| Literature DB >> 9572887 |
B B Lohray1, V Bhushan, B P Rao, G R Madhavan, N Murali, K N Rao, A K Reddy, B M Rajesh, P G Reddy, R Chakrabarti, R K Vikramadithyan, R Rajagopalan, R N Mamidi, H K Jajoo, S Subramaniam.
Abstract
A series of [[(heterocyclyl)ethoxy]benzyl]-2,4-thiazolidinediones have been synthesized by the condensation of corresponding aldehyde 1 and 2,4-thiazolidinedione followed by hydrogenation. Both unsaturated thiazolidinedione 2 and its saturated counterpart 3 have shown antihyperglycemic activity. Many of these compounds have shown superior euglycemic and hypolipidemic activity compared to troglitazone (CS 045). The indole analogue DRF-2189 (3g) was found to be a very potent insulin sensitizer, comparable to BRL-49653 in genetically obese C57BL/6J-ob/ob and 57BL/KsJ-db/db mice. Pharmacokinetic and tissue distribution studies conducted on BRL-49653 and DRF-2189 (3g) indicate that these drugs are well-distributed in target tissues. On the basis of euglycemic activity as well as enhanced selectivity against reduction of triglycerides in plasma, DRF-2189 (3g) has been selected for further evaluation.Entities:
Mesh：
Substances：
Year: 1998 PMID： 9572887 DOI： 10.1021/jm970444e
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446