Search Results - "Groneberg, Robert D"
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Synthesis, structure–property relationships and pharmacokinetic evaluation of ethyl 6-aminonicotinate sulfonylureas as antagonists of the P2Y12 receptor
Published in European journal of medicinal chemistry (01-07-2013)“…The present paper describes the development of a new series of P2Y12 receptor antagonists based on our previously reported piperazinyl urea series 1 (IC50…”
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Tetrazole and ester substituted tetrahydoquinoxalines as potent cholesteryl ester transfer protein inhibitors
Published in Bioorganic & medicinal chemistry letters (01-05-2007)“…The SAR and synthesis of a series of substituted tetrahydroquinoxaline CETP inhibitors is described from early lead to advanced analogs. Cholesteryl ester…”
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5-alkyl-1,3-oxazole derivatives of 6-amino-nicotinic acids as alkyl ester bioisosteres are antagonists of the P2Y12 receptor
Published in Future medicinal chemistry (01-11-2013)“…Recently, we reported ethyl nicotinates as antagonists of the P2Y12 receptor, which is an important target in antiplatelet therapies. A potential liability of…”
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Identification of a Nonpeptidic and Conformationally Restricted Bradykinin B1 Receptor Antagonist with Anti-Inflammatory Activity
Published in Journal of medicinal chemistry (22-02-2007)“…We report the discovery of chroman 28, a potent and selective antagonist of human, nonhuman primate, rat, and rabbit bradykinin B1 receptors (0.4−17 nM). At 90…”
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Potent Nonpeptide Antagonists of the Bradykinin B1 Receptor: Structure−Activity Relationship Studies with Novel Diaminochroman Carboxamides
Published in Journal of medicinal chemistry (03-05-2007)“…The bradykinin B1 receptor is induced following tissue injury and/or inflammation. Antagonists of this receptor have been studied as promising candidates for…”
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Nanomolar Inhibitors for Two Distinct Biological Target Families from a Single Synthetic Sequence: A Next Step in Combinatorial Library Design?
Published in Angewandte Chemie International Edition (02-11-1998)“…One common synthetic route creates small‐molecule libraries directed toward two functionally distinct target families. The novel structural template 1 can…”
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A new class of bradykinin 1 receptor antagonists containing the piperidine acetic acid tetralin core
Published in Bioorganic & medicinal chemistry letters (15-04-2006)“…Compound 1 was an early lead in our bradykinin 1 receptor antagonist program. By adding two conformational constraints to this compound and by exploring the…”
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Dual Inhibition of Phosphodiesterase 4 and Matrix Metalloproteinases by an (Arylsulfonyl)hydroxamic Acid Template
Published in Journal of medicinal chemistry (25-02-1999)Get full text
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Total synthesis of the oligosaccharide fragment of calicheamicin .gamma.1I
Published in Journal of the American Chemical Society (01-10-1990)Get full text
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Synthesis of the calicheamicin gamma(1)(I) oligosaccharide
Published 01-01-1991“…The calicheamicin $\gamma\sb1\sp{\rm I}$ oligosaccharide represents one of the most complex and unique carbohydrates to be isolated to date. Thus, its…”
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Dissertation -
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Synthese von Inhibitoren für zwei Familien biologischer Targets in einer Sequenz: ein nächster Schritt beim Aufbau kombinatorischer Bibliotheken?
Published in Angewandte Chemie (16-10-1998)“…Über nureinen Syntheseweg lassen sich Bibliotheken aus niedermolekularen Verbindungen aufbauen, die auf zwei Targetfamilien mit unterschiedlichen…”
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Synthese von Inhibitoren für zwei Familien biologischer Targets in einer Sequenz: ein nächster Schritt beim Aufbau kombinatorischer Bibliotheken?
Published in Angewandte Chemie (16-10-1998)Get full text
Journal Article