title: Non-peptide alpha v beta 3 antagonists. Part 7: 3-Substituted tetrahydro-naphthyridine derivatives.
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.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA. jiabing_wnag@merck.com
authors.forename: Jiabing
authors.initials: J
authors.lastname: Wang
authors.forename: Michael J
authors.initials: MJ
authors.lastname: Breslin
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Coleman
authors.forename: Mark E
authors.initials: ME
authors.lastname: Duggan
authors.forename: Cecilia A
authors.initials: CA
authors.lastname: Hunt
authors.forename: John H
authors.initials: JH
authors.lastname: Hutchinson
authors.forename: Chih-Tai
authors.initials: CT
authors.lastname: Leu
authors.forename: Sevgi B
authors.initials: SB
authors.lastname: Rodan
authors.forename: Gideon A
authors.initials: GA
authors.lastname: Rodan
authors.forename: Le T
authors.initials: LT
authors.lastname: Duong
authors.forename: George D
authors.initials: GD
authors.lastname: Hartman
mesh_terms: D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis / Q000494:pharmacology*; D000319:Adrenergic beta-Antagonists / Q000138:chemical synthesis / Q000494:pharmacology*; D006801:Humans; D039302:Integrin alphaVbeta3 / Q000037:antagonists & inhibitors*; D015394:Molecular Structure; D009287:Naphthyridines / Q000138:chemical synthesis / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000317:Adrenergic alpha-Antagonists; D000319:Adrenergic beta-Antagonists; D039302:Integrin alphaVbeta3; D009287:Naphthyridines