First Demonstration of In Vivo PDE11A4 Target Engagement for Potential Treatment of Age-Related Memory Disorders

J Med Chem. 2024 Oct 10;67(19):17774-17784. doi: 10.1021/acs.jmedchem.4c01794. Epub 2024 Sep 25.

Abstract

PDE11A4 is a target of interest for the treatment of age-related memory disorders. A previous report from our laboratories described an amide series of potent, selective PDE11A4 inhibitors that was metabolically unstable. Investigation of heterocyclic amide isosteres for the labile amide moiety revealed distinct structure-activity relationships and identified several compounds with potency comparable to the amide series. This manuscript describes the characterization of structure-activity and structure-property relationships in this set, leading to the identification of an orally bioavailable, brain-penetrant, selective and potent PDE11A4 inhibitor. Target engagement experiments demonstrated PDE11A4 inhibition in the hypothalamus of mice that was absent in PDE11A4 knock out animals.

MeSH terms

  • Aging
  • Animals
  • Humans
  • Hypothalamus / metabolism
  • Male
  • Memory Disorders* / drug therapy
  • Mice
  • Mice, Knockout
  • Structure-Activity Relationship