170861-71-9Relevant articles and documents
Isoxazolidine-3,5-dione and noncyclic 1,3-dicarbonyl compounds as hypoglycemic agents
Shinkai, Hisashi,Onogi, Syoji,Tanaka, Masahiro,Shibata, Tsutomu,Iwao, Megumi,Wakitani, Korekiyo,Uchida, Itsuo
, p. 1927 - 1933 (2007/10/03)
Isoxazolidine-3,5-dione 2 (JTT-501), one of the cyclic malonic acid derivatives, was found to decrease blood glucose at an oral dose of 38 mg/kg/day in KKA(y) mice and is currently undergoing evaluation in phase II clinical trials. Further studies on a series of malonic acids and related compounds showed that the 1,3-dicarbonyl structure was important for insulin- sensitizing activity. Dimethyl malonate 10, which was selected as a successor for 2, was the optimum compound in a series of 1,3-dicarbonyl compounds and was more potent than the corresponding thiazolidine-2,4-dione 1.