431988-79-3Relevant articles and documents
Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats
Cameron, Kimberly O.,Lefker, Bruce A.,Chu-Moyer, Margaret Y.,Crawford, David T.,Jardine, Paul DaSilva,DeNinno, Shari L.,Gilbert, Sandra,Grasser, William A.,Ke, HuaZhu,Lu, Bihong,Owen, Thomas A.,Paralkar, Vishwas M.,Qi, Hong,Scott, Dennis O.,Thompson, David D.,Tjoa, Christina M.,Zawistoski, Michael P.
, p. 1799 - 1802 (2007/10/03)
Heptanoic acid lactams, exemplified by 2, were identified as highly selective EP4 agonists via high throughput screening. Lead optimization led to the identification of lactams with a 30-fold increase in EP4 potency in vitro. Compounds demonstrated robust