- Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.
Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.
Bioorganic & medicinal chemistry letters (2004-03-12)
Jiabing Wang, Michael J Breslin, Paul J Coleman, Mark E Duggan, Cecilia A Hunt, John H Hutchinson, Chih-Tai Leu, Sevgi B Rodan, Gideon A Rodan, Le T Duong, George D Hartman
PMID15013021
RESUMO
A series of 3-substituted tetrahydro-[1,8]naphthyridine containing alpha(v)beta(3) antagonists was prepared. A comparison of their in vitro IC(50) values to the electron properties of the 3-substituents revealed a good linear Hammett correlation (rho=-1.96, R(2)=0.959). Electron-withdrawing groups at the 3-position of the tetrahydro-[1,8]naphthyridine decreased potency while electron-donating groups enhanced potency.