Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV‑1 Protease Inhibitors
Posted on 2017-11-13 - 00:00
Using the HIV-1 protease binding
mode of MK-8718 and PL-100 as inspiration,
a novel aspartate binding bicyclic piperazine sulfonamide core was
designed and synthesized. The resulting HIV-1 protease inhibitor containing
this core showed an 60-fold increase in enzyme binding affinity and
a 10-fold increase in antiviral activity relative to MK-8718.
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Bungard, Christopher J.; Williams, Peter D.; Schulz, Jurgen; Wiscount, Catherine M.; Holloway, M. Katharine; Loughran, H. Marie; et al. (2017). Design and Synthesis of Piperazine Sulfonamide Cores Leading to Highly Potent HIV‑1 Protease Inhibitors. ACS Publications. Collection. https://doi.org/10.1021/acsmedchemlett.7b00386
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AUTHORS (29)
- CBChristopher J. BungardPWPeter D. WilliamsJSJurgen SchulzCWCatherine M. WiscountMHM. Katharine HollowayHLH. Marie LoughranJMJesse J. ManikowskiHSHua-Poo SuDBDavid J. BennettLCLehua ChangXCXin-Jie ChuACAlejandro CrespoMDMichael P. DwyerKKKartik KeertikarGMGregori J. MorrielloASAndrew W. StamfordSWSherman T. WaddellBZBin ZhongBHBin HuTJTao Ji
