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J Med Chem. 2009 May 14;52(9):2794-8. doi: 10.1021/jm801583j.

N-aryl-oxazolidin-2-imine muscle selective androgen receptor modulators enhance potency through pharmacophore reorientation.

Author information

1
Discovery 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.

PMID:
19351168
DOI:
10.1021/jm801583j
[Indexed for MEDLINE]

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