5-lipoxygenase-activating protein (FLAP) inhibitors. Part 4: Development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin- 2-ylmethoxy)-1 H -indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor

Journal of Medicinal Chemistry

Volumn 54, Issue 23, 2011, Pages 8013-8029

  Stock, Nicholas S ^a   Bain, Gretchen ^a   Zunic, Jasmine ^a   Li, Yiwei ^a   Ziff, Jeannie ^a   Roppe, Jeffrey ^a   Santini, Angelina ^a   Darlington, Janice ^a   Prodanovich, Pat ^a   King, Christopher D ^a   Baccei, Christopher ^a   Lee, Catherine ^a   Rong, Haojing ^a   Chapman, Charles ^a   Broadhead, Alex ^a   Lorrain, Dan ^a   Correa, Lucia ^a   Hutchinson, John H ^a   Evans, Jilly F ^a   Prasit, Peppi ^a  

^a Amira Pharmaceuticals   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [3 TERT BUTYLSULFANYL 1 [4 (6 ETHOXYPYRIDIN 3 YL)BENZYL] 5 (5 METHYLPYRIDIN 2 YLMETHOXY) 1H INDOL 2 YL] 2,2 DIMETHYLPROPIONIC ACID; AM 803; ARACHIDONATE 5 LIPOXYGENASE ACTIVATING PROTEIN INHIBITOR; GSK 2190915; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; ASTHMA; BLOOD; CONTROLLED STUDY; DRUG BINDING; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG EFFICACY; DRUG HALF LIFE; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; EXPERIMENTAL DOG; FEMALE; HUMAN; IC 50; MALE; NONHUMAN; PHASE 1 CLINICAL TRIAL (TOPIC); PHASE 2 CLINICAL TRIAL (TOPIC); RAT; STRUCTURE ACTIVITY RELATION;

5-LIPOXYGENASE-ACTIVATING PROTEIN INHIBITORS; ADMINISTRATION, ORAL; ANIMALS; ANTI-ASTHMATIC AGENTS; BRONCHOALVEOLAR LAVAGE; CYTOCHROME P-450 ENZYME SYSTEM; DOGS; FEMALE; HUMANS; INDOLES; MALE; PENTANOIC ACIDS; RATS; RATS, SPRAGUE-DAWLEY; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 82555168047     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm2008369     Document Type: Article

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