Triazolopyrimidines identified as reversible myeloperoxidase inhibitors,RSC Medicinal Chemistry

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Triazolopyrimidines identified as reversible myeloperoxidase inhibitors
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-10-26 00:00:00 , DOI: 10.1039/c7md00268h
Franck Duclos _{1,

2,

3} , Lynn M. Abell _{1,

2,

3} , David G. Harden _{1,

2,

3} , Kristen Pike _{1,

2,

3} , Kimberly Nowak _{1,

2,

3} , Gregory A. Locke _{1,

2,

3} , Gerald J. Duke _{1,

2,

3} , Xiaoqin Liu _{1,

2,

3} , Gayani Fernando _{1,

2,

3} , Scott A. Shaw _{1,

2,

3} , Benjamin P. Vokits _{1,

2,

3} , Nicholas R. Wurtz _{1,

2,

3} , Andrew Viet _{1,

2,

3} , Meriah N. Valente _{1,

2,

3} , Sylwia Stachura _{1,

2,

3} , Paul Sleph _{1,

2,

3} , Javed A. Khan _{1,

2,

3} , Ji Gao _{1,

2,

3} , Ashok R. Dongre _{1,

2,

3} , Lei Zhao _{1,

2,

3} , Ruth R. Wexler _{1,

2,

3} , David A. Gordon _{1,

2,

3} , Ellen K. Kick _{1,

2,

3}

Affiliation

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.

中文翻译：

三唑并嘧啶被确定为可逆的髓过氧化物酶抑制剂

髓过氧化物酶是一种作为抗微生物第一反应物参与免疫系统的哺乳动物过氧化物酶，可对入侵的病原体产生次氯酸。由于次氯酸以及其他反应性自由基物质的长期产生，髓过氧化物酶已与多种慢性病理疾病有关。开发了高通量筛选和分类方案，以识别可逆的髓过氧化物酶抑制剂，以潜在地治疗诸如动脉粥样硬化的慢性疾病。描述和鉴定了可逆的髓过氧化物酶抑制剂7-（苄氧基）-3 H- [1,2,3]三唑并[4,5 - d ]嘧啶-5-胺。

更新日期：2017-11-16

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