153939-52-7Relevant academic research and scientific papers
benzyl>-2,4-thiazolidinediones as Potent Antihyperglycemic Agents
Cantello, Barrie C.C.,Cawthorne, Michael A.,Cottam, Graham P.,Duff, Peter T.,Haigh, David,et al.
, p. 3977 - 3985 (2007/10/02)
A series of -2,4-thiazolidinediones and benzyl>-2,4-thiazolidinediones was synthesized from the corresponding aldehydes.Compounds from the urea series, exemplified by 16, showed antihyperglycemic potency comparable with known agents of the type such as pioglitazone and troglitazone (CS-045).The benzoxazole 49, a cyclic analogue of 16, was a very potent enhancer of insulin sensitivity, and by modification of the aromatic heterocycle, an aminopyridine, 37, was identified as a lead compound from SAR studies.Evaluation of antihyperglycemic activity together with effects on blood hemoglobin content, to determine the therapeutic index, was performed in 8-day repeat administration studies in genetically obese C57 BI/6 ob/ob mice.From these studies, BRL 49653 (37) has been selected, on the basis of antihyperglycemic potency combined with enhanced selectivity against reductions in blood hemoglobin content, for further evaluation.
