Publications by authors named "Beth Fleck"

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The importance of target binding kinetics for measuring target binding affinity in drug discovery: a case study from a CRF receptor antagonist program.
Sam R J Hoare, Beth A Fleck, John P Williams, Dimitri E Grigoriadis

Drug Discov Today· January 2020

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Discovery of novel oxazepine and diazepine carboxamides as two new classes of heat shock protein 90 inhibitors.
Timothy Neubert, Mehdi Numa, Justin Ernst, Jeremy Clemens, Paul Krenitsky, Beth Fleck

Bioorg Med Chem Lett· March 2015

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Identification of novel HSP90α/β isoform selective inhibitors using structure-based drug design. demonstration of potential utility in treating CNS disorders such as Huntington's disease.
Justin T Ernst, Timothy Neubert, Michael Liu, Samuel Sperry, Harmon Zuccola, Beth Fleck

J Med Chem· April 2014

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Binding kinetics redefine the antagonist pharmacology of the corticotropin-releasing factor type 1 receptor.
Beth A Fleck, Sam R J Hoare, Rebecca R Pick, Margaret J Bradbury, Dimitri E Grigoriadis

J Pharmacol Exp Ther· May 2012

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Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with improved pharmaceutical characteristics.
Joseph Pontillo, Dongpei Wu, Brett Ching, Sarah Hudson, Marc J Genicot, Beth A Fleck

Bioorg Med Chem Lett· December 2008

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Characterization of thien-2-yl 1S,2R-milnacipran analogues as potent norepinephrine/serotonin transporter inhibitors for the treatment of neuropathic pain.
Brian Dyck, Junko Tamiya, Florence Jovic, Rebecca R Pick, Margaret J Bradbury, Beth A Fleck

J Med Chem· November 2008

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Structure-activity relationship studies on a series of piperazinebenzylalcohols and their ketone and amine analogs as melanocortin-4 receptor ligands.
Dragan Marinkovic, Fabio C Tucci, Joe A Tran, Beth A Fleck, Jenny Wen

Bioorg Med Chem Lett· September 2008

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Synthesis and structure-activity relationships of selective norepinephrine reuptake inhibitors (sNRI) with a heterocyclic ring constraint.
Sarah Hudson, Mehrak Kiankarimi, Wendy Eccles, Yalda S Mostofi, Marc J Genicot, Beth A Fleck

Bioorg Med Chem Lett· August 2008

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Structure-activity relationships of chiral selective norepinephrine reuptake inhibitors (sNRI) with increased oxidative stability.
Sarah Hudson, Mehrak Kiankarimi, Wendy Eccles, Wesley Dwight, Yalda S Mostofi, Beth A Fleck

Bioorg Med Chem Lett· August 2008

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Studies on the structure-activity relationship of bicifadine analogs as monoamine transporter inhibitors.
Mingzhu Zhang, Florence Jovic, Troy Vickers, Brian Dyck, Junko Tamiya, Beth A Fleck

Bioorg Med Chem Lett· July 2008

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Discovery of a potent, selective, and less flexible selective norepinephrine reuptake inhibitor (sNRI).
Dongpei Wu, Joseph Pontillo, Brett Ching, Sarah Hudson, Yinghong Gao, Beth A Fleck

Bioorg Med Chem Lett· July 2008

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Identification of 1S,2R-milnacipran analogs as potent norepinephrine and serotonin transporter inhibitors.
Junko Tamiya, Brian Dyck, Mingzhu Zhang, Kasey Phan, Beth A Fleck

Bioorg Med Chem Lett· June 2008

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Studies on a series of milnacipran analogs containing a heteroaromatic group as potent norepinephrine and serotonin transporter inhibitors.
Troy Vickers, Brian Dyck, Junko Tamiya, Mingzhu Zhang, Florence Jovic, Beth A Fleck

Bioorg Med Chem Lett· June 2008

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Allosteric ligands for the corticotropin releasing factor type 1 receptor modulate conformational states involved in receptor activation.
Sam R J Hoare, Beth A Fleck, Raymond S Gross, Paul D Crowe, John P Williams

Mol Pharmacol· May 2008

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Pharmacological and pharmacokinetic characterization of 2-piperazine-alpha-isopropyl benzylamine derivatives as melanocortin-4 receptor antagonists.
Chen Chen, Fabio C Tucci, Wanlong Jiang, Joe A Tran, Beth A Fleck

Bioorg Med Chem· May 2008

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Design and synthesis of 3-arylpyrrolidine-2-carboxamide derivatives as melanocortin-4 receptor ligands.
Joe A Tran, Fabio C Tucci, Melissa Arellano, Wanlong Jiang, Caroline W Chen, Beth A Fleck

Bioorg Med Chem Lett· March 2008

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Syntheses of tetrahydrothiophenes and tetrahydrofurans and studies of their derivatives as melanocortin-4 receptor ligands.
Joe A Tran, Caroline W Chen, Fabio C Tucci, Wanlong Jiang, Beth A Fleck

Bioorg Med Chem Lett· February 2008

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Studies on the SAR and pharmacophore of milnacipran derivatives as monoamine transporter inhibitors.
Chen Chen, Brian Dyck, Beth A Fleck, Alan C Foster, Jonathan Grey

Bioorg Med Chem Lett· February 2008

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Identification and characterization of pyrrolidine diastereoisomers as potent functional agonists and antagonists of the human melanocortin-4 receptor.
Chen Chen, Wanlong Jiang, Joe A Tran, Fabio C Tucci, Beth A Fleck

Bioorg Med Chem Lett· January 2008

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Studies on the structure-activity relationship of the basic amine of phenylpiperazines as melanocortin-4 receptor antagonists.
Joe A Tran, Melissa Arellano, Beth A Fleck, Joseph Pontillo, Dragan Marinkovic

Med Chem· January 2008

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Synthesis and characterization of pyrrolidine derivatives as potent agonists of the human melanocortin-4 receptor.
Wanlong Jiang, Joe A Tran, Fabio C Tucci, Beth A Fleck, Sam R Hoare

Bioorg Med Chem Lett· December 2007

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Synthesis and characterization of trans-4-(4-chlorophenyl)pyrrolidine-3-carboxamides of piperazinecyclohexanes as ligands for the melanocortin-4 receptor.
Caroline W Chen, Joe A Tran, Beth A Fleck, Fabio C Tucci, Wanlong Jiang

Bioorg Med Chem Lett· December 2007

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Design, synthesis, in vitro, and in vivo characterization of phenylpiperazines and pyridinylpiperazines as potent and selective antagonists of the melanocortin-4 receptor.
Joe A Tran, Wanlong Jiang, Fabio C Tucci, Beth A Fleck, Jenny Wen

J Med Chem· December 2007

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Discovery of 1-[2-[(1S)-(3-dimethylaminopropionyl)amino-2-methylpropyl]-4-methylphenyl]-4-[(2R)-methyl-3-(4-chlorophenyl)-propionyl]piperazine as an orally active antagonist of the melanocortin-4 receptor for the potential treatment of cachexia.
Chen Chen, Wanlong Jiang, Fabio Tucci, Joe A Tran, Beth A Fleck

J Med Chem· November 2007

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Pyrrolidinones as potent functional antagonists of the human melanocortin-4 receptor.
Wanlong Jiang, Fabio C Tucci, Joe A Tran, Beth A Fleck, Jenny Wen

Bioorg Med Chem Lett· October 2007

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