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ID: ALA1146126
Journal: Bioorg Med Chem Lett
Title: Discovery of highly selective EP4 receptor agonists that stimulate new bone formation and restore bone mass in ovariectomized rats.
Authors: Cameron KO, Lefker BA, Chu-Moyer MY, Crawford DT, Jardine PD, DeNinno SL, Gilbert S, Grasser WA, Ke H, Lu B, Owen TA, Paralkar VM, Qi H, Scott DO, Thompson DD, Tjoa CM, Zawistoski MP.
Abstract: 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 bone anabolic effects when administered in vivo in rat models of osteoporosis.
CiteXplore: 16442794