Synthesis and SAR of a novel, potent and structurally simple LTD 4 antagonist of the quinoline class

…, GP Anderson, U Niederhauser, N Subramanian…

Index: Von Sprecher, Andreas; Gerspacher, Marc; Beck, Andreas; Kimmel, Sabine; Wiestner, Hansruedi; Anderson, Gary P.; Niederhauser, Ulrich; Subramanian, Natarajan; Bray, Michael A. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 8 p. 965 - 970

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Citation Number: 34

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.