Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 52, Issue 9, Pages 2794-2798Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm801583j
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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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