential of this mutual prodrug is discussed.
一种新型的互变异构前药，由 4-联苯乙酸（BPA）和槲皮素四甲醚（QTME）组成，作为一种胃刺激性非甾体抗炎药，没有溃疡副作用。已经研究了合成衍生物的物理化学性质，包括水溶解度、分配系数、化学稳定性和酶水解，以评估其前药潜力。还评估了其抗炎、抗溃疡和镇痛活性。结果表明，BPA-QTME 衍生物在化学上是稳定的，生物不稳定的，并且具有最佳的亲脂性。合成化合物也表现出抗炎活性的保留和溃疡形成性的降低。基于这些观察，讨论了这种互变异构前药的治疗潜力。
