Infectious Diseases Center for Excellence in Drug Discovery

Lake Park, NC, United States

Infectious Diseases Center for Excellence in Drug Discovery

Lake Park, NC, United States
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Kazmierski W.M.,Infectious Diseases Center for Excellence in Drug Discovery | Aquino C.,Metabolic Pathways Center for Excellence in Drug Discovery | Chauder B.A.,Metabolic Pathways Center for Excellence in Drug Discovery | Duan M.,Infectious Diseases Center for Excellence in Drug Discovery | And 10 more authors.
Journal of Medicinal Chemistry | Year: 2011

We recently described (J. Med. Chem. 2008, 51, 6538-6546) a novel class of CCR5 antagonists with strong anti-HIV potency. Herein, we detail SAR converting leads 1 and 2 to druglike molecules. The pivotal structural motif enabling this transition was the secondary sulfonamide substituent. Further finetuning of the substituent pattern in the sulfonamide paved the way to enhancing potency and bioavailability and minimizing hERG inhibition, resulting in discovery of clinical compound 122 (GSK163929). © 2011 American Chemical Society.

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