2. Academic Validation
  3. Design, synthesis, and biological evaluations of novel quinolones as HIV-1 non-nucleoside reverse transcriptase inhibitors

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

Affiliation

  • 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.

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