Search Results - "DOUNAY, Amy B"

Challenges and Opportunities in the Discovery of New Therapeutics Targeting the Kynurenine Pathway by Dounay, Amy B, Tuttle, Jamison B, Verhoest, Patrick R

“…The kynurenine pathway is responsible for the metabolism of more than 95% of dietary tryptophan (TRP) and produces numerous bioactive metabolites. Recent…”
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The Asymmetric Intramolecular Heck Reaction in Natural Product Total Synthesis by Dounay, Amy B, Overman, Larry E

“…The Pd(0)-catalyzed vinylation of aryl halides was first reported over 30 years ago in independent studies by Mizoroki and Heck. The transformation that has…”
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Total Synthesis of the Strychnos Alkaloid (+)-Minfiensine: Tandem Enantioselective Intramolecular Heck−Iminium Ion Cyclization by Dounay, Amy B, Humphreys, Philip G, Overman, Larry E, Wrobleski, Aaron D

“…A 1,2,3,4-tetrahydro-9a,4a-(iminoethano)-9H-carbazole (4) is a central structural feature of the Strychnos alkaloid minfiensine (1) and akuammiline alkaloids…”
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Sequential Catalytic Asymmetric Heck−Iminium Ion Cyclization:  Enantioselective Total Synthesis of the Strychnos Alkaloid Minfiensine by Dounay, Amy B, Overman, Larry E, Wrobleski, Aaron D

“…A catalytic asymmetric method for the chemical synthesis of alkaloids containing the 1,2,3,4-tetrahydro-9a,4a-(iminoethano)-9H-carbazole (1) moiety is reported…”
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Catalytic Asymmetric Synthesis of Quaternary Carbons Bearing Two Aryl Substituents. Enantioselective Synthesis of 3-Alkyl-3-Aryl Oxindoles by Catalytic Asymmetric Intramolecular Heck Reactions by Dounay, Amy B, Hatanaka, Keiko, Kodanko, Jeremy J, Oestreich, Martin, Overman, Larry E, Pfeifer, Lance A, Weiss, Matthew M

“…A practical sequence involving three consecutive palladium(0)-catalyzed reactions has been developed for synthesizing 3-alkyl-3-aryloxindoles in high…”
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Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia by Dounay, Amy B, Anderson, Marie, Bechle, Bruce M, Campbell, Brian M, Claffey, Michelle M, Evdokimov, Artem, Evrard, Edelweiss, Fonseca, Kari R, Gan, Xinmin, Ghosh, Somraj, Hayward, Matthew M, Horner, Weldon, Kim, Ji-Young, McAllister, Laura A, Pandit, Jayvardhan, Paradis, Vanessa, Parikh, Vinod D, Reese, Matthew R, Rong, SuoBao, Salafia, Michelle A, Schuyten, Katherine, Strick, Christine A, Tuttle, Jamison B, Valentine, James, Wang, Hong, Zawadzke, Laura E, Verhoest, Patrick R

“…Kynurenine aminotransferase (KAT) II has been identified as a potential new target for the treatment of cognitive impairment associated with schizophrenia and…”
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Discovery and pharmacological characterization of aryl piperazine and piperidine ethers as dual acting norepinephrine reuptake inhibitors and 5-HT1A partial agonists by GRAY, David L, WENJIAN XU, CAMPBELL, Brian M, DOUNAY, Amy B, BARTA, Nancy, BOROSKI, Susan, DENNY, Lynne, EVANS, Lori, STRATMAN, Nancy, PROBERT, Al

“…Compounds that are both norepinephrine reuptake inhibitors (NRI) and 5-HT1(A) partial agonists may have the potential to treat neuropsychiatric disorders…”
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Globally Distributed Drug Discovery of New Antibiotics: Design and Combinatorial Synthesis of Amino Acid Derivatives in the Organic Chemistry Laboratory by Dounay, Amy B, O’Donnell, Martin J, Samaritoni, J. Geno, Popiolek, Lukasz, Schirch, Douglas, Biernasiuk, Anna, Malm, Anna, Lamb, Isaac W, Mudrack, Kristen, Rivera, Daniel G, Ojeda, Gerardo M, Scott, William L

“…An experiment for the synthesis of N-acyl derivatives of natural amino acids has been developed as part of the Distributed Drug Discovery (D3) program…”
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Multi-Institution Research and Education Collaboration Identifies New Antimicrobial Compounds by Fuller, Amelia A, Dounay, Amy B, Schirch, Douglas, Rivera, Daniel G, Hansford, Karl A, Elliott, Alysha G, Zuegg, Johannes, Cooper, Matthew A, Blaskovich, Mark A. T, Hitchens, Jacob R, Burris-Hiday, Sarah, Tenorio, Kristiana, Mendez, Yanira, Samaritoni, J. Geno, O’Donnell, Martin J, Scott, William L

“…New antibiotics are urgently needed to address increasing rates of multidrug resistant infections. Seventy-six diversely functionalized compounds, comprising…”
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Novel 1,2-dihydroquinazolin-2-ones: Design, synthesis, and biological evaluation against Trypanosoma brucei by Pham, ThanhTruc, Walden, Madeline, Butler, Christopher, Diaz-Gonzalez, Rosario, Pérez-Moreno, Guiomar, Ceballos-Pérez, Gloria, Gomez-Pérez, Veronica, García-Hernández, Raquel, Zecca, Henry, Krakoff, Emma, Kopec, Brian, Ichire, Ogar, Mackenzie, Caden, Pitot, Marika, Ruiz, Luis Miguel, Gamarro, Francisco, González-Pacanowska, Dolores, Navarro, Miguel, Dounay, Amy B.

“…[Display omitted] In 2014, a published report of the high-throughput screen of>42,000 kinase inhibitors from GlaxoSmithKline against T. brucei identified 797…”
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PF-04859989 as a template for structure-based drug design: Identification of new pyrazole series of irreversible KAT II inhibitors with improved lipophilic efficiency by Dounay, Amy B., Anderson, Marie, Bechle, Bruce M., Evrard, Edelweiss, Gan, Xinmin, Kim, Ji-Young, McAllister, Laura A., Pandit, Jayvardhan, Rong, SuoBao, Salafia, Michelle A., Tuttle, Jamison B., Zawadzke, Laura E., Verhoest, Patrick R.

“…The structure-based design, synthesis, and biological evaluation of a new pyrazole series of irreversible KAT II inhibitors are described herein. The…”
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Expedient Access to the Okadaic Acid Architecture:  A Novel Synthesis of the C1−C27 Domain by Dounay, Amy B, Urbanek, Rebecca A, Frydrychowski, Valerie A, Forsyth, Craig J

“…A newly designed synthetic entry to the C1−C27 domain of okadaic acid has been developed. This incorporates substantial improvements in the preparations of the…”
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A General Strategy for the Synthesis of Cyclic N-Aryl Hydroxamic Acids via Partial Nitro Group Reduction by McAllister, Laura A, Bechle, Bruce M, Dounay, Amy B, Evrard, Edelweiss, Gan, Xinmin, Ghosh, Somraj, Kim, Ji-Young, Parikh, Vinod D, Tuttle, Jamison B, Verhoest, Patrick R

“…We describe a generalized approach to stereocontrolled synthesis of substituted cyclic hydroxamic acids (3-amino-1-hydroxy-3,4-dihydroquinolinones) by…”
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Importance of the C28–C38 hydrophobic domain of okadaic acid for potent inhibition of protein serine-threonine phosphatases 1 and 2A by Frydrychowski, Valerie A., Urbanek, Rebecca A., Dounay, Amy B., Forsyth, Craig J.

“…Okadaic acid is a potent inhibitor of select serine/threonine protein phosphatases. The importance of the C28–C38 hydrophobic domain of okadaic acid for…”
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Synthesis of ortho-substituted nitroaromatics via improved Negishi coupling conditions by Tuttle, Jamison B., Azzarelli, Joseph M., Bechle, Bruce M., Dounay, Amy B., Evrard, Edelweiss, Gan, Xinmin, Ghosh, Somraj, Henderson, Jaclyn, Kim, Ji-Young, Parikh, Vinod D., Verhoest, Patrick R.

“…We describe modified Negishi coupling conditions that allow improved access to ortho-nitrophenylalanine derivatives. These useful amino acid intermediates can…”
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Design, synthesis, and pharmacological evaluation of azetedine and pyrrolidine derivatives as dual norepinephrine reuptake inhibitors and 5-HT₁A partial agonists by Pettersson, Martin, Campbell, Brian M, Dounay, Amy B, Gray, David L, Xie, Longfei, O’Donnell, Christopher J, Stratman, Nancy C, Zoski, Kim, Drummond, Elena, Bora, Gary, Probert, Al, Whisman, Tammy

“…Compounds with combined norepinephrine reuptake inhibitor (NRI) and serotonin 1A (5-HT₁A) partial agonist pharmacology may offer a new therapeutic approach for…”
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Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions by Tuttle, Jamison B, Anderson, Marie, Bechle, Bruce M, Campbell, Brian M, Chang, Cheng, Dounay, Amy B, Evrard, Edelweiss, Fonseca, Kari R, Gan, Xinmin, Ghosh, Somraj, Horner, Weldon, James, Larry C, Kim, Ji-Young, McAllister, Laura A, Pandit, Jayvardhan, Parikh, Vinod D, Rago, Brian J, Salafia, Michelle A, Strick, Christine A, Zawadzke, Laura E, Verhoest, Patrick R

“…A series of aryl hydroxamates recently have been disclosed as irreversible inhibitors of kynurenine amino transferase II (KAT II), an enzyme that may play a…”
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Design, synthesis, and pharmacological evaluation of phenoxy pyridyl derivatives as dual norepinephrine reuptake inhibitors and 5-HT1A partial agonists by DOUNAY, Amy B, BARTA, Nancy S, MAITI, Samarendra N, ORTWINE, Daniel F, PROBERT, Al, STRATMAN, Nancy C, SUBEDI, Rajendra, WHISMAN, Tammy, WENJIAN XU, ZOSKI, Kim, CAMPBELL, Brian M, COLEMAN, Corey, COLLANTES, Elizabeth M, DENNY, Lynne, DUTTA, Satavisha, GRAY, David L, DONGFENG HOU, IYER, Rathna

“…Preclinical studies suggest that compounds with dual norepinephrine reuptake inhibitor (NRI) and 5-HT(1A) partial agonist properties may provide an important…”
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Synthesis and pharmacological evaluation of aminopyrimidine series of 5-HT1A partial agonists by Dounay, Amy B, Barta, Nancy S, Bikker, Jack A, Borosky, Susan A, Campbell, Brian M, Crawford, Terry, Denny, Lynne, Evans, Lori M, Gray, David L, Lee, Pil, Lenoir, Edward A, Xu, Wenjian

“…Aminopyrimidine 2 (4-(1-(2-(1H-indol-3-yl)ethyl)piperidin-3-yl)-N-cyclopropylpyrimidin-2-amine) emerged from a high throughput screen as a novel 5-HT(1A)…”
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Synthetic Studies toward the C5−C20 Domain of the Azaspiracids by Dounay, Amy B, Forsyth, Craig J

“…An approach toward the C5−C20 THF-fused trioxadispiroketal portion of the azaspiracids is reported. The highly substituted azaspiracid D ring (C16−C19) was…”
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