Zobrazeno 1 - 10
of 13
pro vyhledávání: '"Elyse Bourque"'
Autor:
Yoko Shimizu, S.-H. Sheldon Tai, Nag S. Kumar, Michel Roberge, Elyse Bourque, Masahiro Niikura, Olga Agafitei, James Brian Jaquith, Fahimeh S. Shidmoossavee, Steve Arns, Aruna D. Balgi, Tom A. Pfeifer, Sharon Sun
Publikováno v:
European Journal of Medicinal Chemistry. 120:64-73
The development of treatments for influenza that inhibit the M2 proton channel without being susceptible to the widespread resistance mechanisms associated with the adamantanes is an ongoing challenge. Using a yeast high-throughput yeast growth resto
Autor:
Renato Skerlj, Tuya Ba, Ernest J. McEachern, Elyse Bourque, Ian Baird, Dominique Schols, Wilson Trevor R, Renee Mosi, Jonathan Langille, Yuanxi Zhou, Bryon Carpenter, Michael Bey, Simon P. Fricker, Dana Huskens, Duane Veale, Rebecca S.Y. Wong, Gary Bridger, Curtis Harwig, Veronique Bodart, Ron MacFarland, Markus Metz, Sanjay Danthi
Publikováno v:
ACS Medicinal Chemistry Letters. 3:216-221
A series of CCR5 antagonists representing the thiophene-3-yl-methyl ureas were designed that met the pharmacological criteria for HIV-1 inhibition and mitigated a human ether-a-go-go related gene (hERG) inhibition liability. Reducing lipophilicity wa
Autor:
Renato Skerlj, Gary Bridger, Yuanxi Zhou, Elyse Bourque, Ernest McEachern, Jonathan Langille, Curtis Harwig, Duane Veale, Wen Yang, Tongshong Li, Yongbao Zhu, Michael Bey, Ian Baird, Michael Sartori, Markus Metz, Renee Mosi, Kim Nelson, Veronique Bodart, Rebecca Wong, Simon Fricker, Ron Mac Farland, Dana Huskens, Dominique Schols
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:6950-6954
A series of CCR5 antagonists were optimized for potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells. Compounds that met acceptable ADME criteria, selectivity, human plasma protein binding, potency shift in the presence of
Autor:
Zefferino Santucci, Gary Bridger, Gloria Lau, Dominique Schols, Elyse Bourque, Wen Yang, Simon P. Fricker, Markus Metz, Curtis Harwig, Marilyn C. Darkes, Renato T. Skerlj, Jonathan Langille, Jean Labrecque, Sanjay Danthi
Publikováno v:
Journal of the American Chemical Society. 133:16477-16485
The viral resistance of marketed antiviral drugs including the emergence of new viral resistance of the only marketed CCR5 entry inhibitor, maraviroc, makes it necessary to develop new CCR5 allosteric inhibitors. A mutagenesis/modeling approach was u
Autor:
Renato Skerlj, Gary Bridger, Yuanxi Zhou, Elyse Bourque, Jonathan Langille, Maria Di Fluri, David Bogucki, Wen Yang, Tongshuang Li, Letian Wang, Susan Nan, Ian Baird, Markus Metz, Marilyn Darkes, Jean Labrecque, Gloria Lau, Simon Fricker, Dana Huskens, Dominique Schols
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:2450-2455
A novel series of CCR5 antagonists were identified based on the redesign of Schering C. An SAR was established based on inhibition of CCR5 (RANTES) binding and these compounds exhibited potent inhibition of R5 HIV-1 replication in peripheral blood mo
Autor:
Adam Galey, Stephen G. Withers, Natalia Zisman, Jenna Udechukwu, Jay Paquette, Jason Samuel Tan, Elyse Bourque, Samantha Dercho, Richard Liggins, Fiona C. Ross, Sharon Sun, Murray S. Webb, Vionarica Gusti, Steve Arns
Publikováno v:
Bioorganicmedicinal chemistry letters. 25(12)
Difluorosialic acids (DFSAs) are potent inhibitors of viral neuraminidase that demonstrate activity against oseltamivir- and zanamivir-resistant strains of influenza. Unfortunately, low oral bioavailability precludes their development as second gener
Publikováno v:
Synthesis. :3219-3224
A synthesis of the C14-C28 fragment of Tetronasin features an S E 2 reaction between a cationic η 3 -allylmolybdenum complex and and an α-metallated tetrahydrofuran.
Publikováno v:
The Journal of Organic Chemistry. 68:2390-2397
A thorough study of the transannular Diels-Alder (TADA) reaction of trans-trans-trans macrocyclic trienes was carried out. It led to a better understanding of various parameters that govern the TADA reaction in particular and the Diels-Alder reaction
Autor:
Curtis Harwig, Dominique Schols, Gang Chen, Wen Yang, Duane Veale, Susan Nan, Simon P. Fricker, Alan Kaller, Danielle Guay, Jason M. Crawford, Michael Satori, Markus Metz, Yongbao Zhu, Helen Yee, Maria Krumpak, Elyse Bourque, Wilson Trevor R, David Bogucki, Bryon Carpenter, Michael Bey, David C. Leitch, Ron MacFarland, David Gauthier, Ian Baird, Rebecca Wong, Renato T. Skerlj, Jonathan Langille, Yuanxi Zhou, Gary Bridger, Renee Mosi, Ernest J. McEachern, Tuya Ba, Tong-Shuang Li, Krystyna Vocadlo, Veronique Bodart
Publikováno v:
Journal of medicinal chemistry. 56(20)
The redesign of the previously reported thiophene-3-yl-methyl urea series, as a result of potential cardiotoxicity, was successfully accomplished, resulting in the identification of a novel potent series of CCR5 antagonists containing the imidazolidi
Publikováno v:
Organic Letters. 2:4149-4152
The transannular Diels-Alder reaction of trans-trans-trans macrocyclic triene A, bearing two cis substiuents in C(12) and C(13) as well as a gem-dimethyl in C(4), was studied. Under thermal conditions, only the desired trans-anti-cis tricycle B was o