Title of article
Piperazine-Based CCR5 antagonists as HIV-1 inhibitors. I: 2(S)-methyl piperazine as a key pharmacophore element
Author/Authors
Jayaram R. Tagat، نويسنده , , Stuart W. McCombie، نويسنده , , Ruo W. Steensma، نويسنده , , Sue-Ing Lin، نويسنده , , Dennis V. Nazareno، نويسنده , , Bahige Baroudy، نويسنده , , Nicole Vantuno، نويسنده , , Serena Xu، نويسنده , , Jia Liu، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2001
Pages
4
From page
2143
To page
2146
Abstract
Optimization of the piperidino-piperazines 1 and 2 provided early leads 3 and 4, which showed good activity in the CCR5–RANTES binding assay and in antiviral assays. A systematic study around these structures showed that the 2(S)-methyl piperazine is essential for CCR5 affinity, which is further enhanced by forming the 2,6-dimethyl benzamide of the piperidine.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2001
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
791584
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