Bioorganic and Medicinal Chemistry
Bioorganic and Medicinal Chemistry
4 years ago

Antitrichomonal activity of δ opioid receptor antagonists, 7-benzylidenenaltrexone derivatives

Antitrichomonal activity of δ opioid receptor antagonists, 7-benzylidenenaltrexone derivatives
The 7-benzylidenenaltrexone (BNTX) derivatives 2a–v, 3a–c, 13a–c, and 14a were synthesized from naltrexone (1) and evaluated for their antitrichomonal activity. The structure-activity-relationship studies found that 4-iodo-BNTX (2g) showed the highest activity (IC50 =10.5µM) and the affinity for the opioid receptor was less important for antitrichomonal activity against Trichomonas vaginalis. The morphinan skeleton bearing both the double bond for a Michael acceptor and the phenolic hydroxy group would be a specific template for development of antitrichomonal agents. In addition, the mechanism of the antitrichomonal activity of the BNTX derivatives may differ from that of the standard drug, metronidazole.

Publisher URL: www.sciencedirect.com/science

DOI: S0968089617309860

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