Synthesis and biological activity of 3-substituted 3-desoxynaltrindole derivatives

DOI: 10.1016/S0960-894X(98)00105-X

Source and publish data:

Bioorganic and Medicinal Chemistry Letters p. 799 - 804 (1998)

Update date:2022-07-30

Topics:

Authors:

Kubota, Hitoshi

Rothman, Richard B.

Dersch, Chris

McCullough, Karen

Pinto, Julia

Rice, Kenner C.

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Article abstract of DOI:10.1016/S0960-894X(98)00105-X

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.

Full text of DOI:10.1016/S0960-894X(98)00105-X

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