Search Results - "Moore, Keith P"

Synthesis of Complex Druglike Molecules by the Use of Highly Functionalized Bench-Stable Organozinc Reagents by Greshock, Thomas J., Moore, Keith P., McClain, Ray T., Bellomo, Ana, Chung, Cheol K., Dreher, Spencer D., Kutchukian, Peter S., Peng, Zhengwei, Davies, Ian W., Vachal, Petr, Ellwart, Mario, Manolikakes, Sophia M., Knochel, Paul, Nantermet, Philippe G.

“…The reactivity of a representative set of 17 organozinc pivalates with 18 polyfunctional druglike electrophiles (informers) in Negishi cross‐coupling reactions…”
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Discovery and optimization of 2-pyridinone aminal integrase strand transfer inhibitors for the treatment of HIV by Schreier, John D., Embrey, Mark W., Raheem, Izzat T., Barbe, Guillaume, Campeau, Louis-Charles, Dubost, David, McCabe Dunn, Jamie, Grobler, Jay, Hartingh, Timothy J., Hazuda, Daria J., Klein, Daniel, Miller, Michael D., Moore, Keith P., Nguyen, Natalie, Pajkovic, Natasa, Powell, David A., Rada, Vanessa, Sanders, John M., Sisko, John, Steele, Thomas G., Wai, John, Walji, Abbas, Xu, Min, Coleman, Paul J.

“…[Display omitted] HIV integrase strand transfer inhibitors (InSTIs) represent an important class of antiviral therapeutics with proven efficacy and excellent…”
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Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors by Lindsley, Stacey R., Moore, Keith P., Rajapakse, Hemaka A., Selnick, Harold G., Young, Mary Beth, Zhu, Hong, Munshi, Sanjeev, Kuo, Lawrence, McGaughey, Georgia B., Colussi, Dennis, Crouthamel, Ming-Chih, Lai, Ming-Tain, Pietrak, Beth, Price, Eric A., Sankaranarayanan, Sethu, Simon, Adam J., Seabrook, Guy R., Hazuda, Daria J., Pudvah, Nicole T., Hochman, Jerome H., Graham, Samuel L., Vacca, Joseph P., Nantermet, Philippe G.

“…This Letter describes the design and synthesis of tertiary carbinamine macrocyclic inhibitors of the β-secretase (BACE-1) enzyme. These macrocyclic inhibitors,…”
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A Phenotypic Screen Identifies Potent DPP9 Inhibitors Capable of Killing HIV‑1 Infected Cells by Moore, Keith P., Schwaid, Adam G., Tudor, Matthew, Park, Sangho, Beshore, Douglas C., Converso, Antonella, Shipe, William D., Anand, Rajan, Lan, Ping, Moningka, Remond, Rothman, Deborah M., Sun, Wanying, Chi, An, Cornella-Taracido, Ivan, Adam, Gregory C., Bahnck-Teets, Carolyn, Carroll, Steven S., Fay, John F., Goh, Shih Lin, Lusen, Jeffrey, Quan, Shuo, Rodriguez, Silveria, Xu, Min, Andrews, Christine L., Song, Cheng, Filzen, Tracey, Li, Jing, Hollenstein, Kaspar, Klein, Daniel J., Lammens, Alfred, Lim, U-Ming, Fang, Zhiyu, McHale, Carolyn, Li, Yuan, Lu, Meiqing, Diamond, Tracy L., Howell, Bonnie J., Zuck, Paul, Balibar, Carl J.

“…Although current antiretroviral therapy can control HIV-1 replication and prevent disease progression, it is not curative. Identifying mechanisms that can lead…”
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Reducing Limitation in Probe Design: The Development of a Diazirine-Compatible Suzuki–Miyaura Cross Coupling Reaction by Ichiishi, Naoko, Moore, Keith P, Wassermann, Anne Mai, Wolkenberg, Scott E, Krska, Shane W

“…Access to high quality photoaffinity probe molecules is often constrained by synthetic limitations related to diazirine installation. A survey of recently…”
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Discovery of 2‑Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV‑1 Integrase Strand Transfer Inhibitors by Raheem, Izzat T, Walji, Abbas M, Klein, Daniel, Sanders, John M, Powell, David A, Abeywickrema, Pravien, Barbe, Guillaume, Bennet, Amrith, Clas, Sophie−Dorothee, Dubost, David, Embrey, Mark, Grobler, Jay, Hafey, Michael J, Hartingh, Timothy J, Hazuda, Daria J, Miller, Michael D, Moore, Keith P, Pajkovic, Natasa, Patel, Sangita, Rada, Vanessa, Rearden, Paul, Schreier, John D, Sisko, John, Steele, Thomas G, Truchon, Jean-François, Wai, John, Xu, Min, Coleman, Paul J

“…The search for new molecular constructs that resemble the critical two-metal binding pharmacophore required for HIV integrase strand transfer inhibition…”
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First demonstration of cerebrospinal fluid and plasma A beta lowering with oral administration of a beta-site amyloid precursor protein-cleaving enzyme 1 inhibitor in nonhuman primates by Sankaranarayanan, Sethu, Holahan, Marie A, Colussi, Dennis, Crouthamel, Ming-Chih, Devanarayan, Viswanath, Ellis, Joan, Espeseth, Amy, Gates, Adam T, Graham, Samuel L, Gregro, Allison R, Hazuda, Daria, Hochman, Jerome H, Holloway, Katharine, Jin, Lixia, Kahana, Jason, Lai, Ming-tain, Lineberger, Janet, McGaughey, Georgia, Moore, Keith P, Nantermet, Philippe, Pietrak, Beth, Price, Eric A, Rajapakse, Hemaka, Stauffer, Shaun, Steinbeiser, Melissa A, Seabrook, Guy, Selnick, Harold G, Shi, Xiao-Ping, Stanton, Matthew G, Swestock, John, Tugusheva, Katherine, Tyler, Keala X, Vacca, Joseph P, Wong, Jacky, Wu, Guoxin, Xu, Min, Cook, Jacquelynn J, Simon, Adam J

“…beta-Site amyloid precursor protein (APP)-cleaving enzyme (BACE) 1 cleavage of amyloid precursor protein is an essential step in the generation of the…”
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Convenient Preparations of 2,4-Methanopyrrolidine and 5-Carboxy-2,4-methanopyrrolidines by Krow, Grant R, Lin, Guoliang, Herzon, Seth B, Thomas, Andrew M, Moore, Keith P, Huang, Qiuli, Carroll, Patrick J

“…An efficient four-step synthesis of N-BOC-5-syn- and 5-anti-carboxymethanopyrrolidines (12 and 13) and the conversion of 12 to N-BOC-methanopyrrolidine (2) are…”
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Attenuation of scratch‐induced reactive astrogliosis by novel EphA4 kinase inhibitors by Parmentier‐Batteur, Sophie, Finger, Eleftheria N., Krishnan, Raghu, Rajapakse, Hemaka A., Sanders, John M., Kandpal, Geeta, Zhu, Hong, Moore, Keith P., Regan, Christopher P., Sharma, Sujata, Hess, J. Fred, Williams, Theresa M., Reynolds, Ian J., Vacca, Joseph P., Mark, Robert J., Nantermet, Philippe G.

“…J. Neurochem. (2011) 118, 1016–1031. The EphA4 receptor and its ephrin ligands are involved in astrocytic gliosis following CNS injury. Therefore, a strategy…”
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Correction to Discovery of 2‑Pyridinone Aminals: A Prodrug Strategy to Advance a Second Generation of HIV‑1 Integrase Strand Transfer Inhibitors by Raheem, Izzat T, Walji, Abbas M, Klein, Daniel, Sanders, John M, Powell, David A, Abeywickrema, Pravien, Barbe, Guillaume, Bennet, Amrith, Childers, Karla, Christensen, Melodie, Clas, Sophie−Dorothee, Dubost, David, Embrey, Mark, Grobler, Jay, Hafey, Michael J, Hartingh, Timothy J, Hazuda, Daria J, Kuethe, Jeffrey T, McCabe Dunn, Jamie, Miller, Michael D, Moore, Keith P, Nolting, Andrew, Pajkovic, Natasa, Patel, Sangita, Peng, Zuihui, Rada, Vanessa, Rearden, Paul, Schreier, John D, Sisko, John, Steele, Thomas G, Truchon, Jean-François, Wai, John, Xu, Min, Coleman, Paul J

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Synthesis of Complex Druglike Molecules by the Use of Highly Functionalized Bench-Stable Organozinc Reagents by Greshock, Thomas J., Moore, Keith P., McClain, Ray T., Bellomo, Ana, Chung, Cheol K., Dreher, Spencer D., Kutchukian, Peter S., Peng, Zhengwei, Davies, Ian W., Vachal, Petr, Ellwart, Mario, Manolikakes, Sophia M., Knochel, Paul, Nantermet, Philippe G.

“…The reactivity of a representative set of 17 organozinc pivalates with 18 polyfunctional druglike electrophiles (informers) in Negishi cross‐coupling reactions…”
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Strategies towards Improving the Pharmacokinetic Profile of ε-Substituted Lysinol-Derived HIV Protease Inhibitors by Rajapakse, Hemaka A., Walji, Abbas M., Moore, Keith P., Zhu, Hong, Mitra, Aurpon W., Gregro, Alison R., Tinney, Elizabeth, Burlein, Christine, Touch, Sinoeun, Paton, Brenda L., Carroll, Steven S., DiStefano, Daniel J., Lai, Ming-Tain, Grobler, Jay A., Sanchez, Rosa I., Williams, Theresa M., Vacca, Joseph P., Nantermet, Philippe G.

“…Compounds that are all HAART: Subsequent to accessing the S2 subpocket of HIV protease from the novel lysinol series of HIV protease inhibitors, we now report…”
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Evolution of Tertiary Carbinamine BACE‐1 Inhibitors: Aβ Reduction in Rhesus CSF upon Oral Dosing by Nantermet, Philippe G., Rajapakse, Hemaka A., Stanton, Mathew G., Stauffer, Shaun R., Barrow, James C., Gregro, Allison R., Moore, Keith P., Steinbeiser, Melissa A., Swestock, John, Selnick, Harold G., Graham, Samuel L., McGaughey, Georgia B., Colussi, Dennis, Lai, Ming‐Tain, Sankaranarayanan, Sethu, Simon, Adam J., Munshi, Sanjeev, Cook, Jacquelynn J., Holahan, Marie A., Michener, Maria S., Vacca, Joseph P.

“…Turning up the BACE: Incorporation of an isonicotinic core into oxadiazolyl tertiary carbinamine‐based inhibitors of BACE‐1 has led to the identification of an…”
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Novel Selectfluor and Deoxo-Fluor-Mediated Rearrangements. New 5(6)-Methyl and Phenyl Methanopyrrolidine Alcohols and Fluorides by Krow, Grant R, Lin, Guoliang, Moore, Keith P, Thomas, Andrew M, DeBrosse, Charles, Ross, Charles W, Ramjit, Harri G

“…Stereoselective syntheses of novel 5,6-difunctionalized-2-azabicyclo[2.1.1]hexanes containing 5-anti-fluoro or hydroxyl in one methano bridge and a variety of…”
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Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors by Moore, Keith P., Zhu, Hong, Rajapakse, Hemaka A., McGaughey, Georgia B., Colussi, Dennis, Price, Eric A., Sankaranarayanan, Sethu, Simon, Adam J., Pudvah, Nicole T., Hochman, Jerome H., Allison, Timothy, Munshi, Sanjeev K., Graham, Samuel L., Vacca, Joseph P., Nantermet, Philippe G.

“…This letter describes replacements for the P3 amide moiety present in previously reported tertiary carbinamine macrolactones. Although P-gp efflux issues…”
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Evolution of tertiary carbinamine BACE-1 inhibitors: Abeta reduction in rhesus CSF upon oral dosing by Nantermet, Philippe G, Rajapakse, Hemaka A, Stanton, Mathew G, Stauffer, Shaun R, Barrow, James C, Gregro, Allison R, Moore, Keith P, Steinbeiser, Melissa A, Swestock, John, Selnick, Harold G, Graham, Samuel L, McGaughey, Georgia B, Colussi, Dennis, Lai, Ming-Tain, Sankaranarayanan, Sethu, Simon, Adam J, Munshi, Sanjeev, Cook, Jacquelynn J, Holahan, Marie A, Michener, Maria S, Vacca, Joseph P

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