Triazolopyrimidines identified as reversible myeloperoxidase inhibitors

被引：23

作者：

Duclos, Franck ^{[1
]}

Abell, Lynn M. ^{[1
]}

Harden, David G. ^{[1
]}

Pike, Kristen ^{[1
]}

Nowak, Kimberly ^{[1
]}

Locke, Gregory A. ^{[1
]}

Duke, Gerald J. ^{[1
]}

Liu, Xiaoqin ^{[1
]}

Fernando, Gayani ^{[1
]}

Shaw, Scott A. ^{[1
]}

Vokits, Benjamin P. ^{[1
]}

Wurtz, Nicholas R. ^{[1
]}

Viet, Andrew ^{[1
]}

Valente, Meriah N. ^{[1
]}

Stachura, Sylwia ^{[1
]}

Sleph, Paul ^{[1
]}

Khan, Javed A. ^{[1
]}

Gao, Ji ^{[1
]}

Dongre, Ashok R. ^{[1
]}

Zhao, Lei ^{[1
]}

Wexler, Ruth R. ^{[1
]}

Gordon, David A. ^{[1
]}

Kick, Ellen K. ^{[1
]}

机构：

[1] Bristol Myers Squibb Co, POB 5400, Princeton, NJ 08543 USA

来源：

MEDCHEMCOMM | 2017年 / 8卷 / 11期

关键词：

HIGH-DENSITY-LIPOPROTEIN; APOLIPOPROTEIN-A-I; HUMAN ATHEROSCLEROTIC LESIONS; CATALYZED OXIDATION; CHOLESTEROL EFFLUX; HUMAN ATHEROMA; MECHANISMS; DISEASE; CHLORINATION; HYPOCHLORITE;

D O I：

10.1039/c7md00268h

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Myeloperoxidase, a mammalian peroxidase involved in the immune system as an anti-microbial first responder, can produce hypochlorous acid in response to invading pathogens. Myeloperoxidase has been implicated in several chronic pathological diseases due to the chronic production of hypochlorous acid, as well as other reactive radical species. A high throughput screen and triaging protocol was developed to identify a reversible inhibitor of myeloperoxidase toward the potential treatment of chronic diseases such as atherosclerosis. The identification and characterization of a reversible myeloperoxidase inhibitor, 7-(benzyloxy)-3H-[1,2,3] triazolo[4,5-d]pyrimidin-5-amine is described.

引用

页码：2093 / 2099

页数：7

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