| Autor: |
Lohray, B. B., Bhushan, V., Rao, B. P., Madhavan, G. R., Murali, N., Rao, K. N., Reddy, A. K., Rajesh, B. M., Reddy, P. G., Chakrabarti, R., Vikramadithyan, R. K., Rajagopalan, R., Mamidi, R. N. V. S., Jajoo, H. K., Subramaniam, S. |
| Zdroj: |
Journal of Medicinal Chemistry; May 7, 1998, Vol. 41 Issue: 10 p1619-1630, 12p |
| Abstrakt: |
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. |
| Databáze: |
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