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Combinatorial synthesis of CCR5 antagonists

2001; Elsevier BV; Volume: 11; Issue: 24 Linguagem: Inglês

10.1016/s0960-894x(01)00652-7

1464-3405

Christopher A. Willoughby, Scott C. Berk, Keith G. Rosauer, Silvia Degrado, Kevin T. Chapman, Sandra L. Gould, Martin S. Springer, Lorraine Malkowitz, William A. Schleif, Daria J. Hazuda, Michael D. Miller, Joseph Kessler, Renee Danzeisen, Karen Holmes, Janet Lineberger, Anthony Carella, Gwen Carver, Emilio A. Emini,

Monoclonal and Polyclonal Antibodies Research

Herein we report the preparation of a combinatorial library of compounds with potent CCR5 binding affinity. The library design was aided by SAR generated in a traditional medicinal chemistry effort. Compounds with novel combinations of subunits were discovered that have high binding affinity for the CCR5 receptor. A potent CCR5 antagonist from the library, compound 11 was found to have moderate anti-HIV-1 activity.