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Updated: Jun 24, 2026

Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
Published on: November 15, 2013
N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore
Alexandra A Nirschl1, Yan Zou, Stanley R Krystek
1Discovery Chemistry, Analytical Research & Development, Bristol-Myers Squibb Research and Development, P.O. Box 5400, Princeton, New Jersey 08543-5400, USA.
Abstract:
A novel selective androgen receptor modulator (SARM) scaffold was discovered as a byproduct obtained during synthesis of our earlier series of imidazolidin-2-ones. The resulting oxazolidin-2-imines are among the most potent SARMs known, with many analogues exhibiting sub-nM in vitro potency in binding and functional assays. Despite the potential for hydrolytic instability at gut pH, compounds of the present class showed good oral bioavailability and were highly active in a standard rodent pharmacological model.
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