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  • Title: Design, synthesis, and biological evaluation of novel 2-methylpiperazine derivatives as potent CCR5 antagonists.
    Author: Hu S, Wang Z, Hou T, Ma X, Li J, Liu T, Xie X, Hu Y.
    Journal: Bioorg Med Chem; 2015 Mar 01; 23(5):1157-68. PubMed ID: 25638498.
    Abstract:
    Three series of novel 2-methylpiperazine derivatives were designed and synthesized using a fragment-assembly strategy. Among them, six compounds (13, 16, 18, 22, 33, and 36) showed potent activity against CCR5 comparable to that of the positive control, maraviroc, in calcium mobilization assay. Moreover, some compounds were selected and further tested for their antiviral activity in HIV-1 single cycle assay. As a result, four compounds (13, 16, 33, and 36) showed antiviral activity at the nanomolar level. Additionally, the potent four compounds showed no cytotoxicity at a concentration of 10μM.
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