Search Results - "Greenlee, William J"

Exploring the inhibition of the soluble lytic transglycosylase Cj0843c of Campylobacter jejuni via targeting different sites with different scaffolds by Kumar, Vijay, Boorman, Jacob, Greenlee, William J., Zeng, Ximin, Lin, Jun, van den Akker, Focco

“…Bacterial lytic transglycosylases (LTs) contribute to peptidoglycan cell wall metabolism and are potential drug targets to potentiate β‐lactam antibiotics to…”
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Potent, selective, and orally active adenosine A2A receptor antagonists : Arylpiperazine derivatives of pyrazolo[4,3-e]-1,2,4-triazolo[1 ,5-c]pyrimidines by NEUSTADT, Bernard R, JINSONG HAO, FOSTER, Carolyn, ARIK, Leyla, LACHOWICZ, Jean, NG, Kwokei, FENG, Kung-I, LINDO, Neil, GREENLEE, William J, STAMFORD, Andrew W, TULSHIAN, Deen, ONGINI, Ennio, HUNTER, John, MONOPOLI, Angela, BERTORELLI, Rosalia

“…Antagonism of the adenosine A2A receptor offers great promise in the treatment of Parkinson's disease. Employing the known…”
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Discovery of a nortropanol derivative as a potent and orally active GPR119 agonist for type 2 diabetes by Xia, Yan, Chackalamannil, Samuel, Greenlee, William J., Jayne, Charles, Neustadt, Bernard, Stamford, Andrew, Vaccaro, Henry, Xu, Xiaoying (Lucy), Baker, Hana, O’Neill, Kim, Woods, Morgan, Hawes, Brian, Kowalski, Tim

“…The lead optimization studies of a series of GPR119 agonists incorporating a nortropanol scaffold led to the identification of compound 36j as a potent and…”
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Discovery of Potent Orally Active Thrombin Receptor (Protease Activated Receptor 1) Antagonists as Novel Antithrombotic Agents by Chackalamannil, Samuel, Xia, Yan, Greenlee, William J, Clasby, Martin, Doller, Darìo, Tsai, Hsingan, Asberom, Theodros, Czarniecki, Michael, Ahn, Ho-Sam, Boykow, George, Foster, Carolyn, Agans-Fantuzzi, Jacqueline, Bryant, Matthew, Lau, Janice, Chintala, Madhu

“…Structurally novel thrombin receptor (protease activated receptor 1, PAR-1) antagonists based on the natural product himbacine are described. The prototypical…”
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Discovery of Orally Efficacious Tetracyclic Metabotropic Glutamate Receptor 1 (mGluR1) Antagonists for the Treatment of Chronic Pain by Wu, Wen-Lian, Burnett, Duane A, Domalski, Martin, Greenlee, William J, Li, Cheng, Bertorelli, Rosalia, Fredduzzi, Silva, Lozza, Gianluca, Veltri, Alessio, Reggiani, Angelo

“…Metabotropic glutamate receptor 1 (mGluR1) plays important roles in the neurotransmission and pathogenesis of several neurological disorders, including chronic…”
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Structure-based design of selective, orally available salt-inducible kinase inhibitors that stimulate bone formation in mice by Sato, Tadatoshi, Andrade, Christian D Castro, Yoon, Sung-Hee, Zhao, Yingshe, Greenlee, William J, Weber, Patricia C, Viswanathan, Usha, Kulp, John, Brooks, Daniel J, Demay, Marie B, Bouxsein, Mary L, Mitlak, Bruce, Lanske, Beate, Wein, Marc N

“…Osteoporosis is a major public health problem. Currently, there are no orally available therapies that increase bone formation. Intermittent parathyroid…”
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Discovery of the 3‑Imino-1,2,4-thiadiazinane 1,1-Dioxide Derivative Verubecestat (MK-8931)–A β‑Site Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor for the Treatment of Alzheimer’s Disease by Scott, Jack D, Li, Sarah W, Brunskill, Andrew P. J, Chen, Xia, Cox, Kathleen, Cumming, Jared N, Forman, Mark, Gilbert, Eric J, Hodgson, Robert A, Hyde, Lynn A, Jiang, Qin, Iserloh, Ulrich, Kazakevich, Irina, Kuvelkar, Reshma, Mei, Hong, Meredith, John, Misiaszek, Jeffrey, Orth, Peter, Rossiter, Lana M, Slater, Meagan, Stone, Julie, Strickland, Corey O, Voigt, Johannes H, Wang, Ganfeng, Wang, Hongwu, Wu, Yusheng, Greenlee, William J, Parker, Eric M, Kennedy, Matthew E, Stamford, Andrew W

“…Verubecestat 3 (MK-8931), a diaryl amide-substituted 3-imino-1,2,4-thiadiazinane 1,1-dioxide derivative, is a high-affinity β-site amyloid precursor protein…”
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Discovery of SCH 900271, a Potent Nicotinic Acid Receptor Agonist for the Treatment of Dyslipidemia by Palani, Anandan, Rao, Ashwin U, Chen, Xiao, Huang, Xianhai, Su, Jing, Tang, Haiqun, Huang, Ying, Qin, Jun, Xiao, Dong, Degrado, Sylvia, Sofolarides, Michael, Zhu, Xiaohong, Liu, Zhidan, McKittrick, Brian, Zhou, Wei, Aslanian, Robert, Greenlee, William J, Senior, Mary, Cheewatrakoolpong, Boonlert, Zhang, Hongtao, Farley, Constance, Cook, John, Kurowski, Stan, Li, Qiu, van Heek, Margaret, Wang, Gangfeng, Hsieh, Yunsheng, Li, Fangbiao, Greenfeder, Scott, Chintala, Madhu

“…Structure-guided optimization of a series of C-5 alkyl substituents led to the discovery of a potent nicotinic acid receptor agonist SCH 900271 (33) with an…”
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Discovery of Orally Active 3-Pyridinyl-tropane As a Potent Nociceptin Receptor Agonist for the Management of Cough by Yang, Shu-Wei, Ho, Ginny, Tulshian, Deen, Greenlee, William J, Anthes, John, Fernandez, Xiomara, McLeod, Robbie L, Hey, John A, Xu, Xiaoying

“…A series of 3-pyridinyl-tropane analogues based on previously reported compound 1 have been synthesized and shown to bind to the nociceptin receptor with high…”
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Discovery of 4-[(Z)-(4-Bromophenyl)- (ethoxyimino)methyl]-1‘-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4‘-methyl-1,4‘- bipiperidine N-Oxide (SCH 351125):  An Orally Bioavailable Human CCR5 Antagonist for the Treatment of HIV Infection by Palani, Anandan, Shapiro, Sherry, Clader, John W, Greenlee, William J, Cox, Kathleen, Strizki, Julie, Endres, Michael, Baroudy, Bahige M

“…Structure−activity studies on piperidino-piperidine 3 led to the discovery of SCH 351125 (1), a selective CCR5 antagonist with potent activity against RANTES…”
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Identification of a Selective SCoR2 Inhibitor That Protects Against Acute Kidney Injury by Zhou, Hua-Lin, Hausladen, Alfred, Anand, Puneet, Rajavel, Malligarjunan, Stomberski, Colin T., Zhang, Rongli, Premont, Richard T., Greenlee, William J., van den Akker, Focco, Stamler, Jonathan S.

“…Acute kidney injury (AKI) is associated with high morbidity and mortality, and no drugs are available clinically. Metabolic reprogramming resulting from the…”
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The discovery of tropane derivatives as nociceptin receptor ligands for the management of cough and anxiety by Ho, Ginny D., Anthes, John, Bercovici, Ana, Caldwell, John P., Cheng, Kuo-Chi, Cui, Xiaoming, Fawzi, Ahmad, Fernandez, Xiomara, Greenlee, William J., Hey, John, Korfmacher, Walter, Lu, Sherry X., McLeod, Robbie L., Ng, Fay, Torhan, April Smith, Tan, Zheng, Tulshian, Deen, Varty, Geoffrey B., Xu, Xiaoying, Zhang, Hongtao

“…The discovery of 1 as a high-affinity ligand for the nociceptin receptor has led to the synthesis of a series of tropane (8-methyl-8-azabicyclo[3.2.1]octane)…”
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Discovery of a Novel, Orally Active Himbacine-Based Thrombin Receptor Antagonist (SCH 530348) with Potent Antiplatelet Activity by Chackalamannil, Samuel, Wang, Yuguang, Greenlee, William J, Hu, Zhiyong, Xia, Yan, Ahn, Ho-Sam, Boykow, George, Hsieh, Yunsheng, Palamanda, Jairam, Agans-Fantuzzi, Jacqueline, Kurowski, Stan, Graziano, Michael, Chintala, Madhu

“…The discovery of an exceptionally potent series of thrombin receptor (PAR-1) antagonists based on the natural product himbacine is described. Optimization of…”
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Epigenetics: Novel Therapeutics Targeting Epigenetics by Conway, Stuart J, Woster, Patrick M, Greenlee, William J, Georg, Gunda, Wang, Shaomeng

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Lead Optimization to Advance Protease-Activated Receptor‑1 Antagonists in Early Discovery by 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

“…Vorapaxar is an approved drug for the reduction of thrombotic cardiovascular events in patients with a history of myocardial infarction or with peripheral…”
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Structure based design of iminohydantoin BACE1 inhibitors: Identification of an orally available, centrally active BACE1 inhibitor by 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.

“…From an initial lead 1, a structure-based design approach led to identification of a novel, high-affinity iminohydantoin BACE1 inhibitor that lowers…”
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Himbacine derived thrombin receptor antagonists: Discovery of a new tricyclic core by Clasby, Martin C., Chackalamannil, Samuel, Czarniecki, Michael, Doller, Darío, Eagen, Keith, Greenlee, William J., Lin, Yan, Tagat, Jayaram R., Tsai, Hsingan, Xia, Yan, Ahn, Ho-Sam, Agans-Fantuzzi, Jacqueline, Boykow, George, Chintala, Madhu, Hsieh, Yunsheng, McPhail, Andrew T.

“…The synthesis and biological activity of a novel series of thrombin receptor antagonists is described. This series of compounds showed excellent in vitro and…”
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Discovery of hydroxy pyrimidine Factor IXa inhibitors by Jayne, Charles L., Andreani, Teresa, Chan, Tin-Yau, Chelliah, Mariappan V., Clasby, Martin C., Dwyer, Michael, Eagen, Keith A., Fried, Steve, Greenlee, William J., Guo, Zhuyan, Hawes, Brian, Hruza, Alan, Ingram, Richard, Keertikar, Kartik M., Neelamkavil, Santhosh, Reichert, Paul, Xia, Yan, Chackalamannil, Samuel

“…[Display omitted] The synthesis and structure activity relationship development of a pyrimidine series of heterocyclic Factor IXa inhibitors is described…”
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SAR of tricyclic sulfones as γ-secretase inhibitors by Xu, Ruo, Cole, David, Asberom, Ted, Bara, Tom, Bennett, Chad, Burnett, Duane A., Clader, John, Domalski, Martin, Greenlee, William J., Hyde, Lynn, Josien, Hubert, Li, HongMei, McBriar, Mark, McKittrick, Brian, Pissarnitski, Dmitri, Qiang, Li, Rajagopalan, Murali, Sasikumar, Thavalakulamgara, Su, Jing, Tang, HaiQun, Wu, Wen-Lian, Zhang, LiLi, Zhao, ZhiQiang

“…Novel tricyclic sulfones as γ-secretase inhibitors have been reported by this laboratory for the treatment of Alzheimer＇s disease Compounds in this series have…”
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Application of Fragment-Based NMR Screening, X-ray Crystallography, Structure-Based Design, and Focused Chemical Library Design to Identify Novel μM Leads for the Development of nM BACE-1 (β-Site APP Cleaving Enzyme 1) Inhibitors by Wang, Yu-Sen, Strickland, Corey, Voigt, Johannes H, Kennedy, Matthew E, Beyer, Brian M, Senior, Mary M, Smith, Elizabeth M, Nechuta, Terry L, Madison, Vincent S, Czarniecki, Michael, McKittrick, Brian A, Stamford, Andrew W, Parker, Eric M, Hunter, John C, Greenlee, William J, Wyss, Daniel F

“…Fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design were used to identify novel inhibitors for…”
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