Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2010 May 15;20(10):3026-30.

Synthesis and SAR of novel isoquinoline CXCR4 antagonists with potent anti-HIV activity.

Author information

1
Department of Medicinal Chemistry, Infectious Diseases Center for Excellence in Drug Discovery, GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709-3398, USA. john.6.miller@gsk.com

Abstract

Using AMD070 as a starting point for structural modification, a novel series of isoquinoline CXCR4 antagonists was developed. A structure-activity scan of alternate lower heterocycles led to the 3-isoquinolinyl moiety as an attractive replacement for benzimidazole. Side chain optimization in the isoquinoline series led to a number of compounds with low nanomolar anti-HIV activities and promising rat PK properties.

PMID:
20443225
DOI:
10.1016/j.bmcl.2010.03.118
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center