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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 , Lynn M Abell 1 , David G Harden 1 , Kristen Pike 1 , Kimberly Nowak 1 , Gregory A Locke 1 , Gerald J Duke 1 , Xiaoqin Liu 1 , Gayani Fernando 1 , Scott A Shaw 1 , Benjamin P Vokits 1 , Nicholas R Wurtz 1 , Andrew Viet 1 , Meriah N Valente 1 , Sylwia Stachura 1 , Paul Sleph 1 , Javed A Khan 1 , Ji Gao 1 , Ashok R Dongre 1 , Lei Zhao 1 , Ruth R Wexler 1 , David A Gordon 1 , Ellen K Kick 1
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2017-10-26 00:00:00 , DOI: 10.1039/c7md00268h Franck Duclos 1 , Lynn M Abell 1 , David G Harden 1 , Kristen Pike 1 , Kimberly Nowak 1 , Gregory A Locke 1 , Gerald J Duke 1 , Xiaoqin Liu 1 , Gayani Fernando 1 , Scott A Shaw 1 , Benjamin P Vokits 1 , Nicholas R Wurtz 1 , Andrew Viet 1 , Meriah N Valente 1 , Sylwia Stachura 1 , Paul Sleph 1 , Javed A Khan 1 , Ji Gao 1 , Ashok R Dongre 1 , Lei Zhao 1 , Ruth R Wexler 1 , David A Gordon 1 , Ellen K Kick 1
Affiliation
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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：
三唑并嘧啶被鉴定为可逆性髓过氧化物酶抑制剂
髓过氧化物酶是一种哺乳动物过氧化物酶，作为抗微生物第一反应者参与免疫系统，可以产生次氯酸以应对入侵的病原体。由于次氯酸以及其他活性自由基的长期产生，髓过氧化物酶与多种慢性病理性疾病有关。开发了高通量筛选和分类方案来鉴定髓过氧化物酶的可逆抑制剂，以用于治疗动脉粥样硬化等慢性疾病。描述了可逆髓过氧化物酶抑制剂 7-(benzyloxy)-3 H- [1,2,3]triazolo[4,5- d ]pyrimidin-5-amine的鉴定和表征。
更新日期：2017-10-26
中文翻译：
三唑并嘧啶被鉴定为可逆性髓过氧化物酶抑制剂
髓过氧化物酶是一种哺乳动物过氧化物酶，作为抗微生物第一反应者参与免疫系统，可以产生次氯酸以应对入侵的病原体。由于次氯酸以及其他活性自由基的长期产生，髓过氧化物酶与多种慢性病理性疾病有关。开发了高通量筛选和分类方案来鉴定髓过氧化物酶的可逆抑制剂，以用于治疗动脉粥样硬化等慢性疾病。描述了可逆髓过氧化物酶抑制剂 7-(benzyloxy)-3 H- [1,2,3]triazolo[4,5- d ]pyrimidin-5-amine的鉴定和表征。
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