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Exploration of a new series of CCR5 antagonists: Multi-dimensional optimization of a sub-series containing N-substituted pyrazoles.

Bioorganic & medicinal chemistry letters 2010 Jul 1; In press

Link to PubMed abstract

Lemoine R RC, Petersen A AC, Setti L, Jekle A, Heilek G, Derosier A, Ji C, Berry P, Rotstein D DM

Department of Medicinal Chemistry, Roche Palo Alto LLC, 3431 Hillview Avenue, Palo Alto, CA 94304, USA.

The introduction of N-substituted pyrazoles in a new series of CCR5 antagonists was shown to substantially increase antiviral activity.

Keywords: CCR5