Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors

  • Bioorg Med Chem. 2010 Jul 1;18(13):4601-5. doi: 10.1016/j.bmc.2010.05.036.
Yong-Hong Liang  1 ,  Qiu-Qin He ,  Zhao-Sen Zeng ,  Zhi-Qian Liu ,  Xiao-Qing Feng ,  Fen-Er Chen ,  Jan Balzarini ,  Christophe Pannecouque ,  Erik De Clercq
Affiliations
  • 1. Department of Chemistry, Fudan University, Shanghai 200433, People's Republic of China.
PMID: 20570527 DOI: 10.1016/j.bmc.2010.05.036
Abstract

Nine newly 6-cyano-2-naphthyl substituted diarylpyrimidines (DAPY) were synthesized as non-nucleoside Reverse Transcriptase inhibitors on the basis of our previous work. The Antiviral and cytotoxicity evaluation indicated that these compounds displayed strong activity against wild-type HIV-1 at nanomolar concentrations with selectivity index SI greater than 23 779. The most active compounds 3c and 3e exhibited activity against the double mutant (103N+181C) strains at an EC₅₀ of 0.16 and 0.15 μM, and were more activity than that of efavirenz.