2. Academic Validation
  3. Amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines as CXCR4 antagonists with potent activity against HIV-1

Amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines as CXCR4 antagonists with potent activity against HIV-1

  • Bioorg Med Chem Lett. 2009 Sep 1;19(17):5048-52. doi: 10.1016/j.bmcl.2009.07.037.
Kristjan S Gudmundsson 1,  Paul R Sebahar,  Leah D'Aurora Richardson,  John F Miller,  Elizabeth M Turner,  John G Catalano,  Andrew Spaltenstein,  Wendell Lawrence,  Michael Thomson,  Stephen Jenkinson
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Metabolic and Virology Center of Excellence for Drug Discovery, GlaxoSmithKline Research & Development, Five Moore Drive, Research Triangle Park, NC 27709-3398, USA. [email protected]
PMID: 19640718 DOI: 10.1016/j.bmcl.2009.07.037
Abstract

Several novel amine substituted N-(1H-benzimidazol-2ylmethyl)-5,6,7,8-tetrahydro-8-quinolinamines were synthesized which had potent activity against HIV-1. The synthetic approaches adopted allowed for variation of the substitution pattern and resulting changes in Antiviral activity are highlighted. This led to the identification of compounds with low and sub-nanomolar anti-HIV-1 activity.

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