Novel euglycemic and hypolipidemic agents. 1

被引：81

作者：

Lohray, BB ^{[1
]}

Bhusan, V ^{[1
]}

Rao, BP ^{[1
]}

Medhavan, GR ^{[1
]}

Murali, N ^{[1
]}

Rao, KN ^{[1
]}

Reddy, AK ^{[1
]}

Rajesh, BM ^{[1
]}

Reddy, PG ^{[1
]}

Chakrabarti, R ^{[1
]}

Vikramadithyan, RK ^{[1
]}

Rajagopalan, R ^{[1
]}

Mamidi, RNVS ^{[1
]}

Jajoo, HK ^{[1
]}

Subramanian, S ^{[1
]}

机构：

[1] Dr Reddys Res Fdn, Hyderabad 500050, Andhra Pradesh, India

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1998年 / 41卷 / 10期

关键词：

D O I：

10.1021/jm970444e

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：1619 / 1630

页数：12

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