Synthesis and Structure−Activity Relationships of Carboxyflavones as Structurally Rigid CysLT1 (LTD4) Receptor Antagonists

The synthesis and CysLT1 receptor affinities of a new series of highly rigid 3'- and 4'-(2-quinolinylmethoxy)- or 3'- and 4'-[2-(2-quinolinyl)ethenyl]-substituted, 6-, 7-, or 8-carboxylated flavones are described. CysLT1 receptor affinities of the flavones (down to 11 nM) were de...

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Bibliographic Details
Published in:	Journal of medicinal chemistry Vol. 41; no. 9; pp. 1428 - 1438
Main Authors:	ZWAAGSTRA, Mariël E., TIMMERMAN, Henk, VAN DE STOLPE, Andrea C., DE KANTER, Frans J. J., TAMURA, Masahiro, WADA, Yasushi, ZHANG, Ming-Qiang
Format:	Journal Article
Language:	English
Published:	Washington, DC American Chemical Society 23-04-1998
Subjects:	Animals Anti-Asthmatic Agents - chemical synthesis Anti-Asthmatic Agents - chemistry Anti-Asthmatic Agents - metabolism Anti-Asthmatic Agents - pharmacology Biological and medical sciences Flavonoids - chemical synthesis Flavonoids - chemistry Flavonoids - metabolism Flavonoids - pharmacology Guinea Pigs Ileum - drug effects Ileum - physiology In Vitro Techniques Leukotriene Antagonists Leukotriene D4 - metabolism Leukotriene D4 - pharmacology Lung - drug effects Lung - metabolism Male Medical sciences Membrane Proteins Muscle Contraction - drug effects Muscle, Smooth - drug effects Muscle, Smooth - physiology Pharmacology. Drug treatments Quinolines - chemical synthesis Quinolines - chemistry Quinolines - metabolism Quinolines - pharmacology Receptors, Leukotriene - metabolism Respiratory system Structure-Activity Relationship Rat Bronchodilator Lung Rodentia Quinoline derivatives Steric hindrance Leukotriene D4 Flavonoid Ileum In vitro Vertebrata Mammalia Guinea pig Structure activity relation Carboxylic acid Animal Styrene derivatives Antagonist Chemical synthesis Biological receptor
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