| Literature DB >> 30482620 |
Allyn T Londregan1, Gary Aspnes2, Chris Limberakis2, Paula M Loria2, Kim F McClure2, Donna N Petersen2, Brian Raymer2, Roger B Ruggeri2, Liuqing Wei2, Jun Xiao2, David W Piotrowski2.
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.Entities:
Keywords: Medchem; PCSK9; Parallel synthesis; SAR; Urea
Mesh：
Substances：
Year: 2018 PMID： 30482620 DOI： 10.1016/j.bmcl.2018.10.029
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823