Mitigating hERG Inhibition: Design of Orally Bioavailable CCR5 Antagonists as Potent Inhibitors of R5 HIV-1 Replication

[Image: see text] 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 was the main design criteria used...

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Bibliografski detalji
Glavni autori: Skerlj, Renato, Bridger, Gary, Zhou, Yuanxi, Bourque, Elyse, McEachern, Ernest, Danthi, Sanjay, Langille, Jonathan, Harwig, Curtis, Veale, Duane, Carpenter, Bryon, Ba, Tuya, Bey, Michael, Baird, Ian, Wilson, Trevor, Metz, Markus, MacFarland, Ron, Mosi, Renee, Bodart, Veronique, Wong, Rebecca, Fricker, Simon, Huskens, Dana, Schols, Dominique
Format: Artigo
Jezik:Inglês
Izdano: American Chemical Society 2012
Online pristup:https://ncbi.nlm.nih.gov/pmc/articles/PMC4025809/
https://ncbi.nlm.nih.gov/pubmed/24900457
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml2002604
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