Discovery of novel hydroxy-thiazoles as HIF-α prolyl hydroxylase inhibitors:: SAR, synthesis, and modeling evaluation

被引：39

作者：

Tegley, Christopher M. ^{[1
]}

Viswanadhan, Vellarkad N. ^{[1
]}

Biswas, Kaustav ^{[1
]}

Frohn, Michael J. ^{[1
]}

Peterkin, Tanya A. N. ^{[1
]}

Chang, Catherine ^{[1
]}

Burli, Roland W. ^{[1
]}

Dao, Jennifer H. ^{[1
]}

Veith, Henrike ^{[1
]}

Rogers, Norma ^{[1
]}

Yoder, Sean C. ^{[1
]}

Biddlecome, Gloria ^{[1
]}

Tagari, Philip ^{[1
]}

Allen, Jennifer R. ^{[1
]}

Hungate, Randall W. ^{[1
]}

机构：

[1] Amgen Inc, Thousand Oaks, CA 91320 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 14期

关键词：

proyl hydroxylase inhibitors; HIF-1; alpha; hypoxia; ischemia; anemia; peripheral arterial disease; myocardial infarction; stroke; diabetes; hydroxy-thiazole;

D O I：

10.1016/j.bmcl.2008.06.031

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Inhibition of the PHD2 enzyme has been associated with increased red blood cell levels. From a screening hit, a series of novel hydroxyl-thiazoles were developed as potent PHD2 inhibitors. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：3925 / 3928

页数：4

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