Catechol Diether Analogues as Anti-HIV Agents

OCR Number: 
OCR 5753
Description: 
  • HIV reverse transcriptase (RT) remains a key molecular target and a cornerstone for HIV therapy.
  • Yale researchers have identified catechol diether derivatives as novel, potent anti-HIV agents.
  • These compounds are new non-nucleoside RT inhibitors (NNRTIs) that address continuing issues:
    • concerning the possible emergence of new viral strains
    • improved dosing
    • long-term tolerability
    • safety
  • OCR5753 is the most potent anti-HIV agent with activity towards wild-type HIV-1; it inhibited replication of HIV-1 in infected human T-cells with an EC50 of 55 picomolar.
  • OCR5753 is 10 times more potent than any NNRTI reported to date, including the newest FDA-approved drug, rilpivirine.
  • Development of the catechol diethers can be expected to yield compounds with high therapeutic potential with low toxicity leading to a very high therapeutic index.
Publications: 
Frey, K. M., Gray, W. T., Spasov, K. A., Bollini, M., Gallardo‐Macias, R., Jorgensen, W. L., & Anderson, K. S. (2014). Structure‐Based Evaluation of C5 Derivatives in the Catechol Diether Series Targeting HIV‐1 Reverse Transcriptase. Chemical biology & drug design, 83(5), 541-549. [Pub Med]
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