Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors

  • Bioorg Med Chem Lett. 2006 Aug 15;16(16):4246-51. doi: 10.1016/j.bmcl.2006.05.073.
David Ellis  1 ,  Kelli L Kuhen ,  Beth Anaclerio ,  Baogen Wu ,  Karen Wolff ,  Hong Yin ,  Badry Bursulaya ,  Jeremy Caldwell ,  Donald Karanewsky ,  Yun He
Affiliations
  • 1. Genomics Institute of the Novartis Research Foundation (GNF), San Diego, CA 92121, USA.
PMID: 16782337 DOI: 10.1016/j.bmcl.2006.05.073
Abstract

A novel series of quinolones was discovered as HIV-1 non-nucleoside Reverse Transcriptase inhibitors (NNRTIs) using a structure-based approach. The lead quinolones exhibited single digit nanomolar potency in the HIV-1 replication assays. The preliminary SAR of these quinolones was also established via systematic structural modifications. These novel and potent quinolones could serve as advanced leads for further optimization.