LTD(4) RECEPTOR-BINDING ACTIVITY OF NOVEL PYRIDINE CHROMANOLS - QUALITATIVE CORRELATION WITH PK(A)

Authors
MASAMUNE H EGGLER JF MARFAT A MELVIN LS RUSEK FW TICKNER JE CHENG JB SHIRLEY JT
Citation
H. Masamune et al., LTD(4) RECEPTOR-BINDING ACTIVITY OF NOVEL PYRIDINE CHROMANOLS - QUALITATIVE CORRELATION WITH PK(A), Bioorganic & medicinal chemistry letters, 5(13), 1995, pp. 1371-1376
Citations number
13
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
13
Year of publication
1995
Pages
1371 - 1376
Database
ISI
SICI code
0960-894X(1995)5:13<1371:LRAONP>2.0.ZU;2-C
Abstract
A series of pyridine chromanols were synthesized and evaluated as LTD( 4)-antagonists (LTD(4)-A). The quinoline sidechain of this class of su ch agents, as exemplified by REV-5901, has until now been deemed as es sential for potent activity. However, by manipulating substituents on a pyridine ring, quinoline-like potency can be achieved. The results i ndicate that this is a function of pKa.