496841-09-9Relevant articles and documents
Discovery of potent, orally-active, and muscle-selective androgen receptor modulators based on an N-aryl-hydroxybicyclohydantoin scaffold
Sun, Chongqing,Robl, Jeffrey A.,Wang, Tammy C.,Huang, Yanting,Kuhns, Joyce E.,Lupisella, John A.,Beehler, Blake C.,Golla, Rajasree,Sleph, Paul G.,Seethala, Ramakrishna,Fura, Aberra,Krystek Jr., Stanley R.,An, Yongmi,Malley, Mary F.,Sack, John S.,Salvati, Mark E.,Grover, Gary J.,Ostrowski, Jacek,Hamann, Lawrence G.
, p. 7596 - 7599 (2006)
A novel, N-aryl-bicyclohydantoin selective androgen receptor modulator scaffold was discovered through structure-guided modifications of androgen receptor antagonists. A prototype compound (7R,7aS)-10b from this series is a potent and highly tissue-selective agonist of the androgen receptor. After oral dosing in a rat atrophied levator ani muscle model, (7R,7aS)-10b demonstrated efficacy at restoring levator ani muscle mass to that of intact controls and exhibited >50-fold selectivity for muscle over prostate.
Synthesis and SAR of tetrahydropyrrolo[1,2-b][1,2,5]thiadiazol-2(3H)-one 1,1-dioxide analogues as highly potent selective androgen receptor modulators
Manfredi, Mark C.,Bi, Yingzhi,Nirschl, Alexandra A.,Sutton, James C.,Seethala, Ramakrishna,Golla, Rajasree,Beehler, Blake C.,Sleph, Paul G.,Grover, Gary J.,Ostrowski, Jacek,Hamann, Lawrence G.
, p. 4487 - 4490 (2008/02/12)
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.