Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1377398 | Bioorganic & Medicinal Chemistry Letters | 2007 | 4 Pages |
Abstract
Replacement of the 3-oxo group of 2-chloro-4-[(7R,7aS)-7-hydroxy-1,3-dioxotetrahydro-1H-pyrrolo[1,2c]imidazol-2(3H)-yl]-3-methylbenzonitrile resulted in a sulfamide series of selective androgen receptor modulator (SARM) agonists.
Graphical abstractHerein, we report the effects of replacing the 3-oxo group of 2 with a sulfonyl group (e.g., 3). These tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues were found to be potent SARMs. Synthesis, binding and functional assay SAR, as well as in vivo characterization of a selected analogue in a standard rodent model are presented.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Authors
Mark C. Manfredi, Yingzhi Bi, Alexandra A. Nirschl, James C. Sutton, Ramakrishna Seethala, Rajasree Golla, Blake C. Beehler, Paul G. Sleph, Gary J. Grover, Jacek Ostrowski, Lawrence G. Hamann,