Isoxazolidine-3,5-dione and noncyclic 1,3-dicarbonyl compounds as hypoglycemic agents
Shinkai, H; Onogi, S; Tanaka, M; Shibata, T; Iwao, M; Wakitani, K; Uchida, I
HERO ID
4923720
Reference Type
Journal Article
Year
1998
Language
English
PMID
| HERO ID | 4923720 |
|---|---|
| In Press | No |
| Year | 1998 |
| Title | Isoxazolidine-3,5-dione and noncyclic 1,3-dicarbonyl compounds as hypoglycemic agents |
| Authors | Shinkai, H; Onogi, S; Tanaka, M; Shibata, T; Iwao, M; Wakitani, K; Uchida, I |
| Journal | Journal of Medicinal Chemistry |
| Volume | 41 |
| Issue | 11 |
| Page Numbers | 1927-1933 |
| Abstract | 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 KKAy 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. |
| Doi | 10.1021/jm970771m |
| Pmid | 9599241 |
| Wosid | WOS:000073886300018 |
| Is Certified Translation | No |
| Dupe Override | No |
| Is Public | Yes |
| Language Text | English |