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

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

  • Bioorg Med Chem Lett. 2018 Dec 15;28(23-24):3685-3688. doi: 10.1016/j.bmcl.2018.10.029.
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

Affiliations

  • 1 Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States. Electronic address: allyn.t.londregan@pfizer.com.
  • 2 Pfizer Medicinal Chemistry, Pfizer Inc., Eastern Point Road, Groton, CT 06340, United States.
PMID: 30482620 DOI: 10.1016/j.bmcl.2018.10.029
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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