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Development of Cell-type specific anti-HIV gp120 aptamers for siRNA delivery
Published on: June 23, 2011
Discovery of a small molecule inhibitor through interference with the gp120-CD4 interaction
David H Williams1, Fiona Adam, David R Fenwick
1Department of Chemistry, Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich, Kent, UK. David.H.Williams@pfizer.com
Bioorganic & Medicinal Chemistry Letters
|July 22, 2009
Abstract:
A series of piperazine derivatives were designed and synthesised as gp120-CD4 inhibitors. SAR studies led to the discovery of potent inhibitors in a cell based anti viral assay represented by compounds 9 and 28. The rat pharmacokinetic and antiviral profiles of selected compounds are also presented.

