合成与研究新的顺磁和反磁维拉帕米衍生物。
Synthesis and study of new paramagnetic and diamagnetic verapamil derivatives.
机构信息
Institute of Organic and Medicinal Chemistry, University of Pécs, H-7602 Pécs, PO Box 99, Hungary.
出版信息
Bioorg Med Chem. 2010 Apr 15;18(8):2954-63. doi: 10.1016/j.bmc.2010.02.040. Epub 2010 Feb 25.
New derivatives of verapamil (1) modified with nitroxides and their precursors were synthesized and screened for reactive oxygen species (ROS)-scavenging activities. The basic structure was modified by changing the nitrile group to an amide or the methyl substituent on tertiary nitrogen with nitroxides and their reduced forms (hydroxylamine and secondary amines). Among the new verapamil derivatives compound 16B [Mohan, I. K.; Kahn, M.; Wisel, S.; Selvendiran, K.; Sridhar, A.; Carnes, C.A.; Bognár, B.; Kálai, T.; Hideg, K.; Kuppusamy, P. Am. J. Physiol. Heart Circ. Physiol.2009, 296, 140], modified with hydroxylamine salt of 2,2,6,6-tetramethyl-1,2,3,6-tetrahydropyridine-1-yloxyl proved to be the best ROS scavenger in vitro and protected HSMC and CHO cells against H(2)O(2) induced damage.
新型维拉帕米（1）衍生物经硝酮及其前体修饰，并对其活性氧（ROS）清除活性进行了筛选。通过将腈基改为酰胺或叔氮上的甲基取代基并用硝酮及其还原形式（羟胺和仲胺）进行修饰，改变了基本结构。在新的维拉帕米衍生物中，化合物 16B [Mohan, I. K.; Kahn, M.; Wisel, S.; Selvendiran, K.; Sridhar, A.; Carnes, C.A.; Bognár, B.; Kálai, T.; Hideg, K.; Kuppusamy, P. Am. J. Physiol. Heart Circ. Physiol.2009, 296, 140]，经 2,2,6,6-四甲基-1,2,3,6-四氢吡啶-1-基氧自由基的羟胺盐修饰，被证明是体外最好的 ROS 清除剂，并能保护 HSMC 和 CHO 细胞免受 H2O2 诱导的损伤。
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