A preliminary study of the metabolic stability of a series of benzoxazinone derivatives as potent neuropeptide Y5 antagonists

Bioorg Med Chem Lett. 2005 Aug 15;15(16):3679-84. doi: 10.1016/j.bmcl.2005.05.103.

Abstract

The metabolic stability of benzoxazinone derivatives, a potent series of NPY Y5 antagonists, has been investigated. This study resulted in the identification of the structural moieties prone to metabolic transformations and which strongly influenced the in vitro half-life. This provides opportunities to optimize the structure of this new class of NPY Y5 antagonists.

MeSH terms

  • Drug Evaluation, Preclinical
  • Drug Stability
  • Molecular Structure
  • Oxazines / chemistry
  • Oxazines / metabolism*
  • Oxazines / pharmacology*
  • Receptors, Neuropeptide Y / antagonists & inhibitors*
  • Receptors, Neuropeptide Y / metabolism
  • Structure-Activity Relationship

Substances

  • Oxazines
  • Receptors, Neuropeptide Y
  • neuropeptide Y5 receptor