We recently reported the synthesis and pharmacological evaluation of an analogue of the kappa opioid receptor antagonist nor-BNI where its two phenolic OH groups were replaced by carboxamido groups (CONH2). As expected from our understanding of the SARs of other carboxamido-substituted natural product-derived opioids, the nor-BNI analogue had very low affinity for kappa and other opioid receptors. We now report our results where the carboxamido analogue 1  of another well know kappa antagonist GNTI (2  ) was made and found to have very high binding affinity [Ki = 0.032 nM] to the kappa receptor. (Supported by NIDA grants R01 DA012180 and K05-DA00360)

Divergent SAR for carboxamido-substituted kappa opioid receptor antagonists

243rd National Meeting (2012)

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