Olgen Süreyya, Kiliç Zuhal, Ada Ahmet O, Coban Tülay
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Ankara, Tandogan, Ankara, Turkey.
Arch Pharm (Weinheim). 2007 Mar;340(3):140-6. doi: 10.1002/ardp.200600176.
The interest in the application of antioxidants for medical treatment has been growing recently. A lot of evidence has proven the link between the development of human diseases and oxidative stress. Indole derivatives were found to be very effective in protecting against oxidative stress. Recent exciting findings have demonstrated that several indole derivatives (IDs) are strong inhibitors of superoxide anion (SOD) and lipid peroxidation (LP). In this study, a series of novel N-H and N-substituted indole-3-propanamide derivatives (I3PADs) have been prepared and their efficiencies were investigated towards SOD and LP. Among the synthesized I3PADs, compounds 5 and 7-12 significantly inhibited O2*- in the range of 94-100%. In addition, N-H I3PADs showed a stronger inhibitory effect (compounds 1-5, 56-83%) on lipid peroxidation levels than SOD.
近年来，抗氧化剂在医学治疗中的应用受到越来越多的关注。大量证据已证实人类疾病的发展与氧化应激之间存在联系。人们发现吲哚衍生物在抵御氧化应激方面非常有效。最近令人兴奋的研究结果表明，几种吲哚衍生物（ID）是超氧阴离子（SOD）和脂质过氧化（LP）的强效抑制剂。在本研究中，制备了一系列新型的N - H和N - 取代吲哚 - 3 - 丙酰胺衍生物（I3PAD），并研究了它们对SOD和LP的抑制效果。在合成的I3PAD中，化合物5以及7 - 12对超氧阴离子（O2* - ）的抑制率在94% - 100%之间。此外，N - H I3PAD对脂质过氧化水平的抑制作用（化合物1 - 5，抑制率为56% - 83%）比其对SOD的抑制作用更强。
