Yoshioka T, Fujita T
Chemtech Labo., Tokyo, Japan.
Yakugaku Zasshi. 1997 Sep;117(9):597-610. doi: 10.1248/yakushi1947.117.9_597.
An interest in compounds having both the quenching activity of the active oxygen species (antioxidant activity) and hypoglycemic and/or hypolipidemic activities significantly increases in the field of angiopathic disease, especially in the elderly. We studied hindered phenols in order to find biologically active compounds having the above activities. As a result, several compounds, such as 1,3-benzoxathioles, phenoxypentanoic acids, phenoxypentanols, 2-chloro-3-phenylpropionic acids, and thiazolidines, were found. Among these compounds, a thiazolidine, troglitazone, (CS-045), 1, showed desired biological properties both in vitro and in vivo without causing any increase in liver weight, and so was developed as a new type of antidiabetic agent. In this review, the structural design and the biological activities including antioxidant activities are described.
在血管病变疾病领域,尤其是在老年人群中,对同时具有活性氧淬灭活性(抗氧化活性)以及降血糖和/或降血脂活性的化合物的关注度显著增加。我们研究了受阻酚类,以寻找具有上述活性的生物活性化合物。结果,发现了几种化合物,如1,3 - 苯并噻唑、苯氧基戊酸、苯氧基戊醇、2 - 氯 - 3 - 苯基丙酸和噻唑烷。在这些化合物中,一种噻唑烷——曲格列酮(CS - 045),1,在体外和体内均表现出所需的生物学特性,且不会导致肝脏重量增加,因此被开发为一种新型抗糖尿病药物。在这篇综述中,将描述其结构设计以及包括抗氧化活性在内的生物学活性。