149168-09-2Relevant academic research and scientific papers
Substituted indoles as potent and orally active 5-lipoxygenase activating protein (FLAP) inhibitors
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
, p. 2391 - 2396 (2007/10/03)
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.
(hetero-arylmethoxy)indoles as inhibitors of leukotriene biosynthesis
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, (2008/06/13)
Compounds having the formula I: STR1 are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, pl
