Article

Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor.

Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
Bioorganic & Medicinal Chemistry Letters (impact factor: 2.55). 08/2004; 14(13):3419-24. DOI:10.1016/j.bmcl.2004.04.078 pp.3419-24
Source: PubMed

ABSTRACT Efforts toward the exploration of the title compounds as CCR5 antagonists are disclosed. The basis for such work stems from the fact that cellular proliferation of HIV-1 requires the cooperative assistance of both CCR5 and CD4 receptors. The synthesis and SAR of pyrrolidineacetic acid derivatives as CCR5 antagonists displaying potent binding and antiviral properties in a HeLa cell-based HIV-1 infectivity assay are discussed.

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Keywords

antiviral properties
 
CCR5
 
CCR5 antagonists
 
CD4 receptors
 
cellular proliferation
 
HeLa cell-based HIV-1 infectivity assay
 
potent binding
 
pyrrolidineacetic acid derivatives