| 19620004 |
Williams DH, Adam F, Fenwick DR, Fok-Seang J, Gardner I, Hay D, Jaiessh R, Middleton DS, Mowbray CE, Parkinson T, Perros M, Pickford C, Platts M, Randall A, Siddle D, Stephenson PT, Tran TD, Vuong H: Discovery of a small molecule inhibitor through interference with the gp120-CD4 interaction. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5246-9. Epub 2009 Jun 25.
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. |
32(0,1,1,2) |