Chemistry Department, Zanjan University, Iran.
Arch Pharm (Weinheim). 2011 Sep;344(9):588-94. doi: 10.1002/ardp.201000271. Epub 2011 Aug 25.
Coumarin and benzothiazole scaffolds can be found in a number of natural or synthetic antioxidants. In an effort to develop a novel radical scavenger and potential antioxidant, a series of coumarin derivatives containing 2-methylbenzothiazoline motif and related compounds was synthesized and evaluated for their DPPH (1,1-diphenyl-2-picrylhydrazyl) and ABTS(•+) (2,2'-azinobis(3-ethylbenzothiazoline-6-sulfonic acid) radicals scavenging activities. Among them, 7-hydroxy-3-(2-methyl-2,3-dihydrobenzo[d]thiazol-2-yl)-2H-chromen-2-one (3e) has shown a significant free radical scavenging activity. From the structure-activity point of view, it was found that phenolic coumarin ring and benzothiazoline moiety in target compounds may contribute to the scavenging activity against free radicals.
香豆素和苯并噻唑骨架可以在许多天然或合成抗氧化剂中找到。为了开发一种新型的自由基清除剂和潜在的抗氧化剂，我们合成了一系列含有 2-甲基苯并噻唑啉基序的香豆素衍生物和相关化合物，并评估了它们对 DPPH（1,1-二苯基-2-苦基肼基）和 ABTS(•+)（2,2'-偶氮双（3-乙基苯并噻唑啉-6-磺酸）自由基清除活性。其中，7-羟基-3-(2-甲基-2,3-二氢苯并[d]噻唑-2-基)-2H-色烯-2-酮（3e）表现出显著的自由基清除活性。从构效关系来看，发现目标化合物中酚羟基香豆素环和苯并噻唑啉部分可能有助于清除自由基的活性。
