62646-04-2Relevant academic research and scientific papers
COMPOSITIONS AND TREATMENTS COMPRISING 5-LIPOXYGENASE-ACTIVATING PROTEIN INHIBITORS AND NITRIC OXIDE MODULATORS
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Page/Page column 99, (2008/12/06)
Disclosed herein are compositions and compounds that combine an inhibitor of 5-lipoxygenase activating protein (FLAP) and a modulator of NO levels in a mammal. The NO modulator can be an agent that induces the production of NO in a mammal, or can be an ag
Synthesis of indolylalkoxyiminoalkylcarboxylates as leukotriene biosynthesis inhibitors
Kolasa, Teodozyj,Bhatia, Pramila,Brooks, Clint D. W.,Hulkower, Keren I.,Bouska, Jennifer B.,Harris, Richard R.,Bell, Randy L.
, p. 507 - 514 (2007/10/03)
A series of substituted indolylalkoxyiminoalkylcarboxylates were found to be potent leukotriene biosynthesis inhibitors. The structure-activity relationships were investigated. Representative potent inhibitors identified were the quinolyl 3a (A-86885) and pyridyl 3b (A-86886) congeners with in vitro IC50s of 21 and 9 nM and in vivo leukotriene inhibition in the rat with oral ED50s of 0.9 and 1.7 mg/kg, respectively.
INDOLE IMINOOXY DERIVATIVES WHICH INHIBIT LEUKOTRIENE BIOSYNTHESIS
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, (2008/06/13)
Compounds of the structure where A1 is alkylene or cycloalkylene; A2 is a valence bond, alkylene, or cycloalkylene; R1 is selected from hydrogen, alkylthio, optionally substituted phenylthio, optionally substituted phenylalkylthio, optionally substituted
THIOPYRANO(2,3,4-C,D) INDOLYLOXIME ETHER ALKYLCARBOXYLATES
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, (2008/06/13)
Compounds of the structure R1 is selected from the group consisting of are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes.These compounds are useful in the treatment or amelioration of allergic and inflammator
Friedel-Crafts Cyclization of 2-(3-Indolylthio)propionic Acids. An Unusual Rearrangement Leading to 4-Sulfur-Substituted Tricyclic Indoles
Chung, John Y. L.,Reamer, Robert A.,Reider, Paul J.
, p. 4717 - 4720 (2007/10/02)
The intramolecular Friedel-Crafts acylation of 2-(3-indolylthio)propionic acid 1 has been found to undergo an unprecedented rearrangement to provide a novel tricyclic indole having the sulfur substituted on C-4 rather than on the expected C-3.A mechanism for its formation is proposed.This rearrangement also proceeded with good optical retention when a chiral substrate was used.Key Words: Friedel-Crafts acylation; rearrangement; tricyclic indoles; 4-thio-indoles; thiopyranoindoles.
