[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.
Yoshioka
T
T
Chemtech Labo., Tokyo, Japan.
Fujita
T
T
D000818:Animals; D000975:Antioxidants / Q000138:chemical synthesis / Q000494:pharmacology; D002839:Chromans / Q000138:chemical synthesis / Q000494:pharmacology; D015195:Drug Design; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D000960:Hypolipidemic Agents / Q000138:chemical synthesis / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology; D045162:Thiazolidinediones; D000077288:Troglitazone
D000975:Antioxidants; D002839:Chromans; D007004:Hypoglycemic Agents; D000960:Hypolipidemic Agents; D013844:Thiazoles; D045162:Thiazolidinediones; D000077288:Troglitazone