8-AMINO-6-(ARYLSULFONYL)-5-NITROQUINOLINES - NOVEL NONPEPTIDE NEUROPEPTIDE Y1 RECEPTOR ANTAGONISTS

Authors
WRIGHT J BOLTON G CRESWELL M DOWNING D GEORGIC L HEFFNER T HODGES J MACKENZIE R WISE L
Citation
J. Wright et al., 8-AMINO-6-(ARYLSULFONYL)-5-NITROQUINOLINES - NOVEL NONPEPTIDE NEUROPEPTIDE Y1 RECEPTOR ANTAGONISTS, Bioorganic & medicinal chemistry letters, 6(15), 1996, pp. 1809-1814
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
15
Year of publication
1996
Pages
1809 - 1814
Database
ISI
SICI code
0960-894X(1996)6:15<1809:8-NNN>2.0.ZU;2-3
Abstract
A novel series of 8-amino-6-(arylsulphonyl)-5-nitroquinoline neuropept ide Y1 (NPY) receptor antagonists is reported. The 8-amino and 5-nitro groups were important for NPY1 binding affinity as changes caused lar ge drops in potency. The 6-arylsulphonyl group was necessary; however, substitution on the phenyl was tolerated. The 2-isopropyl analog 21 w as a moderately potent, highly selective NPY1 receptor antagonist. Cop yright (C) 1996 Elsevier Science Ltd