Catechol Diether Analogues as Anti-HIV Agents

• 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.
• Issued US Patent & Reference