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. 2018 Dec 15;28(23-24):3685-3688.
doi: 10.1016/j.bmcl.2018.10.029. Epub 2018 Oct 22.

Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9

Allyn T Londregan  1 , Gary Aspnes  2 , Chris Limberakis  2 , Paula M Loria  2 , Kim F McClure  2 , Donna N Petersen  2 , Brian Raymer  2 , Roger B Ruggeri  2 , Liuqing Wei  2 , Jun Xiao  2 , David W Piotrowski  2
Affiliations

Discovery of N-(piperidin-3-yl)-N-(pyridin-2-yl)piperidine/piperazine-1-carboxamides as small molecule inhibitors of PCSK9

Allyn T Londregan et al. Bioorg Med Chem Lett. .

Abstract

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.

Keywords: Medchem; PCSK9; Parallel synthesis; SAR; Urea.

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