| Literature DB >> 21353550 |
Xianfeng Li1, Suoming Zhang, Yong-Kang Zhang, Yang Liu, Charles Z Ding, Yasheen Zhou, Jacob J Plattner, Stephen J Baker, Wei Bu, Liang Liu, Wieslaw M Kazmierski, Maosheng Duan, Richard M Grimes, Lois L Wright, Gary K Smith, Richard L Jarvest, Jing-Jing Ji, Joel P Cooper, Matthew D Tallant, Renae M Crosby, Katrina Creech, Zhi-Jie Ni, Wuxin Zou, Jon Wright.
Abstract
We have synthesized and evaluated a new series of acyclic P4-benzoxaborole-based HCV NS3 protease inhibitors. Structure-activity relationships were investigated, leading to the identification of compounds 5g and 17 with low nanomolar potency in the enzymatic and cell-based replicon assay. The linker-truncated compound 5j was found to exhibit improved absorption and oral bioavailability in rats, suggesting that further reduction of molecular weight and polar surface area could result in improved drug-like properties of this novel series.Entities:
Mesh：
Substances：
Year: 2011 PMID： 21353550 DOI： 10.1016/j.bmcl.2011.02.006
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823