Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor
Cumming, Jared N., Smith, Elizabeth M., Wang, Lingyan, Misiaszek, Jeffrey, Durkin, James, Pan, Jianping, Iserloh, Ulrich, Wu, Yusheng, Zhu, Zhaoning, Strickland, Corey, Voigt, Johannes, Chen, Xia, Kennedy, Matthew E., Kuvelkar, Reshma, Hyde, Lynn A., Cox, Kathleen, Favreau, Leonard, Czarniecki, Michael F., Greenlee, William J., McKittrick, Brian A., Parker, Eric M., Stamford, Andrew W.
Published in Bioorganic & medicinal chemistry letters (01.04.2012)
Published in Bioorganic & medicinal chemistry letters (01.04.2012)
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Journal Article
Discovery of Cyclic Acylguanidines as Highly Potent and Selective β-Site Amyloid Cleaving Enzyme (BACE) Inhibitors: Part IInhibitor Design and Validation
Zhu, Zhaoning, Sun, Zhong-Yue, Ye, Yuanzan, Voigt, Johannes, Strickland, Corey, Smith, Elizabeth M, Cumming, Jared, Wang, Lingyan, Wong, Jesse, Wang, Yu-Sen, Wyss, Daniel F, Chen, Xia, Kuvelkar, Reshma, Kennedy, Matthew E, Favreau, Leonard, Parker, Eric, McKittrick, Brian A, Stamford, Andrew, Czarniecki, Michael, Greenlee, William, Hunter, John C
Published in Journal of medicinal chemistry (11.02.2010)
Published in Journal of medicinal chemistry (11.02.2010)
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Journal Article
Design and Validation of Bicyclic Iminopyrimidinones As Beta Amyloid Cleaving Enzyme‑1 (BACE1) Inhibitors: Conformational Constraint to Favor a Bioactive Conformation
Mandal, Mihirbaran, Zhu, Zhaoning, Cumming, Jared N, Liu, Xiaoxiang, Strickland, Corey, Mazzola, Robert D, Caldwell, John P, Leach, Prescott, Grzelak, Michael, Hyde, Lynn, Zhang, Qi, Terracina, Giuseppe, Zhang, Lili, Chen, Xia, Kuvelkar, Reshma, Kennedy, Matthew E, Favreau, Leonard, Cox, Kathleen, Orth, Peter, Buevich, Alexei, Voigt, Johannes, Wang, Hongwu, Kazakevich, Irina, McKittrick, Brian A, Greenlee, William, Parker, Eric M, Stamford, Andrew W
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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Journal Article
Iminoheterocycles as γ-secretase modulators
Caldwell, John P., Bennett, Chad E., McCracken, Troy M., Mazzola, Robert D., Bara, Thomas, Buevich, Alexei, Burnett, Duane A., Chu, Inhou, Cohen-Williams, Mary, Josein, Hubert, Hyde, Lynn, Lee, Julie, McKittrick, Brian, Song, Lixin, Terracina, Giuseppe, Voigt, Johannes, Zhang, Lili, Zhu, Zhaoning
Published in Bioorganic & medicinal chemistry letters (15.09.2010)
Published in Bioorganic & medicinal chemistry letters (15.09.2010)
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Journal Article
Discovery of Novel Hydroxamates as Highly Potent Tumor Necrosis Factor-α Converting Enzyme Inhibitors: Part IDiscovery of Two Binding Modes
Zhu, Zhaoning, Mazzola, Robert, Sinning, Lisa, McKittrick, Brian, Niu, Xiaoda, Lundell, Daniel, Sun, Jing, Orth, Peter, Guo, Zhuyan, Madison, Vincent, Ingram, Richard, Beyer, Brian M
Published in Journal of medicinal chemistry (28.02.2008)
Published in Journal of medicinal chemistry (28.02.2008)
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Journal Article
Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators
Qin, Jun, Dhondi, Pawan, Huang, Xianhai, Mandal, Mihirbaran, Zhao, Zhiqiang, Pissarnitski, Dmitri, Zhou, Wei, Aslanian, Robert, Zhu, Zhaoning, Greenlee, William, Clader, John, Zhang, Lili, Cohen-Williams, Mary, Jones, Nicholas, Hyde, Lynn, Palani, Anandan
Published in Bioorganic & medicinal chemistry letters (15.01.2011)
Published in Bioorganic & medicinal chemistry letters (15.01.2011)
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Journal Article
Design and discovery of 1,3-benzodiazepines as novel dopamine antagonists
Zhu, Zhaoning, Sun, Zhong-Yue, Ye, Yuanzan, McKittrick, Brian, Greenlee, William, Czarniecki, Michael, Fawzi, Ahmad, Zhang, Hongtao, Lachowicz, Jean E.
Published in Bioorganic & medicinal chemistry letters (01.09.2009)
Published in Bioorganic & medicinal chemistry letters (01.09.2009)
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Journal Article
Discovery and SAR of cyclic isothioureas as novel NPY Y1 receptor antagonists
SUN, Zhong-Yue, ZHAONING ZHU, YUANZAN YE, MCKITTRICK, Brian, CZARNIECKI, Michael, GREENLEE, William, MULLINS, Deborra, GUZZI, Mario
Published in Bioorganic & medicinal chemistry letters (01.12.2009)
Published in Bioorganic & medicinal chemistry letters (01.12.2009)
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Journal Article
Structure and activity relationships of tartrate-based TACE inhibitors
Li, Dansu, Popovici-Muller, Janeta, Belanger, David B., Caldwell, John, Dai, Chaoyang, David, Maria, Girijavallabhan, Vinay M., Lavey, Brian J., Lee, Joe F., Liu, Zhidan, Mazzola, Rob, Rizvi, Razia, Rosner, Kristin E., Shankar, Bandarpalle, Spitler, Jim, Ting, Pauline C., Vaccaro, Henry, Yu, Wensheng, Zhou, Guowei, Zhu, Zhaoning, Niu, Xiaoda, Sun, Jing, Guo, Zhuyan, Orth, Peter, Chen, Shiying, Kozlowski, Joseph A., Lundell, Daniel J., Madison, Vincent, McKittrick, Brian, Piwinski, John J., Shih, Neng-Yang, Shipps, Gerald W., Siddiqui, M. Arshad, Strickland, Corey O.
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
Published in Bioorganic & medicinal chemistry letters (15.08.2010)
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Journal Article
Generation of Leads for γ‑Secretase Modulation
Mandal, Mihirbaran, Buevich, Alexei, Caldwell, John P, Hyde, Lynn, Huang, Xianhai, Liu, Xiaoxiang, McKittrick, Brian, Mazzola, Robert D, Pissarnitski, Dmitri, Palani, Anandan, Zhang, Lili, Parker, Eric, Xiao, Li, Rindgen, Diane, Zhu, Zhaoning
Published in Journal of medicinal chemistry (13.08.2020)
Published in Journal of medicinal chemistry (13.08.2020)
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Journal Article
Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of UCB7362
Lowe, Martin A., Cardenas, Alvaro, Valentin, Jean-Pierre, Zhu, Zhaoning, Abendroth, Jan, Castro, Jose L., Class, Reiner, Delaunois, Annie, Fleurance, Renaud, Gerets, Helga, Gryshkova, Vitalina, King, Lloyd, Lorimer, Donald D., MacCoss, Malcolm, Rowley, Julian H., Rosseels, Marie-Luce, Royer, Leandro, Taylor, Richard D., Wong, Melanie, Zaccheo, Oliver, Chavan, Vishal P., Ghule, Gokul A., Tapkir, Bapusaheb K., Burrows, Jeremy N., Duffey, Maëlle, Rottmann, Matthias, Wittlin, Sergio, Angulo-Barturen, Iñigo, Jiménez-Díaz, María Belén, Striepen, Josefine, Fairhurst, Kate J., Yeo, Tomas, Fidock, David A., Cowman, Alan F., Favuzza, Paola, Crespo-Fernandez, Benigno, Gamo, Francisco Javier, Goldberg, Daniel E., Soldati-Favre, Dominique, Laleu, Benoît, de Haro, Teresa
Published in Journal of medicinal chemistry (27.10.2022)
Published in Journal of medicinal chemistry (27.10.2022)
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Journal Article
Unprecedented Reversal of Regioselectivity during Methanolysis and an Interception of Curtius Rearrangement
Mandal, Mihirbaran, Buevich, Alexei V., Wang, Hongwu, Brunskill, Andrew, Orth, Peter, Caldwell, John P., Liu, Xiaoxiang, Mazzola, Robert, Cumming, Jared, McKittrick, Brian, Zhu, Zhaoning, Stamford, Andrew
Published in European journal of organic chemistry (24.09.2021)
Published in European journal of organic chemistry (24.09.2021)
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Journal Article
Lead Optimization to Advance Protease-Activated Receptor‑1 Antagonists in Early Discovery
Mandal, Mihirbaran, Madeira, Maria, Amin, Rupesh P, Buevich, Alexei V, Cheng, Alan, Labroli, Marc, Liu, Xiaoxiang, Acton, John, Pio, Barbara, Basso, Andrea, Chobanian, Harry, Dong, Grace, Dropinski, Jamie, Guo, Yan, Guo, Zhuyan, Kurowski, Stan, Korfmacher, Walter, Lee, Sandra, Meng, Dongfang, Ondeyka, Debra, Yang, Zhiqiang, Zhang, Rumin, Wei, Huijun, Wu, Zhicai, Zhang, Fengqi, Wollenberg, Gordon, Biftu, Tesfaye, Greenlee, William J, Chintala, Madhu, Maletic, Milana, Zhu, Zhaoning
Published in Journal of medicinal chemistry (14.04.2022)
Published in Journal of medicinal chemistry (14.04.2022)
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Journal Article
Structure-Based Design of an Iminoheterocyclic β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates
Mandal, Mihirbaran, Wu, Yusheng, Misiaszek, Jeffrey, Li, Guoqing, Buevich, Alexei, Caldwell, John P, Liu, Xiaoxiang, Mazzola, Robert D, Orth, Peter, Strickland, Corey, Voigt, Johannes, Wang, Hongwu, Zhu, Zhaoning, Chen, Xia, Grzelak, Michael, Hyde, Lynn A, Kuvelkar, Reshma, Leach, Prescott T, Terracina, Giuseppe, Zhang, Lili, Zhang, Qi, Michener, Maria S, Smith, Brad, Cox, Kathleen, Grotz, Diane, Favreau, Leonard, Mitra, Kaushik, Kazakevich, Irina, McKittrick, Brian A, Greenlee, William, Kennedy, Matthew E, Parker, Eric M, Cumming, Jared N, Stamford, Andrew W
Published in Journal of medicinal chemistry (14.04.2016)
Published in Journal of medicinal chemistry (14.04.2016)
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Journal Article
Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety
Mandal, Mihirbaran, Mitra, Kaushik, Grotz, Diane, Lin, Xinjie, Palamanda, Jairam, Kumari, Pramila, Buevich, Alexei, Caldwell, John P, Chen, Xia, Cox, Kathleen, Favreau, Leonard, Hyde, Lynn, Kennedy, Matthew E, Kuvelkar, Reshma, Liu, Xiaoxiang, Mazzola, Robert D, Parker, Eric, Rindgen, Diane, Sherer, Edward, Wang, Hongwu, Zhu, Zhaoning, Stamford, Andrew W, Cumming, Jared N
Published in Journal of medicinal chemistry (13.12.2018)
Published in Journal of medicinal chemistry (13.12.2018)
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Journal Article
Cyclic Hydroxyamidines as Amide Isosteres: Discovery of Oxadiazolines and Oxadiazines as Potent and Highly Efficacious γ-Secretase Modulators in Vivo
Sun, Zhong-Yue, Asberom, Theodros, Bara, Thomas, Bennett, Chad, Burnett, Duane, Chu, Inhou, Clader, John, Cohen-Williams, Mary, Cole, David, Czarniecki, Michael, Durkin, James, Gallo, Gioconda, Greenlee, William, Josien, Hubert, Huang, Xianhai, Hyde, Lynn, Jones, Nicholas, Kazakevich, Irina, Li, Hongmei, Liu, Xiaoxiang, Lee, Julie, MacCoss, Malcolm, Mandal, Mihir B, McCracken, Troy, Nomeir, Amin, Mazzola, Robert, Palani, Anandan, Parker, Eric M, Pissarnitski, Dmitri A, Qin, Jun, Song, Lixin, Terracina, Giuseppe, Vicarel, Monica, Voigt, Johannes, Xu, Ruo, Zhang, Lili, Zhang, Qi, Zhao, Zhiqiang, Zhu, Xiaohong, Zhu, Zhaoning
Published in Journal of medicinal chemistry (12.01.2012)
Published in Journal of medicinal chemistry (12.01.2012)
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Journal Article
Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor That Affords Robust CNS Aβ Reduction
Stamford, Andrew W, Scott, Jack D, Li, Sarah W, Babu, Suresh, Tadesse, Dawit, Hunter, Rachael, Wu, Yusheng, Misiaszek, Jeffrey, Cumming, Jared N, Gilbert, Eric J, Huang, Chunli, McKittrick, Brian A, Hong, Liwu, Guo, Tao, Zhu, Zhaoning, Strickland, Corey, Orth, Peter, Voigt, Johannes H, Kennedy, Matthew E, Chen, Xia, Kuvelkar, Reshma, Hodgson, Robert, Hyde, Lynn A, Cox, Kathleen, Favreau, Leonard, Parker, Eric M, Greenlee, William J
Published in ACS medicinal chemistry letters (08.11.2012)
Published in ACS medicinal chemistry letters (08.11.2012)
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Journal Article
Efficient synthesis and reaction pathway studies of novel fused morpholine oxadiazolines for use as gamma secretase modulators
Huang, Xianhai, Pissarnitski, Dmitri, Li, Hongmei, Asberom, Theodros, Josien, Hubert, Zhu, Xiaohong, Vicarel, Monica, Zhao, Zhiqiang, Rajagopalan, Murali, Palani, Anandan, Aslanian, Robert, Zhu, Zhaoning, Greenlee, William, Buevich, Alexei
Published in Tetrahedron letters (21.11.2012)
Published in Tetrahedron letters (21.11.2012)
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