Bioorganic and Medicinal Chemistry Letters p. 2391 - 2396 (1999)
Update date:2022-08-04
Topics:
Frenette, Richard
Hutchinson, John H.
Leger, Serge
Therien, Michel
Brideau, Christine
Chan, Chi C.
Charleson, Stella
Ethier, Diane
Guay, Jocelyne
Jones, Tom R.
McAuliffe, Malia
Piechuta, Hanna
Riendeau, Denis
Tagari, Philip
Girard, Yves
This paper reports on the SAR investigation of inhibitors of 5- lipoxygenase activating protein (FLAP) based on MK-0591. Emphasis was made on modifications to the nature of the link between the indole and the quinoline moieties, to the substitution pattern around the two heterocycles and to possible replacements of the quinoline moiety. Lead optimization culminated in (3-[1-(4-chlorobenzyl)-3-(t-butylthio)-5-(pyridin-2-ylmethoxy)-indol-2- yl]-2,2-dimethylpropanoic acid (18k), as a potent inhibitor of leukotriene biosynthesis that is well absorbed and active in functional models.
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