Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants.

doi:10.1021/jm201278q

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Article

Discovery of novel urea-based hepatitis C protease inhibitors with high potency against protease-inhibitor-resistant mutants.

Journal of medicinal chemistry - 12 Apr 2012

Kazmierski Wieslaw M, Hamatake Robert, Duan Maosheng, Wright Lois L, Smith Gary K, Jarvest Richard L, Ji Jing-Jing, Cooper Joel P, Tallant Matthew D, Crosby Renae M, Creech Katrina, Wang Amy, Li Xianfeng, Zhang Suoming, Zhang Yong-Kang, Liu Yang, Ding Charles Z, Zhou Yasheen, Plattner Jacob J, Baker Stephen J, Bu Wei, Liu Liang

Abstract excerpt

The macrocyclic urea 2, a byproduct in the synthesis of benzoxaborole 1, was identified to be a novel and potent HCV protease inhibitor. We further explored this motif by synthesizing additional urea-based inhibitors and by characterizing them in replicase HCV protease-resistant mutants assay. Several compounds, exemplified by 12, were found to be more potent in HCV replicon assays than leading second generation...

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PMID: 22471376
DOI: 10.1021/jm201278q

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