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

Authors :
Wang J
Breslin MJ
Coleman PJ
Duggan ME
Hunt CA
Hutchinson JH
Leu CT
Rodan SB
Rodan GA
Duong LT
Hartman GD
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2004 Feb 23; Vol. 14 (4), pp. 1049-52.
Publication Year :
2004

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.

Details

Language :
English
ISSN :
0960-894X
Volume :
14
Issue :
4
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
15013021
Full Text :
https://doi.org/10.1016/j.bmcl.2003.11.036