Ongoing efforts from these laboratories have resulted in the identification of 5-(piperidin-1-yl)-3-phenylpentylsulfones as a potent CCR5 antagonists. The syntheses and biological activities such as ...analogs are described.
Cellular proliferation of HIV-1 requires the cooperative assistance of both the CCR5 and CD4 receptors. Our medicinal chemistry efforts in this area have resulted in the identification of
N-alkyl piperidine sulfones as CCR5 antagonists. These compounds display potent binding and show antiviral properties in HIV-1 spread cell-based assays.
Two insulin-dependent diabetic patients with advanced nonproliferative and early proliferative retinopathy showed regression of diabetic retinopathy after three weeks of intensive plasmapheresis. ...Because of the sudden unexplained death in one patient, the study was stopped. However, these observations in this pilot study suggest that factors mediated through plasma contribute to the pathogenesis of diabetic microangiopathy.
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