title: Evaluation of endo- and exo-aryl-substitutions and central scaffold modifications on diphenyl substituted alkanes as 5-lipoxygenase activating protein inhibitors.
abstract: A search for a suitable replacement for the central norbornyl scaffold presented in the recently disclosed novel FLAP inhibitors is herein described, as well as the SAR study performed on the endo and exo-aryl groups.
authors.affiliation: Discovery and Preclinical Sciences, Merck Research Laboratories, Rahway, NJ 07065, USA. lin_chu@merck.com
authors.forename: Lin
authors.initials: L
authors.lastname: Chu
authors.forename: Helen M
authors.initials: HM
authors.lastname: Armstrong
authors.forename: Linda L
authors.initials: LL
authors.lastname: Chang
authors.forename: Amy F
authors.initials: AF
authors.lastname: Cheng
authors.forename: Lawrence
authors.initials: L
authors.lastname: Colwell
authors.forename: Jisong
authors.initials: J
authors.lastname: Cui
authors.forename: Jilly
authors.initials: J
authors.lastname: Evans
authors.forename: Amy
authors.initials: A
authors.lastname: Galka
authors.forename: Mark T
authors.initials: MT
authors.lastname: Goulet
authors.forename: Nancy
authors.initials: N
authors.lastname: Hayes
authors.forename: Jane
authors.initials: J
authors.lastname: Lo
authors.forename: John
authors.initials: J
authors.lastname: Menke
authors.forename: Hyun O
authors.initials: HO
authors.lastname: Ok
authors.forename: Debra L
authors.initials: DL
authors.lastname: Ondeyka
authors.forename: Minal
authors.initials: M
authors.lastname: Patel
authors.forename: Grace M
authors.initials: GM
authors.lastname: Quaker
authors.forename: Heather
authors.initials: H
authors.lastname: Sings
authors.forename: Stephanie L
authors.initials: SL
authors.lastname: Witkin
authors.forename: Annie
authors.initials: A
authors.lastname: Zhao
authors.forename: Feroze
authors.initials: F
authors.lastname: Ujjainwalla
mesh_terms: D058946:5-Lipoxygenase-Activating Protein Inhibitors / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D058927:5-Lipoxygenase-Activating Proteins / Q000737:chemistry* / Q000378:metabolism; D000473:Alkanes / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D000818:Animals; D018926:Anti-Allergic Agents / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D001555:Benzene Derivatives / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D007275:Injections, Intravenous; D009504:Neutrophils / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D058946:5-Lipoxygenase-Activating Protein Inhibitors; D058927:5-Lipoxygenase-Activating Proteins; C548592:ALOX5AP protein, human; D000473:Alkanes; D018926:Anti-Allergic Agents; D001555:Benzene Derivatives