2. Academic Validation
  3. Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors

Synthesis and biological evaluation of novel amprenavir-based P1-substituted bi-aryl derivatives as ultra-potent HIV-1 protease inhibitors

  • Bioorg Med Chem Lett. 2012 Mar 1;22(5):1976-9. doi: 10.1016/j.bmcl.2012.01.037.
Jianwei Yan 1,  Ning Huang,  Shukun Li,  Liu-Meng Yang,  Weiqiang Xing,  Yong-Tang Zheng,  Youhong Hu
Affiliations

Affiliation

  • 1 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Shanghai 201203, China.
PMID: 22306123 DOI: 10.1016/j.bmcl.2012.01.037
Abstract

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.

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