- QUINOLINE DERIVATIVE HAVING SEROTONIN-3 RECEPTOR ANTAGONIZING ACTIVITY
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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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- 5-HT3 Receptor Antagonists. 1. New Quinoline Derivatives
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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
- Hayashi, Hiroaki,Miwa, Yoshikazu,Miki, Ichiro,Ichikawa, Shunji,Yoda, Noboyuki,et al.
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p. 4893 - 4902
(2007/10/02)
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- QUINOLINE SUBSTITUTED OXOMETHYL OR THIOXOMETHYL GLYCINE DERIVATIVES AND ALDOSE REDUCTASE INHIBITON THEREWITH
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A compound of the formula (I): or a pharmaceutically acceptable salt thereof, wherein Y is S or O; R is hydrogen or alkyl having from about 1 to about 4carbon atoms; R1 is hydrogen, alkyl having from about 1 to about 4carbon atoms, alkoxy having from about 1 to about 4carbon atoms, halogen or trifluoromethyl; R2 is hydrogen or unsubstituted or substituted alkyl having from about 1 to about 4 carbon atoms; and R3 is hydrogen, alkyl having from about 1 to about 6carbon atoms, cycloalkyl having from about 3 to about 6 carbon atoms, alkoxy having from about 1 to about 4 carbon atoms, aryloxy having from about 6 to about 10 carbon atoms, alkylthio having from about 1 to about 4 carbon atoms, hydroxyalkoxy having from about 1 to about 4 carbon atoms, or unsubstituted or substituted phenyl is useful to obtain inhibition of aldose reduction in animals, including humans.
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