Abstract
The two geminal ethyl groups in the succinic acid moiety of CGP57698 (4-[3-(7-fluoro-2-quinolinyl-methoxy)phenyl-amino]-2,2-diethyl-4-oxo- butanoic acid) are responsible for the high in vitro and in vivo potency of this peptidoleukotriene antagonist of the quinoline type. The synthesis and structure activity relationships of CGP57698 and its analogs are described.
MeSH terms
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Animals
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Anti-Asthmatic Agents / chemical synthesis
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Anti-Asthmatic Agents / chemistry
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Anti-Asthmatic Agents / pharmacology
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Biological Availability
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Bronchoconstriction / drug effects
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Callithrix
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Guinea Pigs
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Indicators and Reagents
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Leukotriene Antagonists / chemical synthesis*
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Leukotriene Antagonists / chemistry
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Leukotriene Antagonists / pharmacology
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Leukotriene D4 / antagonists & inhibitors*
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Leukotriene E4 / antagonists & inhibitors
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Molecular Conformation
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Molecular Structure
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Quinolines / chemical synthesis*
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Quinolines / chemistry*
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Quinolines / pharmacology
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Rats
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Structure-Activity Relationship
Substances
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Anti-Asthmatic Agents
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CGP 57698
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Indicators and Reagents
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Leukotriene Antagonists
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Quinolines
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Leukotriene D4
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Leukotriene E4