Design, synthesis, and docking studies of novel telmisartan-glitazone hybrid analogs for the treatment of metabolic syndrome

被引：10

作者：

Chittiboyina, Amar G. ^{[1
]}

Mizuno, Cassia S. ^{[1
]}

Desai, Prashant V. ^{[1
]}

Patny, Akshay ^{[1
]}

Kurtz, Theodore W. ^{[2
]}

Pershadsingh, Harrihar A. ^{[3
]}

Speth, Robert C. ^{[4
]}

Karamyan, Vardan ^{[4
]}

Avery, Mitchell A. ^{[1
,5
,6
]}

机构：

[1] Univ Mississippi, Sch Pharm, Dept Med Chem, University, MS 38677 USA

[2] Univ Calif San Francisco, Dept Lab Med, San Francisco, CA 94122 USA

[3] Univ Calif Irvine, Dept Family Med, Irvine, CA 92668 USA

[4] Univ Mississippi, Dept Pharmacol, University, MS 38677 USA

[5] Univ Mississippi, Natl Ctr Nat Prod Res, University, MS 38677 USA

[6] Univ Mississippi, Dept Chem & Biochem, University, MS 38677 USA

来源：

MEDICINAL CHEMISTRY RESEARCH | 2009年 / 18卷 / 07期

基金：

美国国家卫生研究院;

关键词：

Metabolic syndrome; Type; 2; diabetes; PPAR gamma; Glitazones; Hypertension; AT(1) antagonist; Telmisartan; ANGIOTENSIN-II; RECEPTOR ANTAGONISTS; AT(1) RECEPTOR; RESIDUES; BINDING; GAMMA;

D O I：

10.1007/s00044-008-9152-x

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel hybrid class of telmisartan-rosiglitazone molecules was synthesized in an attempt to discover a dual peroxisome proliferator-activated receptor gamma (PPAR gamma) agonist/angiotensin II antagonist for treatment for metabolic syndrome. Almost all the synthesized molecules showed moderate PPAR gamma activity. However, none of the hybrid analogs showed binding affinity toward the AT(1) receptor.

引用

页码：589 / 610

页数：22

共 18 条

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