| Literature DB >> 17931865 |
Thorsten E Fisher1, Boyoung Kim, Donnette D Staas, Terry A Lyle, Steven D Young, Joseph P Vacca, Matthew M Zrada, Daria J Hazuda, Peter J Felock, William A Schleif, Lori J Gabryelski, M Reza Anari, Christopher J Kochansky, John S Wai.
Abstract
A series of potent novel 8-hydroxy-3,4-dihydropyrrolo[1,2-a]pyrazine-1(2H)-one HIV-1 integrase inhibitors was identified. These compounds inhibited the strand transfer process of HIV-1 integrase and viral replication in cells. Compound 12 is active against replication of HIV-1 in cell culture with a CIC(95) of 0.31microM. Further SAR exploration led to the preparation of pseudosymmetrical tricyclic pyrrolopyrazine inhibitors 23 and 24 with further improvement in antiviral activity.Entities:
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Year: 2007 PMID： 17931865 DOI： 10.1016/j.bmcl.2007.09.086
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823