Pyrazolo-Piperidines Exhibit Dual Inhibition of CCR5/CXCR4 HIV Entry and Reverse Transcriptase.
Basic Information
ID: ALA3608277
Journal: ACS Med Chem Lett
Title: Pyrazolo-Piperidines Exhibit Dual Inhibition of CCR5/CXCR4 HIV Entry and Reverse Transcriptase.
Authors: Cox BD, Prosser AR, Sun Y, Li Z, Lee S, Huang MB, Bond VC, Snyder JP, Krystal M, Wilson LJ, Liotta DC.
Abstract: We report novel anti-HIV-1 agents with combined dual host-pathogen pharmacology. Lead compound 3, composed of a pyrazole-piperidine core, exhibits three concurrent mechanisms of action: (1) non-nucleoside reverse transcriptase inhibition, (2) CCR5-mediated M-tropic viral entry inhibition, and (3) CXCR4-based T-tropic viral entry inhibition that maintains native chemokine ligand binding. This discovery identifies important tool compounds for studying viral infectivity and prototype agents that block HIV-1 entry through dual chemokine receptor ligation.
CiteXplore: 26191361
DOI: 10.1021/acsmedchemlett.5b00036
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