Author/Authors :
J. Scott Sawyer، نويسنده , , K. Jeff Thrasher، نويسنده , , Nicholas J. Bach، نويسنده , , Peter W. Stengel، نويسنده , , Sandra L. Cockerham، نويسنده , , Steven A. Silbaugh، نويسنده , , Carlos R. Roman، نويسنده , , Larry L. Froelich، نويسنده , , Jerome H. Fleisch، نويسنده ,
Abstract :
A series of quinoline-substituted dihydroindoles has been synthesized and evaluated as antagonists of the cysLT1 receptor. This series, exemplified by 2 (LY302905; pKi = 8.3 for inhibition of binding of 3H-LTD4 to guinea pig lung membranes), represents reduced analogues of the corresponding indoles that were previously shown to be potent, orally active cysLT1 receptor antagonists. These dihydroindole compounds generally displayed increased in vitro and in vivo (oral) activity.
