N-Aryl-oxazolidin-2-imine Muscle Selective Androgen Receptor Modulators Enhance Potency through Pharmacophore Reorientation
2009
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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