Search Results - "Sha, Deyou"

Discovery of potent, selective sulfonylfuran urea endothelial lipase inhibitors by Goodman, Krista B., Bury, Michael J., Cheung, Mui, Cichy-Knight, Maria A., Dowdell, Sarah E., Dunn, Allison K., Lee, Dennis, Lieby, Jeffrey A., Moore, Michael L., Scherzer, Daryl A., Sha, Deyou, Suarez, Dominic P., Murphy, Dennis J., Harpel, Mark R., Manas, Eric S., McNulty, Dean E., Annan, Roland S., Matico, Rosalie E., Schwartz, Benjamin K., Trill, John J., Sweitzer, Thomas D., Wang, Da-yuan, Keller, Paul M., Krawiec, John A., Jaye, Michael C.

“…A series of potent, selective sulfonylfuran urea endothelial lipase inhibitors is reported. Mechanism of action studies are also discussed. Endothelial lipase…”
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CCR2 receptor antagonists: Optimization of biaryl sulfonamides to increase activity in whole blood by Wang, Gren Z., Haile, Pamela A., Daniel, Tom, Belot, Benjamin, Viet, Andrew Q., Goodman, Krista B., Sha, Deyou, Dowdell, Sarah E., Varga, Norbert, Hong, Xuan, Chakravorty, Subhas, Webb, Christine, Cornejo, Carla, Olzinski, Alan, Bernard, Roberta, Evans, Christopher, Emmons, Amanda, Briand, Jacques, Chung, Chun-Wa, Quek, Ruben, Lee, Dennis, Gough, Peter J., Sehon, Clark A.

“…A series of biarylsulfonamides was identified as hCCR2 receptor antagonist but suffered from high plasma protein binding resulting in a >100 fold shift in…”
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Synthesis and GABA receptor potency of 3-thiomethyl-4-(hetero)aryl-5-amino-1-phenylpyrazoles by Meegalla, Sanath K., Doller, Dario, Sha, DeYou, Soll, Rich, Wisnewski, Nancy, Silver, Gary M., Dhanoa, Dale

“…GABA receptor potency of 3-thiomethyl-4-(hetero)aryl-5-amino-1-phenylpyrazoles 4 and their synthesis is described. A convenient synthetic route to novel…”
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Development of potent and selective small-molecule human Urotensin-II antagonists by McAtee, John J., Dodson, Jason W., Dowdell, Sarah E., Girard, Gerald R., Goodman, Krista B., Hilfiker, Mark A., Sehon, Clark A., Sha, Deyou, Wang, Gren Z., Wang, Ning, Viet, Andrew Q., Zhang, Daohua, Aiyar, Nambi V., Behm, David J., Carballo, Luz H., Evans, Christopher A., Fries, Harvey E., Nagilla, Rakesh, Roethke, Theresa J., Xu, Xiaoping, Yuan, Catherine C.K., Douglas, Stephen A., Neeb, Michael J.

“…This work describes the development of potent and selective human Urotensin-II antagonists starting from lead compound 1. Several problems relating to oral…”
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Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles by McAtee, John J., Dodson, Jason W., Dowdell, Sarah E., Erhard, Karl, Girard, Gerald R., Goodman, Krista B., Hilfiker, Mark A., Jin, Jian, Sehon, Clark A., Sha, Deyou, Shi, Dongchuan, Wang, Feng, Wang, Gren Z., Wang, Ning, Wang, Yonghui, Viet, Andrew Q., Yuan, Catherine C.K., Zhang, Daohua, Aiyar, Nambi V., Behm, David J., Carballo, Luz H., Evans, Christopher A., Fries, Harvey E., Nagilla, Rakesh, Roethke, Theresa J., Xu, Xiaoping, Douglas, Stephen A., Neeb, Michael J.

“…Redesign of the potent human urotensin-II antagonist 1 with the 2-pyrrolidinylmethyl-3-phenyl-piperidine core to a new chemical series with a substituted…”
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Synthesis and insecticidal activity of fluorinated 2-(2,6-dichloro-4-trifluoromethylphenyl)-2,4,5,6-tetrahydrocyclopentapyrazoles by Meegalla, Sanath K., Doller, Dario, Liu, Ruiping, Sha, DeYou, Lee, YuKai, Soll, Richard M., Wisnewski, Nancy, Silver, Gary M., Dhanoa, Dale

“…Synthesis and insecticidal activities of fused fluorinated tetrahydrocyclopentapyrazoles (generic structure 1) will be presented. A number of fluorinated…”
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Phenoxyphenyl Pyridines as Novel State-Dependent, High-Potency Sodium Channel Inhibitors by Shao, Bin, Victory, Sam, Ilyin, Victor I, Goehring, R. Richard, Sun, Qun, Hogenkamp, Derk, Hodges, Diane D, Islam, Khondaker, Sha, Deyou, Zhang, Chongwu, Nguyen, Phong, Robledo, Silvia, Sakellaropoulos, George, Carter, Richard B

“…In the search for more efficacious drugs to treat neuropathic pain states, a series of phenoxyphenyl pyridines was designed based on…”
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Allium Chemistry:  Synthesis of 1-[Alk(en)ylsulfinyl]propyl Alk(en)yl Disulfides (Cepaenes), Antithrombotic Flavorants from Homogenates of Onion (Allium cepa) by Block, Eric, Gulati, Harsh, Putman, David, Sha, Deyou, You, Niannian, Zhao, Shu-Hai

“…A series of 1-[alk(en)ylsulfinyl]propyl alk(en)yl disulfides (α-sulfinyl disulfides) of structure RS(O)CHEtSSR‘, R, R‘ = Me, (E,Z)-MeCHCH, n-Pr, and…”
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Discovery of Ruzasvir (MK-8408): A Potent, Pan-Genotype HCV NS5A Inhibitor with Optimized Activity against Common Resistance-Associated Polymorphisms by Tong, Ling, Yu, Wensheng, Chen, Lei, Selyutin, Oleg, Dwyer, Michael P, Nair, Anilkumar G, Mazzola, Robert, Kim, Jae-Hun, Sha, Deyou, Yin, Jingjun, Ruck, Rebecca T, Davies, Ian W, Hu, Bin, Zhong, Bin, Hao, Jinglai, Ji, Tao, Zan, Shuai, Liu, Rong, Agrawal, Sony, Xia, Ellen, Curry, Stephanie, McMonagle, Patricia, Bystol, Karin, Lahser, Frederick, Carr, Donna, Rokosz, Laura, Ingravallo, Paul, Chen, Shiying, Feng, Kung-I, Cartwright, Mark, Asante-Appiah, Ernest, Kozlowski, Joseph A

“…We describe the research that led to the discovery of compound 40 (ruzasvir, MK-8408), a pan-genotypic HCV nonstructural protein 5A (NS5A) inhibitor with a…”
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Cerastecin Inhibition of the Lipooligosaccharide Transporter MsbA to Combat Acinetobacter baumannii : From Screening Impurity to In Vivo Efficacy by Skudlarek, Jason W, Cooke, Andrew J, Mitchell, Helen J, Babaoglu, Kerim, Shaw, Anthony W, Tong, Ling, Nomland, Ashley B, Labroli, Marc, Sha, Deyou, Mulhearn, James J, Wu, Chengwei, Li, Sarah W, Beshore, Douglas C, Hughes, Jonathan M E, Jouffroy, Matthieu, Wang, Hao, Balibar, Carl J, Painter, Ronald E, Shen, Pamela, Lange, Henry S, Ishchenko, Andrii, Chen, Yun-Ting, Klein, Daniel J, Tracy, Rodger W, Miller, Randy R, Cabalu, Tamara D, Wu, Zhe, Leithead, Andrew, Scapin, Giovanna, Hruza, Alan W, Dzhekieva, Liudmila, Bukhtiyarova, Marina, Homsher, Michelle F, Xu, Min, Bahnck-Teets, Carolyn, McKenney, David, Buevich, Alexei V, Liu, Jian, Zhang, Li-Kang, Meng, Tao, Kelly, Terri, DiNunzio, Edward, Soisson, Stephen, Cheng, Robert K Y, Hennig, Michael, Raheem, Izzat, Walker, Scott S

“…, a commonly multidrug-resistant Gram-negative bacterium responsible for large numbers of bloodstream and lung infections worldwide, is increasingly difficult…”
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Discovery of Highly Selective and Potent HDAC3 Inhibitors Based on a 2‑Substituted Benzamide Zinc Binding Group by Liu, Jian, Yu, Younong, Kelly, Joseph, Sha, Deyou, Alhassan, Abdul-Basit, Yu, Wensheng, Maletic, Milana M, Duffy, Joseph L, Klein, Daniel J, Holloway, M. Katharine, Carroll, Steve, Howell, Bonnie J, Barnard, Richard J. O, Wolkenberg, Scott, Kozlowski, Joseph A

“…The selectivity of histone deacetylase inhibitors (HDACis) is greatly impacted by the zinc binding groups. In an effort to search for novel zinc binding…”
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Rapid Affinity and Microsomal Stability Ranking of Crude Mixture Libraries of Histone Deacetylase Inhibitors by Tyagarajan, Sriram, Andrews, Christine L., Beshore, Douglas C., Buevich, Alexei V., Curran, Patrick J., Dandliker, Peter, Greshock, Thomas J., Hoar, Jason, Kim, Alex, Karnachi, Prabha, Knemeyer, Ian, Kozlowski, Joseph, Liu, Jian, Maletic, Milana, Myers, Robert, Rada, Vanessa, Sha, Deyou, Sauvagnat, Berengere, Vachal, Petr, Wolkenberg, Scott, Yu, Wensheng, Yu, Younong, Krska, Shane W.

“…The science of drug discovery involves multiparameter optimization of molecular structures through iterative design–make–test cycles. For medicinal chemistry…”
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Substituted tetracyclic indole core derivatives of HCV NS5A inhibitor MK-8742 by Yu, Wensheng, Zhou, Guowei, Coburn, Craig A., Zeng, Qingbei, Tong, Ling, Dwyer, Michael P., Hu, Bin, Zhong, Bin, Hao, Jinglai, Ji, Tao, Zan, Shuai, Chen, Lei, Mazzola, Robert, Kim, Jae-Hun, Sha, Deyou, Selyutin, Oleg, Rosenblum, Stuart B., Lavey, Brian, Nair, Anilkumar G., Heon Kim, Seong, Keertikar, Kerry M., Rokosz, Laura, Agrawal, Sony, Liu, Rong, Xia, Ellen, Zhai, Ying, Curry, Stephanie, McMonagle, Patricia, Ingravallo, Paul, Asante-Appiah, Ernest, Chen, Shiying, Kozlowski, Joseph A.

“…[Display omitted] As part of an ongoing effort in NS5A inhibition at Merck we now describe our efforts for introducing substitution around the tetracyclic…”
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Cerastecins inhibit membrane lipooligosaccharide transport in drug-resistant Acinetobacter baumannii by Wang, Hao, Ishchenko, Andrii, Skudlarek, Jason, Shen, Pamela, Dzhekieva, Liudmila, Painter, Ronald E., Chen, Yun-Ting, Bukhtiyarova, Marina, Leithead, Andrew, Tracy, Rodger, Babaoglu, Kerim, Bahnck-Teets, Carolyn, Buevich, Alexei, Cabalu, Tamara D., Labroli, Marc, Lange, Henry, Lei, Ying, Li, Wei, Liu, Jian, Mann, Paul A., Meng, Tao, Mitchell, Helen J., Mulhearn, James, Scapin, Giovanna, Sha, Deyou, Shaw, Anthony W., Si, Qian, Tong, Ling, Wu, Chengwei, Wu, Zhe, Xiao, Jing Chen, Xu, Min, Zhang, Li-Kang, McKenney, David, Miller, Randy R., Black, Todd A., Cooke, Andrew, Balibar, Carl J., Klein, Daniel J., Raheem, Izzat, Walker, Scott S.

“…Carbapenem-resistant Acinetobacter baumannii infections have limited treatment options. Synthesis, transport and placement of lipopolysaccharide or…”
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Allium Chemistry:  Supercritical Fluid Extraction and LC−APCI−MS of Thiosulfinates and Related Compounds from Homogenates of Garlic, Onion, and Ramp. Identification in Garlic and Ramp and Synthesis of 1-Propanesulfinothioic Acid S-Allyl Ester by Calvey, Elizabeth M, Matusik, Jean E, White, Kevin D, DeOrazio, Russell, Sha, Deyou, Block, Eric

“…Supercritical fluid (SF) extracts of homogenized garlic (Allium sativum L.), ramp (A. tricoccum Ait.), and onion (A. cepa) were characterized with liquid…”
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Efficient syntheses of 2-(2,6-dichloro-4-trifluoromethyl-phenyl)tetrahydrocyclopenta, tetrahydrothiopyrano, hexahydrocycloheptapyrazoles and tetrahydroindazoles by Meegalla, Sanath K., Doller, Dario, Liu, Ruiping, Sha, Deyou, Soll, Richard M., Dhanoa, Dale S.

“…Two methods are described for the regiospecific synthesis of 3,4-fused-cycloalkyl-1-arylpyrazoles; the key step is the reaction between aryl hydrazines and…”
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Allium chemistry : Identification of organosulfur compounds in ramp (Allium tricoccum) homogenates by CALVEY, E. M, WHITE, K. D, MATUSIK, J. E, SHA, D, BLOCK, E

“…Supercritical fluid (SF) extracts of homogenized ramp (Allium tricoccum Ait.) were separated and characterized with liquid chromatography coupled with…”
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Allium chemistry: identification of organosulfur compounds in ramp (allium tricoccum) homogenates fn1 fn1Dedicated with best wishes to Professor G. H. Neil Towers on the occasion of his 75th birthday by Calvey, Elizabeth M., White, Kevin D., Matusik, Jean E., Sha, Deyou, Block, Eric

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