Design, synthesis, and biological evaluation of novel 4-hydroxypyrone derivatives as HIV-1 protease inhibitors

  • Bioorg Med Chem Lett. 2005 Jul 1;15(13):3257-62. doi: 10.1016/j.bmcl.2005.04.057.
Chun-Lai Sun  1 ,  Rui-Fang Pang ,  Hang Zhang ,  Ming Yang
Affiliations
  • 1. National Research Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100083, People's Republic of China.
PMID: 15923115 DOI: 10.1016/j.bmcl.2005.04.057
Abstract

Twenty-four 4-hydroxypyrone derivatives were synthesized with a facile synthetic method to develop novel HIV Protease Inhibitors. Most of them were shown to display good Antiviral activities in SIV-infected CEM cells. The introduction of alpha-naphthylmethyl group to C-6 of 5,6-dihydropyran-2-ones led to an effective Antiviral compound that showed an EC(50) value at 1.7 microM with a therapeutic index of 46.