Synthesis, radical scavenging activity and structure–activity relationship of uric acid analogs
作者:Daisuke Yasuda、Kyoko Takahashi、Tomohiro Kakinoki、Yoko Tanaka、Tomoyuki Ohe、Shigeo Nakamura、Tadahiko Mashino
DOI:10.1039/c2md20287e
日期:——
Uric acid (UA) is known to play an important role as an endogenous antioxidant. However, its insolubility in the serum is a risk for hyperuricemia. We assume that UA is an equivalent to hydroquinone or p-aminophenol, which can be oxidized to quinone/quinoimine and thus acts as a radical scavenger. Based on this hypothesis, a series of UA analogs was designed and synthesized. In the chemical radical
尿酸已知(UA)作为内源性抗氧化剂起着重要作用。然而,其在血清中的不溶性是高尿酸血症的风险。我们假设UA等于对苯二酚 要么 对氨基苯酚,可以被氧化成 醌/ quinoimine,因此可充当自由基清除剂。基于该假设,设计并合成了一系列UA类似物。在化学自由基清除测定中,活性化合物被认为是对苯二酚 要么 对氨基苯酚等价物。高度官能化的UA结构对于具有自由基清除活性不是必需的。有效的活性5-羟基吲哚酮(1a,2a和3a)显示出足够的活性,且具有高溶解性和低细胞毒性。