Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Duane Veale"'
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a9674269a09a599b87e9e9ed8edb34dc
https://doi.org/10.1021/ml2002604
https://doi.org/10.1021/ml2002604
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fe8c7c65ea6806cdd761d65d01e7a8e4
https://doi.org/10.1016/j.bmcl.2011.09.133
https://doi.org/10.1016/j.bmcl.2011.09.133
Autor:
Curtis Harwig, Rossana Wauthy, Renato Skerlj, Fluri Maria Di, Yongbao Zhu, Duane Veale, Dominique Schols, Gary Bridger, Helen Yee, Wen Yang, Wilson Trevor R, David Bogucki, Christopher Ronald Smith, Erik De Clercq, Krystyna A. Skupinska, Jonathon Langille, Jason M. Crawford, Dana Huskens, Ernie Mceachern
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:262-266
An early lead from the AMD070 program was optimized and a structure-activity relationship was developed for a novel series of heterocyclic containing compounds. Potent CXCR4 antagonists were identified based on anti-HIV-1 activity and Ca(2+) flux inh
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63b434e9cc08b4cd6ef59fcf57d365da
https://doi.org/10.1016/j.bmcl.2010.11.023
https://doi.org/10.1016/j.bmcl.2010.11.023
Publikováno v:
Canadian Journal of Chemistry. 82:240-253
The photochemistry of naphthols 1, 2, 4, 5 and 9, and phenol 10 has been studied in aqueous solution with the primary aim of exploring the viability of such compounds for naphthoquinone and quinone methide photogeneration, along the lines already dem
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::698acaf0c287142b865e79fec353cdd8
https://doi.org/10.1139/v03-184
https://doi.org/10.1139/v03-184
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
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::63349d2f129c824dd1d79fd4e3bd1bc8
https://pubmed.ncbi.nlm.nih.gov/24090135
https://pubmed.ncbi.nlm.nih.gov/24090135
Autor:
Dana Huskens, Ernest J. McEachern, Yongbao Zhu, Helen Yee, Krystyna A. Skupinska, Michael Sartori, Alan Kaller, Gary Bridger, Renato Skerlj, Erik De Clercq, Duane Veale, Ian Baird, Letian Wang, Kate Burrage, Dominique Schols, Wen Yang, Christopher Ronald Smith, Curtis Harwig, Rossana Wauthy
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(5)
A novel series of CXCR4 antagonists were identified based on the substantial redesign of AMD070. These compounds possessed potent anti-HIV-1 activity and showed excellent pharmacokinetics in rat and dog.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::75cb77b6ca0b89a136d84dcf38390783
https://pubmed.ncbi.nlm.nih.gov/21295470
https://pubmed.ncbi.nlm.nih.gov/21295470
Autor:
Duane Veale, Jason B. Crawford, Gary Bridger, Erik De Clercq, Dominique Schols, Ernest J. McEachern, Bem Atsma, Katrien Princen, Jonathon Langille, Renato Skerlj, Yuanxi Zhou, Al Kaller, Curtis Harwig, Sigrid Hatse, Susan Nan, Wilson Trevor R
Publikováno v:
Journal of medicinal chemistry. 53(8)
The redesign of azamacrocyclic CXCR4 chemokine receptor antagonists resulted in the discovery of novel, small molecule, orally bioavailable compounds that retained T-tropic (CXCR4 using, X4) anti-HIV-1 activity. A structure-activity relationship (SAR
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::663101abb0ab1751a6b2a5c1fb261d05
https://pubmed.ncbi.nlm.nih.gov/20297846
https://pubmed.ncbi.nlm.nih.gov/20297846