227937-97-5Relevant academic research and scientific papers
Non-peptide αvβ3 antagonists: Identification of potent, chain-shortened RGD mimetics that incorporate a central pyrrolidinone constraint
Perkins, James J.,Duong,Fernandez-Metzler, Carmen,Hartman, George D.,Kimmel, Donald B.,Leu, Chih-Tai,Lynch, Joseph J.,Prueksaritanont, Thomayant,Rodan, Gideon A.,Rodan, Sevgi B.,Duggan, Mark E.,Meissner, Robert S.
, p. 4285 - 4288 (2007/10/03)
Antagonists of the integrin receptor αvβ3 are expected to have utility in the treatment of osteoporosis through inhibition of bone resorption. A series of potent, chain-shortened, pyrrolidinone-containing αvβ3 receptor antagonists is described. Two sets of diasteromeric pairs of high-affinity antagonists demonstrated marked differences in log P values, which translated into differing dog pharmacokinetic properties. One member of this set was demonstrated to be effective in reducing bone resorption in rats.
