Search Results - "Matasi, Julius"

The anxiolytic-like effects of the novel, orally active nociceptin opioid receptor agonist 8-[bis(2-methylphenyl)methyl]-3-phenyl-8-azabicyclo[3.2.1]octan-3-ol (SCH 221510) by Varty, Geoffrey B, Lu, Sherry X, Morgan, Cynthia A, Cohen-Williams, Mary E, Hodgson, Robert A, Smith-Torhan, April, Zhang, Hongtao, Fawzi, Ahmad B, Graziano, Michael P, Ho, Ginny D, Matasi, Julius, Tulshian, Deen, Coffin, Vicki L, Carey, Galen J

“…Orphanin FQ/nociceptin (OFQ/N) is the endogenously occurring peptide ligand for the nociceptin opioid receptor (NOP) that produces anxiolytic-like effects in…”
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Synthesis and SAR development of novel P2X₇ receptor antagonists for the treatment of pain: Part 2 by Brumfield, Stephanie, Matasi, Julius J, Tulshian, Deen, Czarniecki, Michael, Greenlee, William, Garlisi, Charles, Qiu, Hongchen, Devito, Kristine, Chen, Shu-Cheng, Sun, Yongliang, Bertorelli, Rosalia, Ansell, Justin, Geiss, William, Le, Van-Duc, Martin, Gregory S, Vellekoop, Samuel A, Haber, James, Allard, Melissa L

“…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 SAR development of novel mGluR1 antagonists for the treatment of chronic pain by Brumfield, Stephanie, Korakas, Peter, Silverman, Lisa S., Tulshian, Deen, Matasi, Julius J., Qiang, Li, Bennett, Chad E., Burnett, Duane A., Greenlee, William J., Knutson, Chad E., Wu, Wen-Lian, Sasikumar, T.K., Domalski, Martin, Bertorelli, Rosalia, Grilli, Mariagrazia, Lozza, Gianluca, Reggiani, Angelo, Li, Cheng

“…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 by Matasi, Julius J., Caldwell, John P., Hao, Jinsong, Neustadt, Bernard, Arik, Leyla, Foster, Carolyn J., Lachowicz, Jean, Tulshian, Deen B.

“…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 by Caldwell, John P., Matasi, Julius J., Zhang, Hongtao, Fawzi, Ahmad, Tulshian, Deen B.

“…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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Synthesis and structure–activity relationships of N-substituted spiropiperidines as nociceptin receptor ligands: Part 2 by Caldwell, John P., Matasi, Julius J., Fernandez, Xiomara, McLeod, Robbie L., Zhang, Hongtao, Fawzi, Ahmad, Tulshian, Deen B.

“…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 by Matasi, Julius J, Brumfield, Stephanie, Tulshian, Deen, Czarnecki, Michael, Greenlee, William, Garlisi, Charles G, Qiu, Hongchen, Devito, Kristine, Chen, Shu-Cheng, Sun, Youngliang, Bertorelli, Rosalia, Geiss, William, Le, Van-Duc, Martin, Gregory S, Vellekoop, Samuel A, Haber, James, Allard, Melissa L

“…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 by Matasi, Julius J, Caldwell, John P, Zhang, Hongtao, Fawzi, Ahmad, Cohen-Williams, Mary E, Varty, Geoffrey B, Tulshian, Deen B

“…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 by SILVERMAN, Lisa S, CALDWELL, John P, ONGINI, Ennio, GREENLEE, William J, KISELGOF, Eugenia, MATASI, Julius J, TULSHIAN, Deen B, ARIK, Leyla, FOSTER, Carolyn, BERTORELLI, Rosalia, MONOPOLI, Angela

“…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 by Matasi, Julius J, Caldwell, John P, Zhang, Hongtao, Fawzi, Ahmad, Higgins, Guy A, Cohen-Williams, Mary E, Varty, Geoffrey B, Tulshian, Deen B

“…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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Enantioselective Synthesis of Functionalized Tropanes by Rhodium(II) Carboxylate-Catalyzed Decomposition of Vinyldiazomethanes in the Presence of Pyrroles by Davies, Huw M. L, Matasi, Julius J, Hodges, L. Mark, Huby, Nicholas J. S, Thornley, Craig, Kong, Norman, Houser, Jeffrey H

“…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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Divergent Pathways in the Intramolecular Reactions between Rhodium-Stabilized Vinylcarbenoids and Pyrroles:  Construction of Fused Tropanes and 7-Azabicyclo[4.2.0]octadienes by Davies, Huw M. L, Matasi, Julius J, Ahmed, Gulzar

“…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 by Yan, Jingbo, Zhu, Jin, Matasi, Julius J, Herndon, James W

“…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 by Davies, Huw M. L, Kuhn, Lisa A, Thornley, Craig, Matasi, Julius J, Sexton, Tammy, Childers, Steven R

“…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 by Matasi, Julius J, Yan, Jingbo, Herndon, James W

“…The intramolecular coupling of conjugated enynes with cyclopropylcarbene complexes has been investigated. The desired products of the reaction,…”
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Effect of carbenoid structure on the reactivity of rhodium-stabilized carbenoids by Davies, Huw M.L., Mark Hodges, L., Matasi, Julius J., Hansen, Tore, Stafford, Douglas G.

“…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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Discovery of pyrrolo-benzo-1,4-diazines as potent Nav1.7 sodium channel blockers by Ho, Ginny D., Tulshian, Deen, Bercovici, Ana, Tan, Zheng, Hanisak, Jennifer, Brumfield, Stephanie, Matasi, Julius, Heap, Charles R., Earley, William G., Courneya, Brandy, Jason Herr, R., Zhou, Xiaoping, Bridal, Terry, Rindgen, Diane, Sorota, Steve, Yang, Shu-Wei

“…A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5…”
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Bioavailable pyrrolo-benzo-1,4-diazines as Nav1.7 sodium channel blockers for the treatment of pain by Yang, Shu-Wei, Ho, Ginny D., Tulshian, Deen, Bercovici, Ana, Tan, Zheng, Hanisak, Jennifer, Brumfield, Stephanie, Matasi, Julius, Sun, Xianfeng, Sakwa, Samuel A., Herr, R. Jason, Zhou, Xiaoping, Bridal, Terry, Urban, Mark, Vivian, Jeffrey, Rindgen, Diane, Sorota, Steve

“…A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5…”
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Bioavailable pyrrolo-benzo-1,4-diazines as Na(v)1.7 sodium channel blockers for the treatment of pain by Yang, Shu-Wei, Ho, Ginny D, Tulshian, Deen, Bercovici, Ana, Tan, Zheng, Hanisak, Jennifer, Brumfield, Stephanie, Matasi, Julius, Sun, Xianfeng, Sakwa, Samuel A, Herr, R Jason, Zhou, Xiaoping, Bridal, Terry, Urban, Mark, Vivian, Jeffrey, Rindgen, Diane, Sorota, Steve

“…A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized to improve the profile of the previous lead compound 1. The syntheses, structure-activity…”
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Initial optimization and series evolution of diaminopyrimidine inhibitors of interleukin-1 receptor associated kinase 4 by Seganish, W. Michael, McElroy, William T., Herr, R. Jason, Brumfield, Stephanie, Greenlee, William J., Harding, James, Komanduri, Venukrishnan, Matasi, Julius, Prakash, Koraboina Chandra, Tulshian, Deen, Yang, Jinhai, Yet, Larry, Devito, Kristine, Fossetta, James, Garlisi, Charles G., Lundell, Daniel, Niu, Xiaoda, Sondey, Christopher

“…[Display omitted] IRAK4 plays a key role in TLR/IL-1 signaling. Previous efforts identified a series of aminopyrimidine IRAK4 inhibitors that possess good…”
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