Preclinical activity of VX-787, a first-in-class, orally bioavailable inhibitor of the influenza virus polymerase PB2 subunit
Byrn, Randal A, Jones, Steven M, Bennett, Hamilton B, Bral, Chris, Clark, Michael P, Jacobs, Marc D, Kwong, Ann D, Ledeboer, Mark W, Leeman, Joshua R, McNeil, Colleen F, Murcko, Mark A, Nezami, Azin, Perola, Emanuele, Rijnbrand, Rene, Saxena, Kumkum, Tsai, Alice W, Zhou, Yi, Charifson, Paul S
Published in Antimicrobial agents and chemotherapy (01.03.2015)
Published in Antimicrobial agents and chemotherapy (01.03.2015)
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Discovery of a Novel, First-in-Class, Orally Bioavailable Azaindole Inhibitor (VX-787) of Influenza PB2
Clark, Michael P, Ledeboer, Mark W, Davies, Ioana, Byrn, Randal A, Jones, Steven M, Perola, Emanuele, Tsai, Alice, Jacobs, Marc, Nti-Addae, Kwame, Bandarage, Upul K, Boyd, Michael J, Bethiel, Randy S, Court, John J, Deng, Hongbo, Duffy, John P, Dorsch, Warren A, Farmer, Luc J, Gao, Huai, Gu, Wenxin, Jackson, Katrina, Jacobs, Dylan H, Kennedy, Joseph M, Ledford, Brian, Liang, Jianglin, Maltais, François, Murcko, Mark, Wang, Tiansheng, Wannamaker, M. Woods, Bennett, Hamilton B, Leeman, Joshua R, McNeil, Colleen, Taylor, William P, Memmott, Christine, Jiang, Min, Rijnbrand, Rene, Bral, Christopher, Germann, Ursula, Nezami, Azin, Zhang, Yuegang, Salituro, Francesco G, Bennani, Youssef L, Charifson, Paul S
Published in Journal of medicinal chemistry (14.08.2014)
Published in Journal of medicinal chemistry (14.08.2014)
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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
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
Published in Journal of medicinal chemistry (11.09.2008)
Published in Journal of medicinal chemistry (11.09.2008)
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Second-Generation Antibacterial Benzimidazole Ureas: Discovery of a Preclinical Candidate with Reduced Metabolic Liability
Grillot, Anne-Laure, Tiran, Arnaud Le, Shannon, Dean, Krueger, Elaine, Liao, Yusheng, O’Dowd, Hardwin, Tang, Qing, Ronkin, Steve, Wang, Tiansheng, Waal, Nathan, Li, Pan, Lauffer, David, Sizensky, Emmanuelle, Tanoury, Jerry, Perola, Emanuele, Grossman, Trudy H, Doyle, Tim, Hanzelka, Brian, Jones, Steven, Dixit, Vaishali, Ewing, Nigel, Liao, Shengkai, Boucher, Brian, Jacobs, Marc, Bennani, Youssef, Charifson, Paul S
Published in Journal of medicinal chemistry (13.11.2014)
Published in Journal of medicinal chemistry (13.11.2014)
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Journal Article
Discovery of Novel, Orally Bioavailable Pyrimidine Ether-Based Inhibitors of ELOVL1
Boyd, Michael J, Collier, Philip N, Clark, Michael P, Deng, Hongbo, Kesavan, Sarathy, Ronkin, Steven M, Waal, Nathan, Wang, Jian, Cao, Jingrong, Li, Pan, Come, Jon, Davies, Ioana, Duffy, John P, Cochran, John E, Court, John J, Chandupatla, Kishan, Jackson, Katrina L, Maltais, Francois, O’Dowd, Hardwin, Boucher, Christina, Considine, Tony, Taylor, William P, Gao, Hong, Chakilam, Ananthisrinivas, Engtrakul, Juntyma, Crawford, Dan, Doyle, Elizabeth, Phillips, Jonathan, Kemper, Raymond, Swett, Rebecca, Empfield, James, Bunnage, Mark E, Charifson, Paul S, Magavi, Sanjay Shivayogi
Published in Journal of medicinal chemistry (23.12.2021)
Published in Journal of medicinal chemistry (23.12.2021)
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Discovery and Optimization of Pyrazole Amides as Inhibitors of ELOVL1
Come, Jon H, Senter, Timothy J, Clark, Michael P, Court, John J, Gale-Day, Zachary, Gu, Wenxin, Krueger, Elaine, Liang, Jianglin, Morris, Mark, Nanthakumar, Suganthini, O’Dowd, Hardwin, Maltais, Francois, Iyer, Ganesh, Andreassi, John, Boucher, Christina, Considine, Tony, Moody, Cameron S, Taylor, William, Mohanty, Arun K, Huang, Yulin, Zuccola, Harmon, Coll, Joyce, Bonanno, Kenneth C, Gagnon, Kevin J, Gan, Lu, Lu, Fan, Gao, Hong, Chakilam, Ananthisrinivas, Engtrakul, Juntyma, Song, Bin, Crawford, Dan, Doyle, Elisabeth, Kramer, Tal, Vought, Bryan, Phillips, Jonathan, Kemper, Raymond, Sanders, Martin, Swett, Rebecca, Furey, Brinley, Winquist, Ray, Bunnage, Mark E, Jackson, Katrina L, Charifson, Paul S, Magavi, Sanjay S
Published in Journal of medicinal chemistry (23.12.2021)
Published in Journal of medicinal chemistry (23.12.2021)
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Discovery of pyrazolthiazoles as novel and potent inhibitors of bacterial gyrase
Ronkin, Steven M., Badia, Michael, Bellon, Steve, Grillot, Anne-Laure, Gross, Christian H., Grossman, Trudy H., Mani, Nagraj, Parsons, Jonathan D., Stamos, Dean, Trudeau, Martin, Wei, Yunyi, Charifson, Paul S.
Published in Bioorganic & medicinal chemistry letters (01.05.2010)
Published in Bioorganic & medicinal chemistry letters (01.05.2010)
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Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors
Boyd, Michael J., Bandarage, Upul K., Bennett, Hamilton, Byrn, Randal R., Davies, Ioana, Gu, Wenxin, Jacobs, Marc, Ledeboer, Mark W., Ledford, Brian, Leeman, Joshua R., Perola, Emanuele, Wang, Tiansheng, Bennani, Youssef, Clark, Michael P., Charifson, Paul S.
Published in Bioorganic & medicinal chemistry letters (01.05.2015)
Published in Bioorganic & medicinal chemistry letters (01.05.2015)
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Novel 2‑Substituted 7‑Azaindole and 7‑Azaindazole Analogues as Potential Antiviral Agents for the Treatment of Influenza
Bandarage, Upul K., Clark, Michael P., Perola, Emanuele, Gao, Huai, Jacobs, Marc D., Tsai, Alice, Gillespie, Jeffery, Kennedy, Joseph M., Maltais, François, Ledeboer, Mark W., Davies, Ioana, Gu, Wenxin, Byrn, Randal A., Nti Addae, Kwame, Bennett, Hamilton, Leeman, Joshua R., Jones, Steven M., O’Brien, Colleen, Memmott, Christine, Bennani, Youssef, Charifson, Paul S.
Published in ACS medicinal chemistry letters (09.02.2017)
Published in ACS medicinal chemistry letters (09.02.2017)
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Design, synthesis and biological evaluation of potent NAD+-dependent DNA ligase inhibitors as potential antibacterial agents. Part 2: 4-Amino-pyrido[2,3-d]pyrimidin-5(8H)-ones
Wang, Tiansheng, Duncan, Leonard, Gu, Wenxin, O’Dowd, Hardwin, Wei, Yunyi, Perola, Emanuele, Parsons, Jonathan, Gross, Christian H., Moody, Cameron Stuver, Ryan Arends, S.J., Charifson, Paul S.
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
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Journal Article
Novel Ranking System for Identifying Efficacious Anti-Influenza Virus PB2 Inhibitors
Tsai, Alice W, McNeil, Colleen F, Leeman, Joshua R, Bennett, Hamilton B, Nti-Addae, Kwame, Huang, Cassey, Germann, Ursula A, Byrn, Randal A, Berlioz-Seux, Francoise, Rijnbrand, Rene, Clark, Michael P, Charifson, Paul S, Jones, Steven M
Published in Antimicrobial agents and chemotherapy (01.10.2015)
Published in Antimicrobial agents and chemotherapy (01.10.2015)
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Dual Targeting of GyrB and ParE by a Novel Aminobenzimidazole Class of Antibacterial Compounds
GROSSMAN, Trudy H, BARTELS, Douglas J, MANI, Nagraj, MULLIN, Steve, GROSS, Christian H, PARSONS, Jonathan D, YUSHENG LIAO, GRILLOT, Anne-Laure, STAMOS, Dean, OLSON, Eric R, CHARIFSON, Paul S
Published in Antimicrobial Agents and Chemotherapy (01.02.2007)
Published in Antimicrobial Agents and Chemotherapy (01.02.2007)
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Crystal Structures of Escherichia coli Topoisomerase IV ParE Subunit (24 and 43 Kilodaltons): a Single Residue Dictates Differences in Novobiocin Potency against Topoisomerase IV and DNA Gyrase
BELLON, Steven, PARSONS, Jonathan D, YUNYI WEI, HAYAKAWA, Koto, SWENSON, Lora L, CHARIFSON, Paul S, LIPPKE, Judith A, ALDAPE, Robert, GROSS, Christian H
Published in Antimicrobial Agents and Chemotherapy (01.05.2004)
Published in Antimicrobial Agents and Chemotherapy (01.05.2004)
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Journal Article
Discovery of Novel, Orally Bioavailable β‑Amino Acid Azaindole Inhibitors of Influenza PB2
Farmer, Luc J., Clark, Michael P., Boyd, Michael J., Perola, Emanuele, Jones, Steven M., Tsai, Alice, Jacobs, Marc D., Bandarage, Upul K., Ledeboer, Mark W., Wang, Tiansheng, Deng, Hongbo, Ledford, Brian, Gu, Wenxin, Duffy, John P., Bethiel, Randy S., Shannon, Dean, Byrn, Randal A., Leeman, Joshua R., Rijnbrand, Rene, Bennett, Hamilton B., O’Brien, Colleen, Memmott, Christine, Nti-Addae, Kwame, Bennani, Youssef L., Charifson, Paul S.
Published in ACS medicinal chemistry letters (09.02.2017)
Published in ACS medicinal chemistry letters (09.02.2017)
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Journal Article
In Vitro Characterization of the Antibacterial Spectrum of Novel Bacterial Type II Topoisomerase Inhibitors of the Aminobenzimidazole Class
MANI, Nagraj, GROSS, Christian H, GROSSMAN, Trudy H, PARSONS, Jonathan D, HANZELKA, Brian, MÜH, Ute, MULLIN, Steve, YUSHENG LIAO, GRILLOT, Anne-Laure, STAMOS, Dean, CHARIFSON, Paul S
Published in Antimicrobial Agents and Chemotherapy (01.04.2006)
Published in Antimicrobial Agents and Chemotherapy (01.04.2006)
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