Antidiabetic and adipogenic properties in a newly synthesized thiazolidine derivative, FPFS-410.

Abstract	We report here a newly synthesized cyanoimino-oxothiazolidine derivative, FPFS-410, which has properties to ameliorate both hyperglycemia and dyslipidemia. Treatment of genetically obese-diabetic db/db mice with FPFS-410 markedly ameliorates severe hyperglycemia and hypertriglyceridemia. Although the oxothiazolidine ring of FPFS-410 shares a structural similarity with other thiazolidinedione derivatives, reporter assays showed that FPFS-410 was much less potent to activate peroxisome proliferators-activated receptor gamma (PPAR gamma) as compared with pioglitazone. When 3T3-L1 preadipocytes were treated with FPFS-410, intracellular accumulation of lipids was facilitated in a similar fashion to pioglitazone. Moreover, treatment with FPFS-410 throughout the differentiation course resulted in a significant increase in glucose transport. These results suggest that FPFS-410 may provide a useful therapeutic candidate for diabetes mellitus and dyslipidemia.
Authors	Nobuyoshi Norisada, Hiroaki Masuzaki, Muneya Fujimoto, Gen Inoue, Kiminori Hosoda, Tatsuya Hayashi, Mayumi Watanabe, Shizuko Muraoka, Fumio Yoneda, Kazuwa Nakao
Journal	Metabolism: clinical and experimental (Metabolism) Vol. 53 Issue 12 Pg. 1532-7 (Dec 2004) ISSN: 0026-0495 [Print] United States
PMID	15562395 (Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Blood Glucose FPFS-410 Hypoglycemic Agents Hypolipidemic Agents PPAR gamma Thiazoles Thiazolidinediones Triglycerides Deoxyglucose Pioglitazone
Topics	3T3-L1 Cells Adipocytes (cytology, drug effects, metabolism) Animals Biological Transport Blood Glucose (drug effects, metabolism) Cell Differentiation (drug effects) Deoxyglucose (metabolism) Hypoglycemic Agents (pharmacology) Hypolipidemic Agents (pharmacology) Male Mice Mice, Inbred C57BL Molecular Structure PPAR gamma (agonists, genetics, metabolism) Pioglitazone Thiazoles (pharmacology) Thiazolidinediones (pharmacology) Triglycerides (blood)

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