Search Results - "Beshore, Douglas C."

Total Syntheses of (+)-Lyconadin A and (−)-Lyconadin B by Beshore, Douglas C, Smith, Amos B

“…The enantioselective syntheses of (+)-lyconadin A and (−)-lyconadin B are described. Key bond constructions include a strategy-level intramolecular…”
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Conserved allosteric inhibitory site on the respiratory syncytial virus and human metapneumovirus RNA-dependent RNA polymerases by Kleiner, Victoria A., O. Fischmann, Thierry, Howe, John A., Beshore, Douglas C., Eddins, Michael J., Hou, Yan, Mayhood, Todd, Klein, Daniel, Nahas, Debbie D., Lucas, Bob J., Xi, He, Murray, Edward, Ma, Daphne Y., Getty, Krista, Fearns, Rachel

“…Respiratory syncytial virus (RSV) and human metapneumovirus (HMPV) are related RNA viruses responsible for severe respiratory infections and resulting disease…”
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MK-7622: A First-in-Class M1 Positive Allosteric Modulator Development Candidate by Beshore, Douglas C., N. Di Marco, Christina, Chang, Ronald K., Greshock, Thomas J., Ma, Lei, Wittmann, Marion, Seager, Matthew A., Koeplinger, Kenneth A., Thompson, Charles D., Fuerst, Joy, Hartman, George D., Bilodeau, Mark T., Ray, William J., Kuduk, Scott D.

“…Identification of ligands that selectively activate the M1 muscarinic signaling pathway has been sought for decades to treat a range of neurological and…”
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The Lyconadins: Enantioselective Total Syntheses of (+)-Lyconadin A and (−)-Lyconadin B by Beshore, Douglas C, Smith, Amos B

“…A full account of the enantioselective total syntheses of (+)-lyconadin A (1) and (−)-lyconadin B (2) is presented. Central to this venture was recognition and…”
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Design and Synthesis of Novel Isoquinoline-3-nitriles as Orally Bioavailable Kv1.5 Antagonists for the Treatment of Atrial Fibrillation by Trotter, B. Wesley, Nanda, Kausik K, Kett, Nathan R, Regan, Christopher P, Lynch, Joseph J, Stump, Gary L, Kiss, Laszlo, Wang, Jixin, Spencer, Robert H, Kane, Stefanie A, White, Rebecca B, Zhang, Rena, Anderson, Kenneth D, Liverton, Nigel J, McIntyre, Charles J, Beshore, Douglas C, Hartman, George D, Dinsmore, Christopher J

“…Novel 3-cyanoisoquinoline Kv1.5 antagonists have been prepared and evaluated in in vitro and in vivo assays for inhibition of the Kv1.5 potassium channel and…”
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Atrial antifibrillatory effects of structurally distinct IKur blockers 3-[(dimethylamino)methyl]-6-methoxy-2-methyl-4-phenylisoquinolin-1(2H)-one and 2-phenyl-1,1-dipyridin-3-yl-2-pyrrolidin-1-yl-ethanol in dogs with underlying heart failure by Regan, Christopher P, Kiss, Laszlo, Stump, Gary L, McIntyre, Charles J, Beshore, Douglas C, Liverton, Nigel J, Dinsmore, Christopher J, Lynch, Jr, Joseph J

“…Drug discovery efforts have focused recently on atrial-selective targets, including the Kv1.5 channel, which underlies the ultrarapid delayed rectifier…”
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Building a Culture of Medicinal Chemistry Knowledge Sharing by Beshore, Douglas C, Haidle, Andrew M, Arasappan, Ashok, Lim, Yeon-Hee, Raheem, Izzat, Roecker, Anthony J, Shockley, Samantha E, Simov, Vladimir

“…Increasing the efficiency of the drug discovery process is a challenge faced by drug hunters everywhere. One strategy medicinal chemists employ to meet this…”
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Evaluation of a non-nucleoside inhibitor of the RSV RNA-dependent RNA polymerase in translatable animal models by Citron, Michael P., Zang, Xiaowei, Leithead, Andrew, Meng, Shi, Rose II, William A., Murray, Edward, Fontenot, Jane, Bilello, John P., Beshore, Douglas C., Howe, John A.

“…Respiratory Syncytial Virus (RSV) causes severe respiratory infections and concomitant disease resulting in significant morbidity and mortality in infants,…”
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Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel by Beshore, Douglas C., Liverton, Nigel J., McIntyre, Charles J., Claiborne, Christopher F., Libby, Brian, Culberson, J. Christopher, Salata, Joseph J., Regan, Christopher P., Lynch, Joseph J., Kiss, Laszlo, Spencer, Robert H., Kane, Stephanie A., White, Rebecca B., Yeh, Suzie, Hartman, George D., Dinsmore, Christopher J.

“…A series of triarylethanolamine inhibitors of the Kv1.5 potassium channel have been prepared and evaluated for their effects in vitro and in vivo. The…”
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Preparation of Substituted Piperazinones via Tandem Reductive Amination−(N,N‘-Acyl Transfer)−Cyclization by Beshore, Douglas C, Dinsmore, Christopher J

“…A one-pot, tandem reductive amination−transamidation−cyclization reaction was employed to produce substituted piperazin-2-ones in good yields. Various amino…”
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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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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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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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Microbial biotransformation - an important tool for the study of drug metabolism by Salter, Rhys, Beshore, Douglas C., Colletti, Steven L., Evans, Liam, Gong, Yong, Helmy, Roy, Liu, Yong, Maciolek, Cheri M., Martin, Gary, Pajkovic, Natasa, Phipps, Richard, Small, James, Steele, Jonathan, de Vries, Ronald, Williams, Headley, Martin, Iain J.

“…Metabolite identification is an integral part of both preclinical and clinical drug discovery and development. Synthesis of drug metabolites is often required…”
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Informing the Selection of Screening Hit Series with in Silico Absorption, Distribution, Metabolism, Excretion, and Toxicity Profiles by Sanders, John M, Beshore, Douglas C, Culberson, J Christopher, Fells, James I, Imbriglio, Jason E, Gunaydin, Hakan, Haidle, Andrew M, Labroli, Marc, Mattioni, Brian E, Sciammetta, Nunzio, Shipe, William D, Sheridan, Robert P, Suen, Linda M, Verras, Andreas, Walji, Abbas, Joshi, Elizabeth M, Bueters, Tjerk

“…High-throughput screening (HTS) has enabled millions of compounds to be assessed for biological activity, but challenges remain in the prioritization of hit…”
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Redefining the Histone Deacetylase Inhibitor Pharmacophore: High Potency with No Zinc Cofactor Interaction by Beshore, Douglas C., Adam, Gregory C., Barnard, Richard J. O., Burlein, Christine, Gallicchio, Steven N., Holloway, M. Katharine, Krosky, Daniel, Lemaire, Wei, Myers, Robert W., Patel, Sangita, Plotkin, Michael A., Powell, David A., Rada, Vanessa, Cox, Christopher D., Coleman, Paul J., Klein, Daniel J., Wolkenberg, Scott E.

“…A novel series of histone deacetylase (HDAC) inhibitors lacking a zinc-binding moiety has been developed and described herein. HDAC isozyme profiling and…”
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MK-7622: A First-in-Class M 1 Positive Allosteric Modulator Development Candidate by Beshore, Douglas C, N Di Marco, Christina, Chang, Ronald K, Greshock, Thomas J, Ma, Lei, Wittmann, Marion, Seager, Matthew A, Koeplinger, Kenneth A, Thompson, Charles D, Fuerst, Joy, Hartman, George D, Bilodeau, Mark T, Ray, William J, Kuduk, Scott D

“…Identification of ligands that selectively activate the M muscarinic signaling pathway has been sought for decades to treat a range of neurological and…”
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Informing the Selection of Screening Hit Series with in Silico Absorption, Distribution, Metabolism, Excretion, and Toxicity Profiles: Miniperspective by Sanders, John M, Beshore, Douglas C, Culberson, J. Christopher, Fells, James I, Imbriglio, Jason E, Gunaydin, Hakan, Haidle, Andrew M, Labroli, Marc, Mattioni, Brian E, Sciammetta, Nunzio, Shipe, William D, Sheridan, Robert P, Suen, Linda M, Verras, Andreas, Walji, Abbas, Joshi, Elizabeth M, Bueters, Tjerk

“…High-throughput screening (HTS) has enabled millions of compounds to be assessed for biological activity, but challenges remain in the prioritization of hit…”
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2,5‐Disubstituted Pyrazolo[4,3‐c]cinnolin‐3‐ones by Beshore, Douglas C., Johnson, Adam W., DiPardo, Robert M., Pitts, Daniel R., Cofre, Victoria, Kuduk, Scott D.

“…Complementary strategies to 2,5‐disubstituted pyrazolo[4,3‐c]cinnolin‐3‐ones are reported herein, providing late stage substituent introduction at either the…”
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Hydroxy cycloalkyl fused pyridone carboxylic acid M1, positive allosteric modulators by KUDUK, Scott D, DIPARDO, Robert M, BILODEAU, Mark T, BESHORE, Douglas C, RAY, William J, LEI MA, WITTMANN, Marion, SEAGER, Matthew A, KOEPLINGER, Kenneth A, THOMPSON, Charles D, HARTMAN, George D

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