Urbani Paolo, Ramunno Anna, Filosa Rosanna, Pinto Aldo, Popolo Ada, Bianchino Erminia, Piotto Stefano, Saturnino Carmela, De Prisco Rocco, Nicolaus Barbara, Tommonaro Giuseppina
Department of Pharmaceutical Sciences, University of Salerno,Via Ponte don Melillo, 84084 Fisciano, (SA) Italy.
Molecules. 2008 Mar 28;13(4):749-61. doi: 10.3390/molecules13040749.
We report the synthesis, antioxidant and antiproliferative activity and a QSAR analysis of synthetic diphenylpropionamide derivatives. Synthesis of these compounds was achieved by direct condensation of 2,2- and 3,3-diphenylpropionic acid and appropriate amines using 1-propylphoshonic acid cyclic anhydride (PPAA) as catalyst. Compound structures were elucidated by NMR analysis and their melting points were measured. The in vitro antioxidant activity of these compounds was tested by evaluating the amount of scavenged ABTS radical and estimating ROS and NO production in LPS stimulated J774.A1 macrophages. All compounds were tested for their effect on viability of cells and results demonstrated that they are not toxic towards the cell lines used. The cytotoxic activity of all compounds was evaluated by a Brine Shrimp Test.
我们报道了合成二苯基丙酰胺衍生物的合成、抗氧化和抗增殖活性以及定量构效关系（QSAR）分析。这些化合物的合成是通过使用1-丙基膦酸环酐（PPAA）作为催化剂，使2,2-和3,3-二苯基丙酸与适当的胺直接缩合来实现的。通过核磁共振（NMR）分析阐明了化合物的结构，并测量了它们的熔点。通过评估清除ABTS自由基的量以及估计脂多糖（LPS）刺激的J774.A1巨噬细胞中活性氧（ROS）和一氧化氮（NO）的产生，测试了这些化合物的体外抗氧化活性。测试了所有化合物对细胞活力的影响，结果表明它们对所使用的细胞系无毒。通过卤虫试验评估了所有化合物的细胞毒性活性。
