QUINOLINE-SUBSTITUTED DIHYDROINDOLES AS CYSLT(1) (LTD(4) RECEPTOR) ANTAGONISTS

Authors
SAWYER JS THRASHER KJ BACH NJ STENGEL PW COCKERHAM SL SILBAUGH SA ROMAN CR FROELICH LL FLEISCH JH
Citation
Js. Sawyer et al., QUINOLINE-SUBSTITUTED DIHYDROINDOLES AS CYSLT(1) (LTD(4) RECEPTOR) ANTAGONISTS, Bioorganic & medicinal chemistry letters, 6(3), 1996, pp. 249-252
Citations number
10
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
6
Issue
3
Year of publication
1996
Pages
249 - 252
Database
ISI
SICI code
0960-894X(1996)6:3<249:QDAC(R>2.0.ZU;2-4
Abstract
series of quinoline-substituted dihydroindoles has been synthesized an d evaluated as antagonists of the cysLT(1) receptor. This series, exem plified by 2 (LY302905, pKi = 8.3 for inhibition of binding of H-3-LTD (4) to guinea pig lung membranes), represents reduced analogues of the corresponding indoles that were previously shown to be potent, orally active cysLT(1) receptor antagonists. These dihydroindole compounds g enerally displayed increased in vitro and in vivo (oral) activity.