Literature DB >> 19620004

Discovery of a small molecule inhibitor through interference with the gp120-CD4 interaction.

David H Williams1, Fiona Adam, David R Fenwick, Juin Fok-Seang, Iain Gardner, Duncan Hay, Rawal Jaiessh, Donald S Middleton, Charles E Mowbray, Tanya Parkinson, Manos Perros, Christopher Pickford, Michelle Platts, Amy Randall, Daniel Siddle, Peter T Stephenson, Thien-Duc Tran, Hannah Vuong.   

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.

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Year:  2009        PMID: 19620004     DOI: 10.1016/j.bmcl.2009.06.080

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Core chemotype diversification in the HIV-1 entry inhibitor class using field-based bioisosteric replacement.

Authors:  Marina Tuyishime; Rae Lawrence; Simon Cocklin
Journal:  Bioorg Med Chem Lett       Date:  2015-10-27       Impact factor: 2.823

  1 in total

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