Bioorganic & Medicinal Chemistry Letters 2004-02-23

Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.

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

Index: Bioorg. Med. Chem. Lett. 14 , 1049, (2004)

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Abstract

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.