Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors.
Jianwei Yan, Ning Huang, Shukun Li, Liu-Meng Yang, Weiqiang Xing, Yong-Tang Zheng, Youhong Hu
文献索引:Bioorg. Med. Chem. Lett. 5th ed., 22 , 1976-1979, (2012)
全文:HTML全文
摘要
A series of P1-substituted biaryl amprenavir derivatives was designed and synthesized. These compounds were evaluated for enzyme inhibition and antiviral activity in vitro. Several compounds showed highly efficient antiviral activity with EC(50) values down to 0.10nM, which are more potent than marketed HIV-1 protease inhibitors. Docking study indicated that 12c has similar binding mode to amprenavir with full occupancy in P1.Copyright © 2012 Elsevier Ltd. All rights reserved.
相关化合物
相关文献:
2014-12-01
[Eur. J. Drug Metab. Pharmacokinet. 39(4) , 263-76, (2014)]
2014-08-15
[J. Chromatogr. B. Analyt. Technol. Biomed. Life Sci. 965 , 244-53, (2014)]
2015-01-01
[PLoS ONE 10(2) , e0116886, (2015)]
2013-05-23
[J. Med. Chem. 56(10) , 4017-27, (2013)]
2012-01-01
[In Vivo 26(2) , 287-91, (2012)]