Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics

Amy E Zartman; Le T Duong; Carmen Fernandez-Metzler; George D Hartman; Chih-Tai Leu; Thomayant Prueksaritanont; Gideon A Rodan; Sevgi B Rodan; Mark E Duggan; Robert S Meissner

doi:10.1016/j.bmcl.2005.01.051

Nonpeptide alpha(v)beta3 antagonists: identification of potent, chain-shortened 7-oxo RGD mimetics

Bioorg Med Chem Lett. 2005 Mar 15;15(6):1647-50. doi: 10.1016/j.bmcl.2005.01.051.

Authors

Amy E Zartman¹, Le T Duong, Carmen Fernandez-Metzler, George D Hartman, Chih-Tai Leu, Thomayant Prueksaritanont, Gideon A Rodan, Sevgi B Rodan, Mark E Duggan, Robert S Meissner

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. [email protected]

PMID: 15745815
DOI: 10.1016/j.bmcl.2005.01.051

Abstract

Potent, novel 7-oxo alpha(v)beta3 antagonists have been prepared. These antagonists offer decreased plasma protein binding and excellent pharmacokinetic profiles.

MeSH terms

Animals
Dogs
Heterocyclic Compounds, 2-Ring / chemistry*
Heterocyclic Compounds, 2-Ring / pharmacokinetics
Heterocyclic Compounds, 2-Ring / pharmacology*
Integrin alphaVbeta3 / antagonists & inhibitors*
Models, Chemical
Molecular Structure
Oligopeptides
Osteoporosis / drug therapy
Structure-Activity Relationship

Substances

Heterocyclic Compounds, 2-Ring
Integrin alphaVbeta3
Oligopeptides
arginyl-glycyl-aspartic acid