Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University 06100 Tandogan, Ankara, Turkey.
J Enzyme Inhib Med Chem. 2012 Jun;27(3):428-36. doi: 10.3109/14756366.2011.594048. Epub 2011 Jul 8.
Melatonin (MLT) is a hormone synthesized from the pineal gland. It is a direct scavenger of free radicals, which is related to its capability to defend cells from oxidative stress. Recently MLT-related compounds are under investigation to establish which exhibit the maximum activity with the lowest side effects. In this study 5-chloroindole hydrazide/hydrazone derivatives were synthesized from 5-chloroindole-3-carboxaldehyde and phenyl hydrazine derivatives. All the compounds characterized and in vitro antioxidant activity was investigated against MLT and BHT. Most of the compounds showed strong inhibitory effect on the superoxide radical scavenging assay at 1 mM concentration (79 to 95%). Almost all the tested compounds possessed strong scavenging activity against the DPPH radical scavenging activity with IC(50) values (2 to 60 µM). Lastly, compound 1j revealed stronger inhibitory activity against MLT in the LP inhibitory assay at 0.1mM concentration (51%) while the rest of the compounds showed moderate inhibition.
褪黑素（MLT）是由松果腺合成的激素。它是自由基的直接清除剂，这与其保护细胞免受氧化应激的能力有关。最近，人们正在研究与 MLT 相关的化合物，以确定哪种化合物具有最大的活性和最低的副作用。在这项研究中，5-氯吲哚-3-甲酰肼/腙衍生物是由 5-氯吲哚-3-甲醛和苯肼衍生物合成的。所有化合物均进行了表征，并对其体外抗氧化活性进行了研究，以对抗 MLT 和 BHT。大多数化合物在 1mM 浓度下对超氧自由基清除测定具有很强的抑制作用（79%至 95%）。几乎所有测试的化合物对 DPPH 自由基清除活性均具有很强的清除活性，IC50 值为 2 至 60µM。最后，化合物 1j 在 0.1mM 浓度下的 LP 抑制测定中对 MLT 显示出更强的抑制活性（51%），而其余化合物则表现出中等抑制活性。
