Search Results - "SCHRIMPF, Michael R"

Antiviral Drug Discovery for the Treatment of COVID-19 Infections by Ng, Teresa I, Correia, Ivan, Seagal, Jane, DeGoey, David A, Schrimpf, Michael R, Hardee, David J, Noey, Elizabeth L, Kati, Warren M

“…The coronavirus disease 2019 (COVID-19) pandemic is caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), a recently emerged human…”
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Development of a sensitive high-throughput enzymatic assay capable of measuring sub-nanomolar inhibitors of SARS-CoV2 Mpro by Kovar, Peter, Richardson, Paul L, Korepanova, Alla, Afanador, Gustavo A, Stojkovic, Vladimir, Li, Tao, Schrimpf, Michael R, Ng, Teresa I, Degoey, David A, Gopalakrishnan, Sujatha M, Chen, Jun

“…The SARS-CoV-2 main protease (Mpro) is essential for viral replication because it is responsible for the processing of most of the non-structural proteins…”
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SAR of α7 nicotinic receptor agonists derived from tilorone: Exploration of a novel nicotinic pharmacophore by Schrimpf, Michael R., Sippy, Kevin B., Briggs, Clark A., Anderson, David J., Li, Tao, Ji, Jianguo, Frost, Jennifer M., Surowy, Carol S., Bunnelle, William H., Gopalakrishnan, Murali, Meyer, Michael D.

“…The well-known interferon-inducer tilorone was found to possess potent affinity for the agonist site of the α7 neuronal nicotinic receptor (Ki=56nM). SAR…”
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Structure−Activity Studies and Analgesic Efficacy of N-(3-Pyridinyl)-Bridged Bicyclic Diamines, Exceptionally Potent Agonists at Nicotinic Acetylcholine Receptors by Bunnelle, William H, Daanen, Jerome F, Ryther, Keith B, Schrimpf, Michael R, Dart, Michael J, Gelain, Arianna, Meyer, Michael D, Frost, Jennifer M, Anderson, David J, Buckley, Michael, Curzon, Peter, Cao, Ying-Jun, Puttfarcken, Pamela, Searle, Xenia, Ji, Jianguo, Putman, C. Brent, Surowy, Carol, Toma, Lucio, Barlocco, Daniela

“…A series of exceptionally potent agonists at neuronal nicotinic acetylcholine receptors (nAChRs) has been investigated. Several N-(3-pyridinyl) derivatives of…”
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Metabolism and Disposition of a Novel Selective α 7 Neuronal Acetylcholine Receptor Agonist ABT-126 in Humans: Characterization of the Major Roles for Flavin-Containing Monooxygenases and UDP-Glucuronosyl Transferase 1A4 and 2B10 in Catalysis by Liu, Hong, Stresser, David M, Michmerhuizen, Melissa J, Li, Xiaofeng, Othman, Ahmed A, Reed, Aimee D, Schrimpf, Michael R, Sydor, Jens, Lee, Anthony J

“…Mass balance, metabolism, and excretion of ABT-126, an 7 neuronal acetylcholine receptor agonist, were characterized in healthy male subjects ( = 4) after a…”
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Metabolism and Disposition of a Novel Selective α7 Neuronal Acetylcholine Receptor Agonist ABT-126 in Humans: Characterization of the Major Roles for Flavin-Containing Monooxygenases and UDP-Glucuronosyl Transferase 1A4 and 2B10 in Catalysis by Liu, Hong, Stresser, David M, Michmerhuizen, Melissa J, Li, Xiaofeng, Othman, Ahmed A, Reed, Aimee D, Schrimpf, Michael R, Sydor, Jens, Lee, Anthony J

“…Mass balance, metabolism, and excretion of ABT-126, an α7 neuronal acetylcholine receptor agonist, were characterized in healthy male subjects (n = 4) after a…”
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SAR of alpha 7 nicotinic receptor agonists derived from tilorone: Exploration of a novel nicotinic pharmacophore by Schrimpf, Michael R, Sippy, Kevin B, Briggs, Clark A, Anderson, David J, Li, Tao, Ji, Jianguo, Frost, Jennifer M, Surowy, Carol S, Bunnelle, William H, Gopalakrishnan, Murali, Meyer, Michael D

“…The well-known interferon-inducer tilorone was found to possess potent affinity for the agonist site of the alpha 7 neuronal nicotinic receptor (Ki = 56 nM)…”
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Synthesis and evaluation of new radioligands [11 C]A-833834 and [11 C]A-752274 for positron-emission tomography of α7-nicotinic acetylcholine receptors by Horti, Andrew G, Ravert, Hayden T, Gao, Yongjun, Holt, Daniel P, Bunnelle, William H, Schrimpf, Michael R, Li, Tao, Ji, Jianguo, Valentine, Heather, Scheffel, Ursula, Kuwabara, Hiroto, Wong, Dean F, Dannals, Robert F

“…Abstract Introduction α7-nicotinic acetylcholine receptor (α7-nAChR) is one of the major neuronal nAChR subtypes. α7-nAChR is involved in variety of neuronal…”
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Asymmetric transformation in synthesis: chiral amino acid enolate equivalents by Vedejs, Edwin, Fields, Stephen C, Schrimpf, Michael R

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Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors by SIPPY, Kevin B, ANDERSON, David J, BUNNELLE, William H, HUTCHINS, Charles W, SCHRIMPF, Michael R

“…Several N-pyridin-3-yl spirobicyclic diamines, designed as conformationally restricted analogs of tebanicline (ABT-594), were synthesized as novel ligands for…”
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Design of ligands for the nicotinic acetylcholine receptors: the quest for selectivity by Bunnelle, William H, Dart, Michael J, Schrimpf, Michael R

“…In the last decade, nicotinic acetylcholine receptors (nAChRs) have emerged as important targets for drug discovery. The therapeutic potential of nicotinic…”
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Synthesis and Structure−Activity Relationship Studies of 3,6-Diazabicyclo[3.2.0]heptanes as Novel α4β2 Nicotinic Acetylcholine Receptor Selective Agonists by Ji, Jianguo, Schrimpf, Michael R, Sippy, Kevin B, Bunnelle, William H, Li, Tao, Anderson, David J, Faltynek, Connie, Surowy, Carol S, Dyhring, Tino, Ahring, Philip K, Meyer, Michael D

“…A series of novel, potent neuronal nicotinic acetylcholine receptor (nAChR) ligands derived from 3,6-diazabicyclo[3.2.0]heptane have been synthesized and…”
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Synthesis and SAR of 4-aminocyclopentapyrrolidines as orally active N-type calcium channel inhibitors for inflammatory and neuropathic pain by Beebe, Xenia, Yeung, Clinton M., Darczak, Daria, Shekhar, Shashank, Vortherms, Timothy A., Miller, Loan, Milicic, Ivan, Swensen, Andrew M., Zhu, Chang Z., Banfor, Patricia, Wetter, Jill M., Marsh, Kennan C., Jarvis, Michael F., Scott, Victoria E., Schrimpf, Michael R., Lee, Chih-Hung

“…A novel series of N-type calcium channel inhibitors have been discovered. Optimization of potency and HT-ADME properties provides 4-aminocyclopentapyrrolidines…”
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Syntheses and structure–activity relationship (SAR) studies of 2,5-diazabicyclo[2.2.1]heptanes as novel α7 neuronal nicotinic receptor (NNR) ligands by Li, Tao, Bunnelle, William H., Ryther, Keith B., Anderson, David J., Malysz, John, Helfrich, Rosalind, Grønlien, Jens H., Håkerud, Monika, Peters, Dan, Schrimpf, Michael R., Gopalakrishnan, Murali, Ji, Jianguo

“…A series of biaryl substituted 2,5-diazabicyclo[2.2.1]heptanes were synthesized as potent and selective α7 NNR agonists. Among them, compound 18e shows a α7…”
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Structure–activity relationships of N-substituted ligands for the α7 nicotinic acetylcholine receptor by Mortell, Kathleen H., Schrimpf, Michael R., Bunnelle, William H., Anderson, David J., Gronlien, Jens Halvard, Hagene, Kirsten Thorin, Gopalakrishnan, Murali

“…A series of α7 neuronal nicotinic acetylcholine receptor ligands were designed based on a structural combination of a potent, but non-selective ligand,…”
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An automated electrophysiological assay for differentiating Ca(v)2.2 inhibitors based on state dependence and kinetics by Swensen, Andrew M, Niforatos, Wende, Vortherms, Timothy A, Perner, Richard J, Li, Tao, Schrimpf, Michael R, Scott, Victoria E, Lee, Lance, Jarvis, Michael F, McGaraughty, Steve

“…Ca(V)2.2 (N-type) calcium channels are key regulators of neurotransmission. Evidence from knockout animals and localization studies suggest that Ca(V)2.2…”
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Discovery of fused azetidines as novel selective α4β2 neuronal nicotinic receptor (NNR) agonists by Ji, Jianguo, Bunnelle, William H., Li, Tao, Pace, Jennifer M., Schrimpf, Michael R., Sippy, Kevin B., Anderson, David J., Meyer, Michael D.

“…An efficient synthesis of (1 ,5 )-6-(5-cyano-3-pyridinyl)-3,6-diaza-bicyclo[3.2.0]heptane , a novel potent selective neuronal nicotinic receptor (NNR) agonist,…”
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Synthesis and evaluation of new radioligands [11C]A-833834 and [11C]A-752274 for positron-emission tomography of [alpha]7-nicotinic acetylcholine receptors by Horti, Andrew G, Ravert, Hayden T, Gao, Yongjun, Holt, Daniel P, Bunnelle, William H, Schrimpf, Michael R, Li, Tao, Ji, Jianguo, Valentine, Heather, Scheffel, Ursula, Kuwabara, Hiroto, Wong, Dean F, Dannals, Robert F

“…Introduction: alpha 7-nicotinic acetylcholine receptor ( alpha 7-nAChR) is one of the major neuronal nAChR subtypes. alpha 7-nAChR is involved in variety of…”
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Structure-activity relationships of N-substituted ligands for the a7 nicotinic acetylcholine receptor by Mortell, Kathleen H, Schrimpf, Michael R, Bunnelle, William H, Anderson, David J, Gronlien, Jens Halvard, Hagene, Kirsten Thorin, Gopalakrishnan, Murali

“…A series of a7 neuronal nicotinic acetylcholine receptor ligands were designed based on a structural combination of a potent, but non-selective ligand,…”
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Synthesis and structure-activity relationship studies of 3,6-diazabicyclo[3.2.0]heptanes as novel alpha4beta2 nicotinic acetylcholine receptor selective agonists by Ji, Jianguo, Schrimpf, Michael R, Sippy, Kevin B, Bunnelle, William H, Li, Tao, Anderson, David J, Faltynek, Connie, Surowy, Carol S, Dyhring, Tino, Ahring, Philip K, Meyer, Michael D

“…A series of novel, potent neuronal nicotinic acetylcholine receptor (nAChR) ligands derived from 3,6-diazabicyclo[3.2.0]heptane have been synthesized and…”
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