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Syntheses and SAR studies of 4-(heteroarylpiperdin-1-yl-methyl)-pyrrolidin-1-yl-acetic acid antagonists of the human CCR5 chemokine receptor |
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| Authors: | Shankaran K Donnelly Karla L Shah Shrenik K Guthikonda Ravindra N MacCoss Malcolm Mills Sander G Gould Sandra L Malkowitz Lorraine Siciliano Salvatore J Springer Martin S Carella Anthony Carver Gwen Hazuda Daria Holmes Karen Kessler Joseph Lineberger Janet Miller Michael D Emini Emilio A Schleif William A |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. kothandaraman_shankaran@merck.com |
| 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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