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  • Title: Discovery of N-benzyl-N'-(4-pipyridinyl)urea CCR5 antagonists as anti-HIV-1 agents (II): modification of the acyl portion.
    Author: Duan M, Peckham J, Edelstein M, Ferris R, Kazmierski WM, Spaltenstein A, Wheelan P, Xiong Z.
    Journal: Bioorg Med Chem Lett; 2010 Dec 15; 20(24):7401-4. PubMed ID: 21055933.
    Abstract:
    Modification of the acyl moiety in the CCR5 lead molecule 2 led to identification of several new classes of CCR5 antagonists. Antiviral activity and pharmacokinetic properties of the synthesized compounds were evaluated. Structure-activity relationship (SAR) derived from these studies further guided the optimization efforts, ultimately leading to the discovery of 36 with an acceptable drug-like profile.
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