Search Results - "Kubrak, Dennis"
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( S) -N-(5-Chlorothiophene-2-sulfonyl)-β,β-diethylalaninol a Notch-1-sparing γ-secretase inhibitor
Published in Bioorganic & medicinal chemistry letters (01-02-2009)“…Accumulation of beta-amyloid (Aβ), produced by the proteolytic cleavage of amyloid precursor protein (APP) by β- and γ-secretase, is widely believed to be…”
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Etodolac selectively inhibits human prostaglandin G/H synthase 2 (PGHS-2) versus human PGHS-1
Published in European journal of pharmacology (25-07-1995)“…The isozymes of prostaglandin G/H synthase (PGHS) are shown to be differentially inhibited in vitro by currently marketed nonsteroidal anti-inflammatory drugs…”
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P2-337: Characterization of the affinity of GSI-953 for binding to gamma-secretase and comparison to benchmark gamma-secretase inhibitors
Published in Alzheimer's & dementia (01-07-2008)Get full text
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Discovery of Begacestat, a Notch-1-Sparing γ-Secretase Inhibitor for the Treatment of Alzheimer’s Disease
Published in Journal of medicinal chemistry (11-12-2008)“…SAR on HTS hits 1 and 2 led to the potent, Notch-1-sparing GSI 9, which lowered brain Aβ in Tg2576 mice at 100 mg/kg po. Converting the metabolically labile…”
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N-[(Arylmethoxy)phenyl] carboxylic acids, hydroxamic acids, tetrazoles, and sulfonyl carboxamides. Potent orally active leukotriene D4 antagonists of novel structure
Published in Journal of medicinal chemistry (01-01-1990)“…Four series of N-[(arylmethoxy)phenyl] compounds were prepared as leukotriene D4 (LTD4) antagonists. In the hydroxamic acid series, methyl…”
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N-[(Arylmethoxy)phenyl] and N-[(arylmethoxy)naphthyl] sulfonamides: potent orally active leukotriene d4 antagonists of novel structure
Published in Journal of medicinal chemistry (01-06-1989)“…Two series of compounds, N-[(arylmethoxy)phenyl] sulfonamides and N-[(arylmethoxy)naphthyl] sulfonamides, were prepared as leukotriene D4 (LTD4) antagonists…”
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Synthesis of [[(naphthalenylmethoxy)- and -(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters. A novel series of leukotriene D4 antagonists and 5-lipoxygenase inhibitors
Published in Journal of medicinal chemistry (01-08-1986)“…A series of novel [[(naphthalenylmethoxy)- and [[(quinolinylmethoxy)phenyl]amino]oxoalkanoic acid esters have been prepared. These compounds were tested as…”
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Discovery of a novel series of Notch-sparing γ-secretase inhibitors
Published in Bioorganic & medicinal chemistry (15-07-2008)“…Lead optimization studies of Notch-sparing GSI 2a led to the discovery of analog 8e with improved γ-secretase inhibitory potency and Notch-sparing selectivity…”
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Leukotriene D4 antagonists and 5-lipoxygenase inhibitors. Synthesis of benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters
Published in Journal of medicinal chemistry (01-02-1987)“…A series of novel benzoheterocyclic [(methoxyphenyl)amino]oxoalkanoic acid esters has been prepared. These compounds were tested as inhibitors of rat…”
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Asymmetric synthesis of novel α-amino acids with β-branched side chains
Published in Bioorganic & medicinal chemistry letters (01-05-2007)“…An asymmetric synthesis of α-amino acids with novel β-branched side chains has been implemented. The syntheses feature a p-toluenesulfinylimine induced chiral…”
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P4-244: Discovery of a novel series of notch-sparing γ-secretase inhibitors
Published in Alzheimer's & dementia (01-07-2006)Get full text
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Phenylephrine derivatives as leukotriene D4 antagonists
Published in Journal of medicinal chemistry (01-11-1987)Get full text
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