N2-benzyloxycarbonylguan-9-yl acetic acid derivatives as HIV-1 reverse transcriptase non-nucleoside inhibitors with decreased loss of potency against common drug-resistance mutations

Kassim F. Adebambo, Samantha Zanoli, Michael G. Thomas, Reynel Cancio, Nicola M. Howarth, Giovanni Maga

Research output: Contribution to journalArticle

4 Citations (Scopus)

Abstract

(Chemical Equation Presented) Beating the RT mutants: A novel class of N2-Cbz-guan-9-yl acetic acid derivatives is endowed with anti-HIV-1 reverse transcriptase (RT) activity in the low micromolar range. These compounds have improved efficacy towards drug-resistant RT mutants relative to nevirapine and efavirenz. Their unique scaffold and interesting resistance profiles warrant further development. © 2007 Wiley-VCH Verlag GmbH & Co. KGaA.

Original languageEnglish
Pages (from-to)1405-1409
Number of pages5
JournalChemMedChem
Volume2
Issue number10
DOIs
Publication statusPublished - 8 Oct 2007

Keywords

  • Antiviral agents
  • Drug resistance
  • Kinetic analysis
  • NNRTIs
  • Slow binding

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