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Your search keyword '"Carter, David S."' showing total 5 results
Start Over Author "Carter, David S." Journal journal of medicinal chemistry
5 results on '"Carter, David S."'

1. Boron-Pleuromutilins as Anti-Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis

Author

Jacobs, Robert T., primary, Lunde, Christopher S., additional, Freund, Yvonne R., additional, Hernandez, Vincent, additional, Li, Xianfeng, additional, Xia, Yi, additional, Carter, David S., additional, Berry, Pamela W., additional, Halladay, Jason, additional, Rock, Fernando, additional, Stefanakis, Rianna, additional, Easom, Eric, additional, Plattner, Jacob J., additional, Ford, Louise, additional, Johnston, Kelly L., additional, Cook, Darren A. N., additional, Clare, Rachel, additional, Cassidy, Andrew, additional, Myhill, Laura, additional, Tyrer, Hayley, additional, Gamble, Joanne, additional, Guimaraes, Ana F., additional, Steven, Andrew, additional, Lenz, Franziska, additional, Ehrens, Alexandra, additional, Frohberger, Stefan J., additional, Koschel, Marianne, additional, Hoerauf, Achim, additional, Hübner, Marc P., additional, McNamara, Case W., additional, Bakowski, Malina A., additional, Turner, Joseph D., additional, Taylor, Mark J., additional, and Ward, Stephen A., additional

Published
2019
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2. Boron-Pleuromutilins as Anti-WolbachiaAgents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis

Author

Jacobs, Robert T., Lunde, Christopher S., Freund, Yvonne R., Hernandez, Vincent, Li, Xianfeng, Xia, Yi, Carter, David S., Berry, Pamela W., Halladay, Jason, Rock, Fernando, Stefanakis, Rianna, Easom, Eric, Plattner, Jacob J., Ford, Louise, Johnston, Kelly L., Cook, Darren A. N., Clare, Rachel, Cassidy, Andrew, Myhill, Laura, Tyrer, Hayley, Gamble, Joanne, Guimaraes, Ana F., Steven, Andrew, Lenz, Franziska, Ehrens, Alexandra, Frohberger, Stefan J., Koschel, Marianne, Hoerauf, Achim, Hübner, Marc P., McNamara, Case W., Bakowski, Malina A., Turner, Joseph D., Taylor, Mark J., and Ward, Stephen A.

Abstract

A series of pleuromutilins modified by introduction of a boron-containing heterocycle on C(14) of the polycyclic core are described. These analogs were found to be potent anti-Wolbachiaantibiotics and, as such, may be useful in the treatment of filarial infections caused by Onchocerca volvulus, resulting in Onchocerciasis or river blindness, or Wuchereria bancroftiand Brugia malayiand related parasitic nematodes resulting in lymphatic filariasis. These two important neglected tropical diseases disproportionately impact patients in the developing world. The lead preclinical candidate compound containing 7-fluoro-6-oxybenzoxaborole (15, AN11251) was shown to have good in vitro anti-Wolbachiaactivity and physicochemical and pharmacokinetic properties providing high exposure in plasma. The lead was effective in reducing the Wolbachiaload in filarial worms following oral administration to mice.

Published
2019
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3. Discovery of N-[4-[6-tert-Butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]methanesulfonamide (RG7109), a Potent Inhibitor of the Hepatitis C Virus NS5B Polymerase

Author

Talamas, Francisco X., primary, Abbot, Sarah C., additional, Anand, Shalini, additional, Brameld, Ken A., additional, Carter, David S., additional, Chen, Jun, additional, Davis, Dana, additional, de Vicente, Javier, additional, Fung, Amy D., additional, Gong, Leyi, additional, Harris, Seth F., additional, Inbar, Petra, additional, Labadie, Sharada S., additional, Lee, Eun K., additional, Lemoine, Remy, additional, Le Pogam, Sophie, additional, Leveque, Vincent, additional, Li, Jim, additional, McIntosh, Joel, additional, Nájera, Isabel, additional, Park, Jaehyeon, additional, Railkar, Aruna, additional, Rajyaguru, Sonal, additional, Sangi, Michael, additional, Schoenfeld, Ryan C., additional, Staben, Leanna R., additional, Tan, Yunchou, additional, Taygerly, Joshua P., additional, Villaseñor, Armando G., additional, and Weller, Paul E., additional

Published
2013
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4. Discovery of N-[4-[6-tert-Butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]methanesulfonamide(RG7109), a Potent Inhibitor of the Hepatitis C Virus NS5B Polymerase.

Author

Talamas, Francisco X., Abbot, Sarah C., Anand, Shalini, Brameld, Ken A., Carter, David S., Chen, Jun, Davis, Dana, de Vicente, Javier, Fung, Amy D., Gong, Leyi, Harris, Seth F., Inbar, Petra, Labadie, Sharada S., Lee, Eun K., Lemoine, Remy, Le Pogam, Sophie, Leveque, Vincent, Li, Jim, McIntosh, Joel, and Nájera, Isabel

Published
2014
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5. Discovery of N-[4-[6-tert-butyl-5-methoxy-8-(6-methoxy-2-oxo-1H-pyridin-3-yl)-3-quinolyl]phenyl]methanesulfonamide (RG7109), a potent inhibitor of the hepatitis C virus NS5B polymerase.

Author

Talamas FX, Abbot SC, Anand S, Brameld KA, Carter DS, Chen J, Davis D, de Vicente J, Fung AD, Gong L, Harris SF, Inbar P, Labadie SS, Lee EK, Lemoine R, Le Pogam S, Leveque V, Li J, McIntosh J, Nájera I, Park J, Railkar A, Rajyaguru S, Sangi M, Schoenfeld RC, Staben LR, Tan Y, Taygerly JP, Villaseñor AG, and Weller PE

Subjects
Animals, Antiviral Agents chemistry, Antiviral Agents pharmacokinetics, Dogs, Drug Discovery, Enzyme Inhibitors chemistry, Enzyme Inhibitors pharmacokinetics, Hepacivirus enzymology, Humans, Models, Molecular, Quinolines chemistry, Quinolines pharmacokinetics, Rats, Sulfonamides chemistry, Sulfonamides pharmacokinetics, Antiviral Agents pharmacology, Enzyme Inhibitors pharmacology, Hepacivirus drug effects, Quinolines pharmacology, Sulfonamides pharmacology, Viral Nonstructural Proteins antagonists & inhibitors
Abstract

In the past few years, there have been many advances in the efforts to cure patients with hepatitis C virus (HCV). The ultimate goal of these efforts is to develop a combination therapy consisting of only direct-antiviral agents (DAAs). In this paper, we discuss our efforts that led to the identification of a bicyclic template with potent activity against the NS5B polymerase, a critical enzyme on the life cycle of HCV. In continuation of our exploration to improve the stilbene series, the 3,5,6,8-tetrasubstituted quinoline core was identified as replacement of the stilbene moiety. 6-Methoxy-2(1H)-pyridone was identified among several heterocyclic headgroups to have the best potency. Solubility of the template was improved by replacing a planar aryl linker with a saturated pyrrolidine. Profiling of the most promising compounds led to the identification of quinoline 41 (RG7109), which was selected for advancement to clinical development.

Published
2014
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