Search Results - "Tsou, Nancy N."

Isolation, Structure, and Absolute Stereochemistry of Platensimycin, A Broad Spectrum Antibiotic Discovered Using an Antisense Differential Sensitivity Strategy by Singh, Sheo B, Jayasuriya, Hiranthi, Ondeyka, John G, Herath, Kithsiri B, Zhang, Chaowei, Zink, Deborah L, Tsou, Nancy N, Ball, Richard G, Basilio, Angela, Genilloud, Olga, Diez, Maria Teresa, Vicente, Francisca, Pelaez, Fernando, Young, Katherine, Wang, Jun

“…Fatty acids are essential for survival of bacteria and are synthesized by a series of enzymes including the elongation enzymes, β-ketoacyl acyl carrier protein…”
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A New Planar Chiral Bisphosphine Ligand for Asymmetric Catalysis:  Highly Enantioselective Hydrogenations under Mild Conditions by Pye, Philip J, Rossen, Kai, Reamer, Robert A, Tsou, Nancy N, Volante, R. P, Reider, Paul J

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Efficient Synthesis of NK1 Receptor Antagonist Aprepitant Using a Crystallization-Induced Diastereoselective Transformation by Brands, Karel M. J, Payack, Joseph F, Rosen, Jonathan D, Nelson, Todd D, Candelario, Alexander, Huffman, Mark A, Zhao, Matthew M, Li, Jing, Craig, Bridgette, Song, Zhiguo J, Tschaen, David M, Hansen, Karl, Devine, Paul N, Pye, Philip J, Rossen, Kai, Dormer, Peter G, Reamer, Robert A, Welch, Christopher J, Mathre, David J, Tsou, Nancy N, McNamara, James M, Reider, Paul J

“…An efficient stereoselective synthesis of the orally active NK1 receptor antagonist Aprepitant is described. A direct condensation of N-benzyl ethanolamine…”
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Structural Optimization Affording 2-(R)-(1-(R)-3,5-Bis(trifluoromethyl)phenylethoxy)-3-(S)-(4-fluoro)phenyl-4- (3-oxo-1,2,4-triazol-5-yl)methylmorpholine, a Potent, Orally Active, Long-Acting Morpholine Acetal Human NK-1 Receptor Antagonist by Hale, Jeffrey J, Mills, Sander G, MacCoss, Malcolm, Finke, Paul E, Cascieri, Margaret A, Sadowski, Sharon, Ber, Elzbieta, Chicchi, Gary G, Kurtz, Marc, Metzger, Joseph, Eiermann, George, Tsou, Nancy N, Tattersall, F. David, Rupniak, Nadia M. J, Williams, Angela R, Rycroft, Wayne, Hargreaves, Richard, MacIntyre, D. Euan

“…Structural modifications requiring novel synthetic chemistry were made to the morpholine acetal human neurokinin-1 (hNK-1) receptor antagonist 4, and this…”
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Design, Synthesis, and In Vivo Efficacy of Glycine Transporter-1 (GlyT1) Inhibitors Derived from a Series of [4-Phenyl-1-(propylsulfonyl)piperidin-4-yl]methyl Benzamides by Lindsley, Craig W., Zhao, Zhijian, Leister, William H., O'Brien, Julie, Lemaire, Wei, Williams Jr, David L., Chen, Tsing-Bau, Chang, Raymond S. L., Burno, Maryann, Jacobson, Marlene A., Sur, Cyrille, Kinney, Gene G., Pettibone, Douglas J., Tiller, Philip R., Smith, Sheri, Tsou, Nancy N., Duggan, Mark E., Conn, P. Jeffrey, Hartman, George D.

“…An iterative analogue library synthesis approach rapidly delivered (S)‐13 h, a potent, reversible, and selective GlyT1 inhibitor. (S)‐13 h selectively…”
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Crystallization-Induced Diastereoselection: Asymmetric Synthesis of Substance P Inhibitors by Pye, Philip J., Rossen, Kai, Weissman, Steven A., Maliakal, Ashok, Reamer, Robert A., Ball, Richard, Tsou, Nancy N., Volante, R. P., Reider, Paul J.

“…A novel three‐component condensation followed by a crystallization‐induced asymmetric transformation is used to build this key substance P inhibitor…”
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Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives by Meurer, Laura C., Finke, Paul E., Owens, Karen A., Tsou, Nancy N., Ball, Richard G., Mills, Sander G., MacCoss, Malcolm, Sadowski, Sharon, Cascieri, Margaret A., Tsao, Kwei-Lan, Chicchi, Gary G., Egger, Linda A., Luell, Silvi, Metzger, Joseph M., MacIntyre, D. Euan, Rupniak, Nadia M.J., Williams, Angela R., Hargreaves, Richard J.

“…The optimization of a cyclopentane-based hNK1 antagonist scaffold will be discussed in the context of enhanced water-solubility, sub-nanomolar hNK1 binding…”
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The discovery of potent, selective, and orally bioavailable hNK1 antagonists derived from pyrrolidine by LIN, Peter, LEHUA CHANG, KURTZ, Marc M, TSAO, Kwei-Lan C, WHEELDON, Alan, CARLSON, Emma J, ENG, Waisi, BURNS, H. Donald, HARGREAVES, Richard J, MILLS, Sander G, DEVITA, Robert J, YOUNG, Jonathan R, EID, Ronsar, XINCHUN TONG, SONG ZHENG, BALL, Richard G, TSOU, Nancy N, CHICCHI, Gary G

“…SAR studies on amides, ureas, and vinylogous amides derived from pyrrolidine led to the discovery of several potent hNK(1) antagonists. One particular…”
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Nodulisporic Acid A, a Novel and Potent Insecticide from a Nodulisporium Sp. Isolation, Structure Determination, and Chemical Transformations by Ondeyka, John G, Helms, Gregory L, Hensens, Otto D, Goetz, Michael A, Zink, Deborah L, Tsipouras, Athanasios, Shoop, Wesley L, Slayton, Lyndia, Dombrowski, Anne W, Polishook, Jon D, Ostlind, Dan A, Tsou, Nancy N, Ball, Richard G, Singh, Sheo B

“…The potent insecticidal agent nodulisporic acid A (1a), representative of a new class of indole terpenes, was isolated from fermentations of a Nodulisporium…”
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Diastereoselective Friedel−Crafts Alkylation of Indoles with Chiral α-Phenyl Benzylic Cations. Asymmetric Synthesis of Anti-1,1,2-Triarylalkanes by Chung, John Y. L, Mancheno, Danny, Dormer, Peter G, Variankaval, Narayan, Ball, Richard G, Tsou, Nancy N

“…The reactions of chiral benzyl carbocations bearing α-phenyl substituents with N-sulfonylated indoles afford 1,1,2-triarylalkanes with anti-selectivities. This…”
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Aryl sulfones: a new class of γ-secretase inhibitors by Teall, Martin, Oakley, Paul, Harrison, Timothy, Shaw, Duncan, Kay, Euan, Elliott, Jason, Gerhard, Ute, Castro, José L., Shearman, Mark, Ball, Richard G., Tsou, Nancy N.

“…[Display omitted] The development of a novel series of 4-aryl, 4-phenylsulfonyl cyclohexananone-derived γ-secretase inhibitors for the potential treatment of…”
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Conformational Analysis and Receptor Docking of N-[(1S,2S)-3-(4-Chlorophenyl)-2-(3-cyanophenyl)-1-methylpropyl]-2-methyl-2-{[5-(trifluoromethyl)pyridin-2-yl]oxy}propanamide (Taranabant, MK-0364), a Novel, Acyclic Cannabinoid-1 Receptor Inverse Agonist by Lin, Linus S, Ha, Sookhee, Ball, Richard G, Tsou, Nancy N, Castonguay, Laurie A, Doss, George A, Fong, Tung M, Shen, Chun-Pyn, Xiao, Jing Chen, Goulet, Mark T, Hagmann, William K

“…X-ray crystallographic, NMR spectroscopic, and computational studies of taranabant afforded similar low-energy conformers with a significant degree of rigidity…”
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3-Heteroaryl-2-pyridones:  Benzodiazepine Site Ligands with Functional Selectivity for α2/α3-Subtypes of Human GABAA Receptor-Ion Channels by Collins, Ian, Moyes, Christopher, Davey, William B, Rowley, Michael, Bromidge, Frances A, Quirk, Kathleen, Atack, John R, McKernan, Ruth M, Thompson, Sally-Ann, Wafford, Keith, Dawson, Gerard R, Pike, Andrew, Sohal, Bindi, Tsou, Nancy N, Ball, Richard G, Castro, José L

“…A novel series of 3-heteroaryl-5,6-bis(aryl)-1-methyl-2-pyridones were developed with high affinity for the benzodiazepine (BZ) binding site of human…”
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Asymmetric Synthesis of α,α-Difluoro-β-amino Acid Derivatives from Enantiomerically Pure N-tert-Butylsulfinimines by Staas, Donnette D, Savage, Kelly L, Homnick, Carl F, Tsou, Nancy N, Ball, Richard G

“…Addition of the Reformatsky reagent derived from ethyl bromodifluoroacetate to alkyl- and aryl-substituted N-tert-butylsulfinimines furnishes…”
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Isolation, Structure, and Absolute Stereochemistry of Platensimycin, A Broad Spectrum Antibiotic Discovered Using an Antisense Differential Sensitivity Strategy [J. Am. Chem. Soc. 2006, 128, 11916−11920] by Singh, Sheo B, Jayasuriya, Hiranthi, Ondeyka, John G, Herath, Kithsiri B, Zhang, Chaowei, Zink, Deborah L, Tsou, Nancy N, Ball, Richard G, Basilio, Angela, Genilloud, Olga, Diez, Maria Teresa, Vicente, Francisca, Pelaez, Fernando, Young, Katherine, Wang, Jun

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Design of a novel pyrrolidine scaffold utilized in the discovery of potent and selective human β₃ adrenergic receptor agonists by Morriello, Gregori J, Wendt, Harvey R, Bansal, Alka, Salvo, Jerry Di, Feighner, Scott, He, Jiafang, Hurley, Amanda L, Hreniuk, Donna L, Salituro, Gino M, Reddy, Marat Vijay, Galloway, Sheila M, McGettigan, Katherine K, Laws, George, McKnight, Crystal, Doss, George A, Tsou, Nancy N, Black, Regina M, Morris, Judy, Ball, Richard G, Sanfiz, Anthony T, Streckfuss, Eric, Struthers, Mary, Edmondson, Scott D

“…A novel class of human β₃-adrenergic receptor agonists was designed in effort to improve selectivity and metabolic stability versus previous disclosed β₃-AR…”
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Discovery of a spiroindane based compound as a potent, selective, orally bioavailable melanocortin subtype-4 receptor agonist by He, Shuwen, Ye, Zhixiong, Dobbelaar, Peter H., Sebhat, Iyassu K., Guo, Liangqin, Liu, Jian, Jian, Tianying, Lai, Yingjie, Franklin, Christopher L., Bakshi, Raman K., Dellureficio, James P., Hong, Qingmei, Tsou, Nancy N., Ball, Richard G., Cashen, Doreen E., Martin, William J., Weinberg, David H., MacNeil, Tanya, Tang, Rui, Tamvakopoulos, Constantin, Peng, Qianping, Miller, Randy R., Stearns, Ralph A., Chen, Howard Y., Chen, Airu S., Strack, Alison M., Fong, Tung M., MacIntyre, D. Euan, Wyvratt, Matthew J., Nargund, Ravi P.

“…We report the design, synthesis and properties of spiroindane based compound 1, a potent, selective, orally bioavailable, non-peptide melanocortin subtype-4…”
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A series of 5-(5,6)-dihydrouracil substituted 8-hydroxy-[1,6]naphthyridine-7-carboxylic acid 4-fluorobenzylamide inhibitors of HIV-1 integrase and viral replication in cells by Embrey, Mark W., Wai, John S., Funk, Timothy W., Homnick, Carl F., Perlow, Debbie S., Young, Steven D., Vacca, Joseph P., Hazuda, Daria J., Felock, Peter J., Stillmock, Kara A., Witmer, Marc V., Moyer, Gregory, Schleif, William A., Gabryelski, Lori J., Jin, Lixia, Chen, I-Wu, Ellis, Joan D., Wong, Bradley K., Lin, Jiunn H., Leonard, Yvonne M., Tsou, Nancy N., Zhuang, Linghang

“…Introduction of a 5,6-dihydrouracil functionality in the 5-position of N-(4-fluorobenzyl)-8-hydroxy-[1,6]naphthyridine-7-carboxamide 1 led to a series of…”
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Discovery of potent, selective, and orally bioavailable 3H-spiro[isobenzofuran-1,4'-piperidine] based melanocortin subtype-4 receptor agonists by LIANGQIN GUO, ZHIXIONG YE, TSOU, Nancy N, BALL, Richard G, WEINBERG, David H, MACNEIL, Tanya, RUI TANG, TAMVAKOPOULOS, Constantin, QIANPING PENG, CHEN, Howard Y, CHEN, Airu S, MARTIN, William J, JIAN LIU, EUAN MACINTYRE, D, STRACK, Alison M, FONG, Tung M, WYVRATT, Matthew J, NARGUND, Ravi P, SHUWEN HE, BAKSHI, Raman K, SEBHAT, Iyassu K, DOBBELAAR, Peter H, QINGMEI HONG, TIANYING JIAN, DELLUREFICIO, James P

“…Design, synthesis, and SAR of a series of 3H-spiro[isobenzofuran-1,4'-piperidine] based compounds as potent, selective and orally bioavailable melanocortin…”
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1-Sulfonyl-4-acylpiperazines as Selective Cannabinoid-1 Receptor (CB1R) Inverse Agonists for the Treatment of Obesity by Vachal, Petr, Fletcher, Joan M, Fong, Tung M, Huang, Cathy C. R.-R, Lao, Julie, Xiao, Jing C, Shen, Chun-Pyn, Strack, Alison M, Shearman, Lauren, Stribling, Sloan, Chen, Richard Z, Frassetto, Andrea, Tong, Xinchun, Wang, Junying, Ball, Richard G, Tsou, Nancy N, Hickey, Gerard J, Thompson, Donald F, Faidley, Terry D, Nicolich, Susan, Achanfuo-Yeboah, Joana, Hora, Donald F, Hale, Jeffrey J, Hagmann, William K

“…A novel series of 1-sulfonyl-4-acylpiperazines as selective cannabinoid-1 receptor (CB1R) inverse agonists was discovered through high throughput screening…”
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