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Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-10-22 , DOI: 10.1016/j.bmcl.2018.10.029 Allyn T. Londregan , Gary Aspnes , Chris Limberakis , Paula M. Loria , Kim F. McClure , Donna N. Petersen , Brian Raymer , Roger B. Ruggeri , Liuqing Wei , Jun Xiao , David W. Piotrowski
中文翻译：
N-（哌啶-3-基）-N-（吡啶-2-基）哌啶/哌嗪-1-羧酰胺作为PCSK9的小分子抑制剂的发现
更新日期：2018-10-22
Bioorganic & Medicinal Chemistry Letters ( IF 2.5 ) Pub Date : 2018-10-22 , DOI: 10.1016/j.bmcl.2018.10.029 Allyn T. Londregan , Gary Aspnes , Chris Limberakis , Paula M. Loria , Kim F. McClure , Donna N. Petersen , Brian Raymer , Roger B. Ruggeri , Liuqing Wei , Jun Xiao , David W. Piotrowski
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A series of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides were identified as small molecule PCSK9 mRNA translation inhibitors. Analogues from this new chemical series, such as 4d and 4g, exhibited improved PCSK9 potency, ADME properties, and in vitro safety profiles when compared to earlier lead structures.
中文翻译：
N-（哌啶-3-基）-N-（吡啶-2-基）哌啶/哌嗪-1-羧酰胺作为PCSK9的小分子抑制剂的发现
一系列N-（哌啶-3-基）-N-（吡啶-2-基）哌啶/哌嗪-1-羧酰胺被鉴定为小分子PCSK9 mRNA翻译抑制剂。与早期的铅结构相比，该新化学系列的类似物（例如4d和4g）显示出更高的PCSK9效力，ADME特性和体外安全性。
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