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J Med Chem. 2011 Jun 9;54(11):3756-67. doi: 10.1021/jm200279v. Epub 2011 May 17.

Novel 4,4-disubstituted piperidine-based C-C chemokine receptor-5 inhibitors with high potency against human immunodeficiency virus-1 and an improved human ether-a-go-go related gene (hERG) profile.

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1
GlaxoSmithKline, Research Triangle Park, NC 27709, USA. kazmierski@gsk.com

Abstract

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 fine-tuning 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).

PMID:
21539377
DOI:
10.1021/jm200279v
[Indexed for MEDLINE]
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