title: Synthesis and SAR of a novel, potent and structurally simple LTD4 antagonist of the quinoline class.
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.
authors.affiliation: Research Department, Novartis Pharma AG, Basel, Switzerland. andreas.von_sprecher@pharma.novartis.com
authors.forename: A
authors.initials: A
authors.lastname: von Sprecher
authors.forename: M
authors.initials: M
authors.lastname: Gerspacher
authors.forename: A
authors.initials: A
authors.lastname: Beck
authors.forename: S
authors.initials: S
authors.lastname: Kimmel
authors.forename: H
authors.initials: H
authors.lastname: Wiestner
authors.forename: G P
authors.initials: GP
authors.lastname: Anderson
authors.forename: U
authors.initials: U
authors.lastname: Niederhauser
authors.forename: N
authors.initials: N
authors.lastname: Subramanian
authors.forename: M A
authors.initials: MA
authors.lastname: Bray
mesh_terms: D000818:Animals; D018927:Anti-Asthmatic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001682:Biological Availability; D016084:Bronchoconstriction / Q000187:drug effects; D002144:Callithrix; D006168:Guinea Pigs; D007202:Indicators and Reagents; D020024:Leukotriene Antagonists / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D017998:Leukotriene D4 / Q000037:antagonists & inhibitors*; D017999:Leukotriene E4 / Q000037:antagonists & inhibitors; D008968:Molecular Conformation; D015394:Molecular Structure; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry* / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D018927:Anti-Asthmatic Agents; C112382:CGP 57698; D007202:Indicators and Reagents; D020024:Leukotriene Antagonists; D011804:Quinolines; D017998:Leukotriene D4; D017999:Leukotriene E4