Search Results - "Matasi, Julius J"
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Synthesis and SAR development of novel P2X₇ receptor antagonists for the treatment of pain: Part 2
Published in Bioorganic & medicinal chemistry letters (15-12-2011)“…Novel P2X₇ antagonists were developed using a purine scaffold. These compounds were potent and selective at the P2X₇ receptor in human and rodent as well as…”
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Synthesis and structure–activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands
Published in Bioorganic & medicinal chemistry letters (15-04-2007)“…A series of N-substituted analogs based upon the spiropiperidine core of 1 was synthesized and exhibited high binding affinity to the nociceptin (NOP)…”
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Enantioselective Synthesis of Functionalized Tropanes by Rhodium(II) Carboxylate-Catalyzed Decomposition of Vinyldiazomethanes in the Presence of Pyrroles
Published in Journal of organic chemistry (21-02-1997)“…A series of enantiomerically enriched tropanes was synthesized by the rhodium(II) octanoate-catalyzed reaction of various N-BOC-protected pyrroles with…”
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Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain
Published in Bioorganic & medicinal chemistry letters (01-12-2012)“…High throughput screening identified the pyridothienopyrimidinone 1 as a ligand for the metabotropic glutamate receptor 1 (mGluR1=10nM). Compound 1 has an…”
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The discovery and synthesis of novel adenosine receptor (A 2A) antagonists
Published in Bioorganic & medicinal chemistry letters (01-03-2005)“…The structure–activity relationship investigation using 1 as a template led to the identification of a novel class of compounds as potent and selective…”
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Synthesis and structure–activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: Part 2
Published in Bioorganic & medicinal chemistry letters (15-02-2009)“…A series of N-8 substituted analogs based upon the spiropiperidine core of the original lead compound 1 was synthesized. This lead has been elaborated to…”
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Synthesis and SAR development of novel P2X₇ receptor antagonists for the treatment of pain: Part 1
Published in Bioorganic & medicinal chemistry letters (15-06-2011)“…Structure–activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X₇ receptor antagonists with improved…”
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2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs: highly potent, orally active, adenosine A2A antagonists. Part 1
Published in Bioorganic & medicinal chemistry letters (15-08-2005)“…The structure-activity relationship of this novel class of compounds based on 2-(2-furanyl)-7-phenyl[1,2,4]-triazolo[1,5-c]pyrimidin-5-amine, 1, and its…”
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3H-[1,2,4] -Triazolo[5,1-i]purin -5 -amine derivatives as adenosine A2A antagonists
Published in Bioorganic & medicinal chemistry letters (15-03-2007)“…A novel series of 3-substituted-8-aryl-[1,2,4]-triazolo[5,1-i]purin-5-amine analogs related to Sch 58261 was synthesized in order to identify potent adenosine…”
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2-(2-Furanyl)-7-phenyl[1,2,4]triazolo[1,5-c]pyrimidin-5-amine analogs as adenosine A2A antagonists: the successful reduction of hERG activity. Part 2
Published in Bioorganic & medicinal chemistry letters (15-08-2005)“…The structure-activity relationship (SAR) exploration using 2-(2-furanyl)-7-phenyl[1,2,4]triazolo-[1,5-c]pyrimidin-5-amine (1) as a template led to the…”
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Effect of carbenoid structure on the reactivity of rhodium-stabilized carbenoids
Published in Tetrahedron letters (18-06-1998)“…The outcome of rhodium(II) pivalate catalyzed decomposition of diaozoacetates in the presence of cyclohexane is highly dependent on carbenoid structure…”
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Divergent Pathways in the Intramolecular Reactions between Rhodium-Stabilized Vinylcarbenoids and Pyrroles: Construction of Fused Tropanes and 7-Azabicyclo[4.2.0]octadienes
Published in Journal of organic chemistry (05-04-1996)“…The rhodium(II)-catalyzed intramolecular reaction between vinyldiazomethanes and pyrroles leads to a novel synthesis of fused tropanes. The reaction occurs by…”
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Relative Asymmetric Induction in the Intramolecular Reaction between Alkynes and Cyclopropylcarbene−Chromium Complexes: Stereocontrolled Synthesis of Five-Membered Rings Fused to Oxygen Heterocycles
Published in Journal of organic chemistry (19-02-1999)“…Synthesis of cyclopentenone derivatives fused to oxygen heterocycles by means of the intramolecular coupling of alkynes and cyclopropylcarbene−chromium…”
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Synthesis of 3β-Aryl-8-azabicyclo[3.2.1]octanes with High Binding Affinities and Selectivities for the Serotonin Transporter Site
Published in Journal of medicinal chemistry (21-06-1996)“…A novel entry to tropane analogs of cocaine was developed based on the reaction of rhodium-stabilized vinylcarbenoids with pyrroles. These analogs were tested…”
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Intramolecular coupling of conjugated enynes with cyclopropylcarbene–chromium complexes; a complex reaction pathway
Published in Inorganica Chimica Acta (15-12-1999)“…The intramolecular coupling of conjugated enynes with cyclopropylcarbene complexes has been investigated. The desired products of the reaction,…”
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Synthesis and SAR development of novel P2X 7 receptor antagonists for the treatment of pain: Part 1
Published in Bioorganic & medicinal chemistry letters (15-06-2011)“…Structure–activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X 7 receptor antagonists with improved…”
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Synthesis and SAR development of novel P2X sub(7 receptor antagonists for the treatment of pain: Part 1)
Published in Bioorganic & medicinal chemistry letters (15-06-2011)“…Structure-activity relationship (SAR) efforts around our initial lead compound 1 led to the identification of potent P2X sub(7 receptor antagonists with…”
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