Search Results - "Bauer, Shawn M."
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Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-( N, N-dimethylcarbamimidoyl)benzamido)-5-methoxybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor
Published in Bioorganic & medicinal chemistry letters (15-04-2009)“…Systematic SAR studies of in vitro factor Xa inhibitory activity around compound 1 were performed by modifying each of the three phenyl rings. A class of…”
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Total Synthesis of Motuporin (Nodularin-V)
Published in Journal of the American Chemical Society (14-07-1999)“…The serine/threonine phosphatase (protein phosphatase 1 and 2A) inhibitors constitute a biologically and structurally interesting class of natural products…”
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ADP receptor antagonists as antiplatelet therapeutics
Published in Expert opinion on emerging drugs (01-05-2003)“…With the cloning of the P2Y12 receptor, the molecular basis for ADP-induced platelet aggregation is seemingly complete. Two platelet-bound ADP receptors, P2Y1…”
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N, N-Dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines as potent factor Xa inhibitors
Published in Bioorganic & medicinal chemistry letters (03-05-2004)“…A class of N,N-dialkylated 4-(4-arylsulfonylpiperazine-1-carbonyl)-benzamidines and 4-((4-arylsulfonyl)-2-oxo-piperazin-1-ylmethyl)-benzamidines has been…”
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Parallel synthesis and structure–activity relationships of a series of highly potent, selective, and neutral factor Xa inhibitors
Published in Bioorganic & medicinal chemistry letters (02-08-2004)“…Parallel synthesis and iterative optimization led to the discovery of a series of inhibitors having excellent in vitro and promising in vivo properties…”
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Discovery of betrixaban (PRT054021), N-(5-chloropyridin-2-yl)-2-(4-(N,N-dimethylcarbamimidoyl)benzamido )-5-metho xybenzamide, a highly potent, selective, and orally efficacious factor Xa inhibitor
Published in Bioorganic & medicinal chemistry letters (01-04-2009)“…Systematic SAR studies of in vitro factor Xa inhibitory activity around compound 1 were performed by modifying each of the three phenyl rings. A class of…”
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7
Construction of combinatorial chemical libraries using a rapid and efficient solid phase synthesis based on a multicomponent condensation reaction
Published in Tetrahedron letters (24-09-1998)“…A 96 member library of acylated dipeptides based on a known anticonvulsant was synthesized utilizing an Ugi four component condensation followed by…”
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Multicomponent solution phase synthesis of dehydroamino acid derivatives based on the Passerini reaction
Published in Tetrahedron letters (24-09-1998)“…We have synthesized a library of dehydroamino acid derivatives using a Passerini three component condensation reaction. A number of structurally diverse inputs…”
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