Non-peptide α v β 3 antagonists. Part 7: 3-Substituted tetrahydro- [1,8] naphthyridine derivatives

Autor: Michael J. Breslin, Sevgi B. Rodan, Gideon A. Rodan, Chih-Tai Leu, George D. Hartman, John H. Hutchinson, Le T. Duong, Hunt Cecilia, Mark E. Duggan, Paul J. Coleman, Jiabing Wang
Rok vydání: 2004
Předmět:
Zdroj: Bioorganic & Medicinal Chemistry Letters. 14:1049-1052
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2003.11.036
Popis: A series of 3-substituted tetrahydro-[1,8]naphthyridine containing α v β 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 (ρ=−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.
Databáze: OpenAIRE