[Studies on compounds with antioxidant activity--development of hypoglycemic agents, troglitazone (CS-045)]

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.