New derivatives of verapamil (1) modified with nitroxides and their precursors were synthesized and\udscreened for reactive oxygen species (ROS)-scavenging activities. The basic structure was modified by\udchanging the nitrile group to an amide or the methyl substituent on tertiary nitrogen with nitroxides\udand their reduced forms (hydroxylamine and secondary amines). Among the new verapamil derivatives\udcompound 16B [Mohan, I. K.; Kahn, M.; Wisel, S.; Selvendiran, K.; Sridhar, A.; Carnes, C.A.; Bognár, B.;\udKálai, T.; Hideg, K.; Kuppusamy, P. Am. J. Physiol. Heart Circ. Physiol. 2009, 296, 140], modified with\udhydroxylamine salt of 2,2,6,6-tetramethyl-1,2,3,6-tetrahydropyridine-1-yloxyl proved to be the best\udROS scavenger in vitro and protected HSMC and CHO cells against H2O2 induced damage
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机译:合成了经氮氧化物修饰的维拉帕米(1)的新衍生物及其前体,并筛选了活性氧(ROS)清除活性。通过将腈基换成酰胺或叔氮上的甲基取代基并用一氧化氮及其还原形式(羟胺和仲胺)来修饰基本结构。在新的维拉帕米衍生物\ udcompound 16B中[Mohan,I. K .;卡恩(M. Wisel,S .; K.Selvendiran; A. Sridhar;卡恩斯(CA) B.博格纳尔; T.Kudlai Hideg,K .;库普萨米(P.Am.) J.生理学。心圆。生理。 2009,296,140],用\ 2,2,6,6-四甲基-1,2,3,6-四氢吡啶-1-基氧基\ udhydroxylamine盐改性是最好的\ udROS体外清除剂,并保护了HSMC和CHO细胞抵抗H2O2诱导的损伤
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