Synthesis and SAR of a novel, potent and structurally simple LTD4 antagonist of the quinoline class.

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von Sprecher A, Gerspacher M, Beck A, Kimmel S, Wiestner H, Anderson GP, Niederhauser U, Subramanian N, Bray MA

Synthesis and SAR of a novel, potent and structurally simple LTD4 antagonist of the quinoline class.

Bioorg Med Chem Lett. 1998 Apr 21;8(8):965-70.

PubMed ID

9871521 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Zafirlukast	Cysteinyl leukotriene receptor 1	IC 50 (nM)	44	N/A	N/A	Details