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

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.

journal_name

Bioorg Med Chem Lett

authors

Londregan AT,Aspnes G,Limberakis C,Loria PM,McClure KF,Petersen DN,Raymer B,Ruggeri RB,Wei L,Xiao J,Piotrowski DW

doi

10.1016/j.bmcl.2018.10.029

subject

Has Abstract

pub_date

2018-12-15 00:00:00

pages

3685-3688

issue

23-24

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(18)30831-X

journal_volume

28

pub_type

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