Search Results - "Zhu, Yeheng"

Structural and Thermal Characterization of Halogenated Azidopyridines: Under-Reported Synthons for Medicinal Chemistry by Mandler, Michael D, Degnan, Andrew P, Zhang, Shasha, Aulakh, Darpandeep, Georges, Ketleine, Sandhu, Bhupinder, Sarjeant, Amy, Zhu, Yeheng, Traeger, Sarah C, Cheng, Peter T, Ellsworth, Bruce A, Regueiro-Ren, Alicia

“…Owing to their participation in Click reactions, bifunctional azides are valuable intermediates in the preparation of medicines and biochemical tool compounds…”
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Potent and selective biphenyl azole inhibitors of adipocyte fatty acid binding protein (aFABP) by Sulsky, Richard, Magnin, David R., Huang, Yanting, Simpkins, Ligaya, Taunk, Prakash, Patel, Manorama, Zhu, Yeheng, Stouch, Terry R., Bassolino-Klimas, Donna, Parker, Rex, Harrity, Thomas, Stoffel, Robert, Taylor, David S., Lavoie, Thomas B., Kish, Kevin, Jacobson, Bruce L., Sheriff, Steven, Adam, Leonard P., Ewing, William R., Robl, Jeffrey A.

“…X-ray crystal structure of an FABP inhibitor bound to the active site of aFABP. Herein we report the first disclosure of biphenyl azoles that are nanomolar…”
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Characterization of a novel and selective CB1 antagonist as a radioligand for receptor occupancy studies by Yang, Yifan, Miller, Keith J., Zhu, Yeheng, Hong, Yang, Tian, Yuan, Murugesan, Natesan, Gu, Zhengxiang, O’Tanyi, Eva, Keim, William J., Rohrbach, Kenneth W., Johnghar, Susan, Behnia, Kamelia, Pelleymounter, Mary Ann, Carlson, Kenneth E., Ewing, William R.

“…Ex vivo autoradiography of rat brain sagittal sections following drug treatment utilizing [ 3H]BMS-725519. Obesity remains a significant public health issue…”
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Discovery of pyrazine carboxamide CB1 antagonists: The introduction of a hydroxyl group improves the pharmaceutical properties and in vivo efficacy of the series by Ellsworth, Bruce A., Wang, Ying, Zhu, Yeheng, Pendri, Annapurna, Gerritz, Samuel W., Sun, Chongqing, Carlson, Kenneth E., Kang, Liya, Baska, Rose A., Yang, Yifan, Huang, Qi, Burford, Neil T., Cullen, Mary Jane, Johnghar, Susan, Behnia, Kamelia, Pelleymounter, Mary Ann, Washburn, William N., Ewing, William R.

“…Structure–activity relationships for a series of pyrazine carboxamide CB1 antagonists are reported. Pharmaceutical properties of the series are improved via…”
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Reduction of Site-Specific CYP3A-Mediated Metabolism for Dual Angiotensin and Endothelin Receptor Antagonists in Various in Vitro Systems and in Cynomolgus Monkeys by Zhang, Hongjian, Zhang, Donglu, Li, Wenying, Yao, Ming, D'Arienzo, Celia, Li, Yi-Xin, Ewing, William R, Gu, Zhengxiang, Zhu, Yeheng, Murugesan, Natesan, Shyu, Wen-Chyi, Humphreys, W Griffith

“…2-{Butyryl-[2′-(4,5-dimethyl-isoxazol-3-ylsulfamoyl)-biphenyl-4-ylmethyl]-amino}- N -isopropyl-3-methyl-butyramide (BMS-1) is a potent dual acting…”
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Synthesis of triazolopyridines and triazolopyrimidines using a modified Mitsunobu reaction by Roberge, Jacques Y., Yu, Guixue, Mikkilineni, Amarendra, Wu, Ximao, Zhu, Yeheng, Lawrence, R. Michael, Ewing, William R.

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N-3-Substituted Imidazoquinazolinones:  Potent and Selective PDE5 Inhibitors as Potential Agents for Treatment of Erectile Dysfunction by Rotella, David P, Sun, Zhong, Zhu, Yeheng, Krupinski, John, Pongrac, Ronald, Seliger, Laurie, Normandin, Diane, Macor, John E

“…Phosphodiesterase type 5 (PDE5) inhibitors with improved PDE isozyme selectivity relative to sildenafil may result in agents for the treatment of male erectile…”
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Optimization of Substituted N-3-Benzylimidazoquinazolinone Sulfonamides as Potent and Selective PDE5 Inhibitors by Rotella, David P, Sun, Zhong, Zhu, Yeheng, Krupinski, John, Pongrac, Ronald, Seliger, Laurie, Normandin, Diane, Macor, John E

“…A previous report from these laboratories identified the N-3-benzylimidazoquinazolinone nucleus as a more selective PDE5 inhibitor template compared to the…”
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Overcoming Limitations in Decarboxylative Arylation via Ag–Ni Electrocatalysis by Palkowitz, Maximilian D., Laudadio, Gabriele, Kolb, Simon, Choi, Jin, Oderinde, Martins S., Ewing, Tamara El-Hayek, Bolduc, Philippe N., Chen, TeYu, Zhang, Hao, Cheng, Peter T. W., Zhang, Benxiang, Mandler, Michael D., Blasczak, Vanna D., Richter, Jeremy M., Collins, Michael R., Schioldager, Ryan L., Bravo, Martin, Dhar, T. G. Murali, Vokits, Benjamin, Zhu, Yeheng, Echeverria, Pierre-Georges, Poss, Michael A., Shaw, Scott A., Clementson, Sebastian, Petersen, Nadia Nasser, Mykhailiuk, Pavel K., Baran, Phil S.

“…A useful protocol for achieving decarboxylative cross-coupling (DCC) of redox-active esters (RAE, isolated or generated in situ) and halo­(hetero)­arenes is…”
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Discovery of Milvexian, a High-Affinity, Orally Bioavailable Inhibitor of Factor XIa in Clinical Studies for Antithrombotic Therapy by Dilger, Andrew K, Pabbisetty, Kumar B, Corte, James R, De Lucca, Indawati, Fang, Tianan, Yang, Wu, Pinto, Donald J. P, Wang, Yufeng, Zhu, Yeheng, Mathur, Arvind, Li, Jianqing, Hou, Xiaoping, Smith, Daniel, Sun, Dawn, Zhang, Huiping, Krishnananthan, Subramaniam, Wu, Dauh-Rurng, Myers, Joseph E, Sheriff, Steven, Rossi, Karen A, Chacko, Silvi, Zheng, Joanna J, Galella, Michael A, Ziemba, Theresa, Dierks, Elizabeth A, Bozarth, Jeffrey M, Wu, Yiming, Crain, Earl, Wong, Pancras C, Luettgen, Joseph M, Wexler, Ruth R, Ewing, William R

“…Factor XIa (FXIa) is an enzyme in the coagulation cascade thought to amplify thrombin generation but has a limited role in hemostasis. From preclinical models…”
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Amination of Nitro-Substituted Heteroarenes by Nucleophilic Substitution of Hydrogen by Mandler, Michael D., Suss, Nina, Ramirez, Antonio, Farley, Christopher A., Aulakh, Darpandeep, Zhu, Yeheng, Traeger, Sarah C., Sarjeant, Amy, Davies, Merrill L., Ellsworth, Bruce A., Regueiro-Ren, Alicia

“…An open-air method for the transition metal-free direct amination of nitro­(hetero)­arenes by anilines is disclosed. In this methodology, an aromatic C–H bond…”
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Azatricyclic Inverse Agonists of RORγt That Demonstrate Efficacy in Models of Rheumatoid Arthritis and Psoriasis by Liu, Qingjie, Xiao, Hai-Yun, Batt, Douglas G, Xiao, Zili, Zhu, Yeheng, Yang, Michael G, Li, Ning, Yip, Shiuhang, Li, Peng, Sun, Dawn, Wu, Dauh-Rurng, Ruzanov, Max, Sack, John S, Weigelt, Carolyn A, Wang, Jinhong, Li, Sha, Shuster, David J, Xie, Jenny H, Song, Yunling, Sherry, Tara, Obermeier, Mary T, Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Chacko, Silvi, Khandelwal, Purnima, Dudhgaonkar, Shailesh, Rudra, Anjuman, Nagar, Jignesh, Murali, Venkata, Govindarajan, Arun, Denton, Rex, Zhao, Qihong, Meanwell, Nicholas A, Borzilleri, Robert, Dhar, T. G. Murali

“…Structure–activity relationship studies directed toward the replacement of the fused phenyl ring of the lead hexahydrobenzoindole RORγt inverse agonist series…”
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HURDNet: Heterogeneous UNet Structure With Range-Null Space Decomposition for Hyperspectral Image Reconstruction by Zhu, Yeheng, Wu, Zhijian, Li, Jun, Xu, Jianhua

“…Hyperspectral image (HSI) reconstruction aims to recover a 3D HSI from its degraded 2D measurement. Despite achieving significant progress, most methods do not…”
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Reductions in log P Improved Protein Binding and Clearance Predictions Enabling the Prospective Design of Cannabinoid Receptor (CB1) Antagonists with Desired Pharmacokinetic Properties by Ellsworth, Bruce A, Sher, Philip M, Wu, Ximao, Wu, Gang, Sulsky, Richard B, Gu, Zhengxiang, Murugesan, Natesan, Zhu, Yeheng, Yu, Guixue, Sitkoff, Doree F, Carlson, Kenneth E, Kang, Liya, Yang, Yifan, Lee, Ning, Baska, Rose A, Keim, William J, Cullen, Mary Jane, Azzara, Anthony V, Zuvich, Eva, Thomas, Michael A, Rohrbach, Kenneth W, Devenny, James J, Godonis, Helen E, Harvey, Susan J, Murphy, Brian J, Everlof, Gerry G, Stetsko, Paul I, Gudmundsson, Olafur, Johnghar, Susan, Ranasinghe, Asoka, Behnia, Kamelia, Pelleymounter, Mary Ann, Ewing, William R

“…Several strategies have been employed to reduce the long in vivo half-life of our lead CB1 antagonist, triazolopyridazinone 3, to differentiate the…”
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