Search Results - "Locardi, Elsa"
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Carbohydrate-Based Mimetics in Drug Design: Sugar Amino Acids and Carbohydrate Scaffolds
Published in Chemical reviews (01-02-2002)“…Gruner et al review the synthesis of sugar amino acids (SAAs), their incorporation in peptidic or saccharidic structures, and their potential use in medicinal…”
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Design, Synthesis, and NMR Structure of Linear and Cyclic Oligomers Containing Novel Furanoid Sugar Amino Acids
Published in Chemistry : a European journal (04-10-2002)“…Sugar Amino Acids (SAAs) are sugar moieties containing at least one amino and one carboxyl group. The straightforward synthesis of two furanoid SAAs,…”
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TREN (Tris(2-aminoethyl)amine): An Effective Scaffold for the Assembly of Triple Helical Collagen Mimetic Structures
Published in Journal of the American Chemical Society (27-11-2002)“…A new scaffold, TREN-(suc-OH)3 where TREN is tris(2-aminoethyl)amine and suc is the succinic acid spacers, was incorporated to assemble triple helices composed…”
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Synthesis and Structure−Activity Relationship of Mannose-Based Peptidomimetics Selectively Blocking Integrin α4β7 Binding to Mucosal Addressin Cell Adhesion Molecule-1
Published in Journal of medicinal chemistry (18-12-2003)“…As part of our ongoing research in the development of α4β7 integrin antagonists, we are interested in peptidomimetics based on a rigid scaffold to allow the…”
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Thermodynamics of Formation of the Triple Helix from Free Chains and from Template-Constrained Chains of Collagen-like Monodisperse Poly(Gly-Pro-Hyp) Structures
Published in The journal of physical chemistry. A, Molecules, spectroscopy, kinetics, environment, & general theory (09-12-1999)“…Statistical thermodynamic methods, developed for treating the α-helix−coil transition, are applied herein to describe the formation of the triple helix from…”
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Novel Small Molecule Bradykinin B 2 Receptor Antagonists
Published in Journal of medicinal chemistry (23-07-2009)Get full text
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Peptidomimetic C5a receptor antagonists with hydrophobic substitutions at the C-terminus: Increased receptor specificity and in vivo activity
Published in Bioorganic & medicinal chemistry letters (01-10-2006)“…New C5a receptor antagonists characterized by C-terminal amino acids with hydrophobic substitutions are presented. A new class of peptidomimetic C5a receptor…”
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Novel Small Molecule Bradykinin B2 Receptor Antagonists
Published in Journal of medicinal chemistry (23-07-2009)“…Blockade of the bradykinin B2 receptor provides therapeutic benefit in hereditary angioedema (HAE) and potentially in many other diseases. Herein, we describe…”
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Cyclic Homooligomers from Sugar Amino Acids: Synthesis, Conformational Analysis, and Significance
Published in Journal of the American Chemical Society (29-08-2001)“…Sugar amino acids (SAAs) were designed as new building blocks carrying an amino group and a carboxyl group on a carbohydrate scaffold. By exploiting standard…”
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Novel small molecule bradykinin B 1 receptor antagonists. Part 1: Benzamides and semicarbazides
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…Benzamides and semicarbazides are introduced as new classes of bradykinin B 1 receptor antagonists. The best compounds feature excellent pharmacokinetic…”
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Novel small molecule bradykinin B 1 receptor antagonists. Part 2: 5-membered diaminoheterocycles
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…New bradykinin B1 receptor antagonists based on 5-membered diaminoheterocycles with nanomolar activity are presented. Efforts to find new bradykinin B 1…”
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Novel small molecule bradykinin B 1 receptor antagonists. Part 3: Hydroxyurea derivatives
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…Hydroxy urea analogues have been developed as a new class of bradykinin B1 receptor antagonists. Systematic optimization led to the identification of several…”
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Novel small molecule bradykinin B sub(1) receptor antagonists. Part 1: Benzamides and semicarbazides
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…The synthesis and SAR of two series of bradykinin B sub(1) receptor antagonists is described. The benzamide moiety proved to be a suitable replacement for the…”
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Novel small molecule bradykinin B sub(1) receptor antagonists. Part 2: 5-membered diaminoheterocycles
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…Efforts to find new bradykinin B sub(1) receptor antagonists identified 2-aminobenzimidazole as a novel core. Subsequent transformation into five-membered…”
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Novel small molecule bradykinin B sub(1) receptor antagonists. Part 3: Hydroxyurea derivatives
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…Hydroxy urea moieties are introduced as a new class of bradykinin B sub(1) receptor antagonists. First, the SAR of the lead compound was systematically…”
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Synthesis and NMR Studies of Cyclopeptides Containing a Sugar Amino Acid
Published in Organic letters (25-07-2002)“…Cyclopeptides containing Glucuronic acid methylamine (Gum) alternating with Gly, l-Ala, d-Ala, l-Phe, d-Phe, l-Lys, or d-Lys were synthesized by a combination…”
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Novel Small Molecule Bradykinin 82 Receptor Antagonists
Published in Journal of medicinal chemistry (2009)Get full text
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Novel small molecule bradykinin B1 receptor antagonists. Part 2: 5-membered diaminoheterocycles
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…Efforts to find new bradykinin B(1) receptor antagonists identified 2-aminobenzimidazole as a novel core. Subsequent transformation into five-membered…”
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Journal Article -
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Novel small molecule bradykinin B1 receptor antagonists. Part 1: Benzamides and semicarbazides
Published in Bioorganic & medicinal chemistry letters (01-02-2010)“…The synthesis and SAR of two series of bradykinin B(1) receptor antagonists is described. The benzamide moiety proved to be a suitable replacement for the aryl…”
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