QUINOLINE DERIVATIVE HAVING SEROTONIN-3 RECEPTOR ANTAGONIZING ACTIVITY
Quinoline derivatives represented by formula (I): STR1 wherein A-B-D represents--C(COO--Y)=CH--C(OR)= (wherein Y represents 8-methyl-8-azabicyclo[3.2.1]oct-3-yl group and R represents alkyl) or--C(OH)=C(COX--Y)--CH= (wherein X represents--O--or--NH--; and Y has the same meaning as described above), or a pharmaceutically acceptable salt thereof, possess potent 5HT 3 antagonizing activity and are useful as antiemetic agents.
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(2008/06/13)
5-HT3 Receptor Antagonists. 1. New Quinoline Derivatives
A series of esters and amides of 1-alkyl-2-oxo-1,2-dihydroquinoline-4-carboxylic acid or 2-alkoxyquinoline-4-carboxylic acid containing a basic azabicycloalkyl moiety has been synthesized and evaluated for affinity for the 3H>quipazine-labeled