Search Results - "Deininger, David"

Novel inhibitors of cholesterol degradation in Mycobacterium tuberculosis reveal how the bacterium's metabolism is constrained by the intracellular environment by VanderVen, Brian C, Fahey, Ruth J, Lee, Wonsik, Liu, Yancheng, Abramovitch, Robert B, Memmott, Christine, Crowe, Adam M, Eltis, Lindsay D, Perola, Emanuele, Deininger, David D, Wang, Tiansheng, Locher, Christopher P, Russell, David G

“…Mycobacterium tuberculosis (Mtb) relies on a specialized set of metabolic pathways to support growth in macrophages. By conducting an extensive, unbiased…”
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Novel Dual-Targeting Benzimidazole Urea Inhibitors of DNA Gyrase and Topoisomerase IV Possessing Potent Antibacterial Activity: Intelligent Design and Evolution through the Judicious Use of Structure-Guided Design and Stucture−Activity Relationships by Charifson, Paul S, Grillot, Anne-Laure, Grossman, Trudy H, Parsons, Jonathan D, Badia, Michael, Bellon, Steve, Deininger, David D, Drumm, Joseph E, Gross, Christian H, LeTiran, Arnaud, Liao, Yusheng, Mani, Nagraj, Nicolau, David P, Perola, Emanuele, Ronkin, Steven, Shannon, Dean, Swenson, Lora L, Tang, Qing, Tessier, Pamela R, Tian, Ski-Kai, Trudeau, Martin, Wang, Tiansheng, Wei, Yunyi, Zhang, Hong, Stamos, Dean

“…The discovery of new antibacterial agents with novel mechanisms of action is necessary to overcome the problem of bacterial resistance that affects all…”
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Discovery of Potent, Selective Triazolothiadiazole-Containing c‑Met Inhibitors by Tang, Qing, Aronov, Alex M, Deininger, David D, Giroux, Simon, Lauffer, David J, Li, Pan, Liang, Jianglin, McGinty, Kira, Ronkin, Steven, Swett, Rebecca, Waal, Nathan, Boucher, Diane, Ford, Pamella J, Moody, Cameron S

“…Herein, we report a novel series of highly potent and selective triazolothiadiazole c-Met inhibitors. Starting with molecule 5, we have applied structure-based…”
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2-N-Arylthiazole inhibitors of Mycobacterium tuberculosis by Clark, Michael P., Wang, Tiansheng, Perola, Emanuele, Deininger, David D., Zuccola, Harmon J., Jones, Steven M., Gao, Hong, VanderVen, Brian C., Russell, David G., Shoen, Carolyn M., Cynamon, Michael H., Thomson, John A., Locher, Christopher P.

“…[Display omitted] To develop agents for the treatment of infections caused by Mycobacterium tuberculosis, a novel phenotypic screen was undertaken that…”
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Successful application of serum shift prediction models to the design of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV with improved in vivo efficacy by Perola, Emanuele, Stamos, Dean, Grillot, Anne-Laure, Ronkin, Steven, Wang, Tiansheng, LeTiran, Arnaud, Tang, Qing, Deininger, David D., Liao, Yusheng, Tian, Shi-Kai, Drumm, Joseph E., Nicolau, David P., Tessier, Pamela R., Mani, Nagraj, Grossman, Trudy H., Charifson, Paul S.

“…A series of dual targeting inhibitors of bacterial gyrase B and topoisomerase IV were identified and optimized to mid-to-low nanomolar potency against a…”
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Inhibitors of hepatitis C virus NS3·4A protease. Part 3: P 2 proline variants by Perni, Robert B, Farmer, Luc J, Cottrell, Kevin M, Court, John J, Courtney, Lawrence F, Deininger, David D, Gates, Cynthia A, Harbeson, Scott L, Kim, Joseph L, Lin, Chao, Lin, Kai, Luong, Yu-Ping, Maxwell, John P, Murcko, Mark A, Pitlik, Janos, Rao, B.Govinda, Schairer, Wayne C, Tung, Roger D, Van Drie, John H, Wilson, Keith, Thomson, John A

“…We recently described the identification of an optimized α-ketoamide warhead for our series of HCV NS3·4A inhibitors. We report herein a series of HCV protease…”
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Design and Synthesis of a Novel Series of Orally Bioavailable, CNS-Penetrant, Isoform Selective Phosphoinositide 3‑Kinase γ (PI3Kγ) Inhibitors with Potential for the Treatment of Multiple Sclerosis (MS) by Come, Jon H, Collier, Philip N, Henderson, James A, Pierce, Albert C, Davies, Robert J, Le Tiran, Arnaud, O’Dowd, Hardwin, Bandarage, Upul K, Cao, Jingrong, Deininger, David, Grey, Ron, Krueger, Elaine B, Lowe, Derek B, Liang, Jianglin, Liao, Yusheng, Messersmith, David, Nanthakumar, Suganthi, Sizensky, Emmanuelle, Wang, Jian, Xu, Jinwang, Chin, Elaine Y, Damagnez, Veronique, Doran, John D, Dworakowski, Wojciech, Griffith, James P, Jacobs, Marc D, Khare-Pandit, Suvarna, Mahajan, Sudipta, Moody, Cameron S, Aronov, Alex M

“…The lipid kinase phosphoinositide 3-kinase γ (PI3Kγ) has attracted attention as a potential target to treat a variety of autoimmune disorders, including…”
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Inhibitors of hepatitis C virus NS3·4A protease. Part 3: P2 proline variants by Perni, Robert B, Farmer, Luc J, Cottrell, Kevin M, Court, John J, Courtney, Lawrence F, Deininger, David D, Gates, Cynthia A, Harbeson, Scott L, Kim, Joseph L, Lin, Chao, Lin, Kai, Luong, Yu-Ping, Maxwell, John P, Murcko, Mark A, Pitlik, Janos, Rao, B.Govinda, Schairer, Wayne C, Tung, Roger D, Van Drie, John H, Wilson, Keith, Thomson, John A

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Novel Inhibitors of Cholesterol Degradation in Mycobacterium tuberculosis Reveal How the Bacterium's Metabolism Is Constrained by the Intracellular Environment: e1004679 by VanderVen, Brian C, Fahey, Ruth J, Lee, Wonsik, Liu, Yancheng, Abramovitch, Robert B, Memmott, Christine, Crowe, Adam M, Eltis, Lindsay D, Perola, Emanuele, Deininger, David D, Wang, Tiansheng, Locher, Christopher P, Russell, David G

“…Mycobacterium tuberculosis (Mtb) relies on a specialized set of metabolic pathways to support growth in macrophages. By conducting an extensive, unbiased…”
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Design and synthesis of novel conformationally restricted HIV protease inhibitors by Salituro, Francesco G., Baker, Christopher T., Court, John J., Deininger, David D., Kim, Eunice E., Li, Biquin, Novak, Perry M., Rao, Bhisetti G., Pazhanisamy, S., Porter, Margaret D., Schairer, Wayne C., Tung, Roger D.

“…A set of HIV protease inhibitors represented by compound 2 has previously been described. Structural and conformational analysis of this compound suggested…”
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New modified heterocyclic phenylalanine derivatives. Incorporation into potent inhibitors of human renin by Ocain, Timothy D, Deininger, David D, Russo, Ralph, Senko, Nancie A, Katz, Alan, Kitzen, Jan M, Mitchell, Robert, Oshiro, George, Russo, Anthony

“…Modified heterocyclic phenylalanine analogues designed as replacements for the P3-P4 region were synthesized and incorporated into renin inhibitors. These…”
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Inhibitors of hepatitis C virus NS3·4A protease 2. Warhead SAR and optimization by Perni, Robert B., Pitlik, Janos, Britt, Shawn D., Court, John J., Courtney, Lawrence F., Deininger, David D., Farmer, Luc J., Gates, Cynthia A., Harbeson, Scott L., Levin, Rhonda B., Lin, Chao, Lin, Kai, Moon, Young-Choon, Luong, Yu-Ping, O'Malley, Ethan T., Rao, B.Govinda, Thomson, John A., Tung, Roger D., Van Drie, John H., Wei, Yunyi

“…The α-ketoamide warhead (e.g., 15) was found to be a practical replacement for aliphatic aldehydes in a series of HCV NS3·4A protease inhibitors…”
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Facile preparation of fused ring azolylureas by Drumm, Joseph E., Deininger, David D., LeTiran, Arnaud, Wang, Tiansheng, Grillot, Anne-Laure, Liao, Yusheng, Ronkin, Steven M., Stamos, Dean P., Tang, Qing, Tian, Shi-Kai, Oliver-Shaffer, Patricia

“…Two novel reagents for the preparation of fused ring azolylureas are presented…”
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Inhibitors of hepatitis C virus NS3·4A protease 1. Non-Charged tetrapeptide variants by Perni, Robert B., Britt, Shawn D., Court, John C., Courtney, Lawrence F., Deininger, David D., Farmer, Luc J., Gates, Cynthia A., Harbeson, Scott L., Kim, Joseph L., Landro, James A., Levin, Rhonda B., Luong, Yu-Ping, O'Malley, Ethan T., Pitlik, Janos, Rao, B.Govinda, Schairer, Wayne C., Thomson, John A., Tung, Roger D., Van Drie, John H., Wei, Yunyi

“…Tetrapeptide-based peptidomimetic compounds have been shown to effectively inhibit the hepatitis C virus NS3·4A protease without the need of a charged…”
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Inhibitors of hepatitis C virus NS3.4A protease. Part 3: P2 proline variants by PERNI, Robert B, FARMER, Luc J, KAI LIN, LUONG, Yu-Ping, MAXWELL, John P, MURCKO, Mark A, PITLIK, Janos, GOVINDA RAO, B, SCHAIRER, Wayne C, TUNG, Roger D, VAN DRIE, John H, WILSON, Keith, COTTRELL, Kevin M, THOMSON, John A, COURT, John J, COURTNEY, Lawrence F, DEININGER, David D, GATES, Cynthia A, HARBESON, Scott L, KIM, Joseph L, CHAO LIN

“…We recently described the identification of an optimized alpha-ketoamide warhead for our series of HCV NS3.4A inhibitors. We report herein a series of HCV…”
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Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization by PERNI, Robert B, PITLIK, Janos, CHAO LIN, KAI LIN, MOON, Young-Choon, LUONG, Yu-Ping, O'MALLEY, Ethan T, GOVINDA RAO, B, THOMSON, John A, TUNG, Roger D, VAN DRIE, John H, YUNYI WEI, BRITT, Shawn D, COURT, John J, COURTNEY, Lawrence F, DEININGER, David D, FARMER, Luc J, GATES, Cynthia A, HARBESON, Scott L, LEVIN, Rhonda B

“…The alpha-ketoamide warhead (e.g., 15) was found to be a practical replacement for aliphatic aldehydes in a series of HCV NS3.4A protease inhibitors…”
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Inhibitors of hepatitis C virus NS3.4A protease 1. Non-charged tetrapeptide variants by PERNI, Robert B, BRITT, Shawn D, LEVIN, Rhonda B, LUONG, Yu-Ping, O'MALLEY, Ethan T, PITLIK, Janos, GOVINDA RAO, B, SCHAIRER, Wayne C, THOMSON, John A, TUNG, Roger D, VAN DRIE, John H, YUNYI WEI, COURT, John C, COURTNEY, Lawrence F, DEININGER, David D, FARMER, Luc J, GATES, Cynthia A, HARBESON, Scott L, KIM, Joseph L, LANDRO, James A

“…Tetrapeptide-based peptidomimetic compounds have been shown to effectively inhibit the hepatitis C virus NS3.4A protease without the need of a charged…”
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Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships by Charifson, Paul S, Grillot, Anne-Laure, Grossman, Trudy H, Parsons, Jonathan D, Badia, Michael, Bellon, Steve, Deininger, David D, Drumm, Joseph E, Gross, Christian H, LeTiran, Arnaud, Liao, Yusheng, Mani, Nagraj, Nicolau, David P, Perola, Emanuele, Ronkin, Steven, Shannon, Dean, Swenson, Lora L, Tang, Qing, Tessier, Pamela R, Tian, Ski-Kai, Trudeau, Martin, Wang, Tiansheng, Wei, Yunyi, Zhang, Hong, Stamos, Dean

“…The discovery of new antibacterial agents with novel mechanisms of action is necessary to overcome the problem of bacterial resistance that affects all…”
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Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors by Baker, Christopher T., Salituro, Francesco G., Court, John J., Deininger, David D., Kim, Eunice E., Li, Biquin, Novak, Perry M., Rao, Bhisetti G., Pazhanisamy, S., Schairer, Wayne C., Tung, Roger D.

“…A combination of structure-based design and both solution, and solid-phase synthesis were utilized to derive a potent (nM) series of HIV-1 protease inhibitors…”
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Synthesis and analgesic evaluation of 4-(2-heptyloxy)-7-[(Z)-(3-hydroxycyclohexyl)]indole: a caveat on indole-phenol bioisosterism by Soll, Richard M, Humber, Leslie G, Deininger, David, Asselin, Andre A, Chau, Thuy T, Weichman, Barry M

“…The synthesis of 4-(2-heptyloxy)-7-[(Z)-(3-hydroxycyclohexyl)]indole (7) is described. Compound 7 was tested for analgesic properties in the phenylbenzoquinone…”
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