Bioorganic and Medicinal Chemistry Letters p. 799 - 804 (1998)
Update date:2022-07-30
Topics:
Kubota, Hitoshi
Rothman, Richard B.
Dersch, Chris
McCullough, Karen
Pinto, Julia
Rice, Kenner C.
The 3-unsubstituted and substituted analogs of naltrindole (NTI) were synthesized using palladium-catalyzed transformations, and their binding affinity to opioid receptors was determined. Although the 3-desoxy analog showed comparable δ selectivity with that of NTI, all of the novel compounds possessed low affinity for δ receptors indicating the important role of the 3-oxygen atom of NTI for interaction with δ-opioid receptors.
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