Search Results - "Jagdmann, Erik"
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Small-Molecule Antagonists of the RIG‑I Innate Immune Receptor
Published in ACS chemical biology (21-02-2020)“…The RIG-I receptor plays a key role in the vertebrate innate immune system, where it functions as a sensor for detecting infection by RNA viruses. Although…”
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Small molecules that target group II introns are potent antifungal agents
Published in Nature chemical biology (01-12-2018)“…Specific RNA structures control numerous metabolic processes that impact human health, and yet efforts to target RNA structures de novo have been limited. In…”
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Chemical Synthesis and Characterization of Epicatechin Glucuronides and Sulfates: Bioanalytical Standards for Epicatechin Metabolite Identification
Published in Journal of natural products (Washington, D.C.) (22-02-2013)“…The monoglucuronides and sulfates of epicatechin, 3′-O-methylepicatechin, and 4′-O-methylepicatechin, respectively, were synthesized as authentic bioanalytical…”
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Enantioselective synthesis of orthogonally protected (2R,3R)-(−)-epicatechin derivatives, key intermediates in the de novo chemical synthesis of (−)-epicatechin glucuronides and sulfates
Published in Tetrahedron: asymmetry (15-04-2013)“…Ten orthogonally protected (−)-epicatechin and 3′- or 4′-O-methyl-(−)-epicatechin derivatives were prepared in a regiospecific and enantioselective manner. For…”
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Discovery of (R)‑2-Amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic Acid and Congeners As Highly Potent Inhibitors of Human Arginases I and II for Treatment of Myocardial Reperfusion Injury
Published in Journal of medicinal chemistry (28-03-2013)“…Recent efforts to identify treatments for myocardial ischemia reperfusion injury have resulted in the discovery of a novel series of highly potent…”
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Discovery of Allosteric Potentiators for the Metabotropic Glutamate 2 Receptor: Synthesis and Subtype Selectivity of N-(4-(2-Methoxyphenoxy)phenyl)-N-(2,2,2− trifluoroethylsulfonyl)pyrid-3-ylmethylamine
Published in Journal of medicinal chemistry (17-07-2003)“…This report describes recently discovered novel allosteric modulators of metabotropic glutamate2 (mGlu2) receptors. These pyridylmethylsulfonamides (e.g., 3)…”
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Metabotropic glutamate 2 receptor potentiators: receptor modulation, frequency-dependent synaptic activity, and efficacy in preclinical anxiety and psychosis model(s)
Published in Psychopharmacology (01-04-2005)“…To increase subtype selectivity and provide a novel means to alter receptor function, we discovered and characterization potentiators for the metabotropic…”
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Discovery of N‑Substituted 3‑Amino-4-(3-boronopropyl)pyrrolidine-3-carboxylic Acids as Highly Potent Third-Generation Inhibitors of Human Arginase I and II
Published in Journal of medicinal chemistry (12-09-2019)“…Recent efforts to identify new highly potent arginase inhibitors have resulted in the discovery of a novel family of…”
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Synthesis and Protein Kinase Inhibitory Activity of Balanol Analogues with Modified Benzophenone Subunits
Published in Journal of medicinal chemistry (06-06-2002)“…A series of analogues of the protein kinase C (PKC) inhibitory natural product balanol which bear modified benzophenone subunits are described. The analogues…”
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Synthesis of quaternary α-amino acid-based arginase inhibitors via the Ugi reaction
Published in Bioorganic & medicinal chemistry letters (01-09-2013)“…The Ugi reaction has been successfully applied to the synthesis of novel arginase inhibitors. In an effort to decrease conformational flexibility of the…”
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SAR study of a subtype selective allosteric potentiator of metabotropic glutamate 2 receptor, N-(4-phenoxyphenyl)- N-(3-pyridinylmethyl)ethanesulfonamide
Published in Bioorganic & medicinal chemistry letters (21-06-2004)“…The structure–activity relationship of a subtype selective mGlu2 potentiator, LY181837 is explored. The major excitatory neurotransmitter in the Central…”
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2-Substituted-2-amino-6-boronohexanoic acids as arginase inhibitors
Published in Bioorganic & medicinal chemistry letters (01-04-2013)“…Substitution at the alpha center of the known human arginase inhibitor 2-amino-6-boronohexanoic acid (ABH) is acceptable in the active site pockets of both…”
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Synthesis of quaternary I--amino acid-based arginase inhibitors via the Ugi reaction
Published in Bioorganic & medicinal chemistry letters (01-09-2013)“…The Ugi reaction has been successfully applied to the synthesis of novel arginase inhibitors. In an effort to decrease conformational flexibility of the…”
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Two efficient syntheses of (±)- anti-N-benzyl-3-amino-4-hydroxyhexahydroazepine
Published in Tetrahedron letters (22-05-1995)“…Functionalization of ε-caprolactam ( 3) or Beckmann rearrangement of the syn-oxime derivative of 3-ethoxy-2-cyclohexen-1-one ( 12) provided efficient and…”
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Synthesis and biological evaluation of conformationally constrained bicyclic and tricyclic balanol analogues as inhibitors of protein kinase C
Published in Bioorganic & medicinal chemistry letters (05-10-1995)“…A series of conformationally constrained bicyclic ( 20–25 and 28) and tricyclic ( 26 and 27) balanol analogues was prepared and evaluated as inhibitors of…”
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Increasing the cellular PKC inhibitory activity of balanol: A study of ester analogs
Published in Bioorganic & medicinal chemistry letters (21-09-1995)“…As part of an effort to enhance the cellular activity of balanol analogs 2 and 3, we prepared a series of benzophenone ester analogs of varying steric size and…”
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