What is the impact of the S=O moiety in sulfonamide-type naltrindole (NTI) derivatives on their functional activities?

Label:chem

Topic
A study explored the effects of different functional groups (e.g., C=O in amides, S=O in sulfonamides) on the functional activities of NTI derivatives. The orientation and chemical properties of these groups were hypothesized to influence receptor binding and activity.
Answer
The S=O moiety in sulfonamide-type NTI derivatives can function as a surrogate for the amide carbonyl moiety (C=O) in influencing functional activities. For instance, both amide-type (e.g., SYK-623) and sulfonamide-type (e.g., SYK-839) NTI derivatives with a cyclopropyl moiety exhibited inverse agonist activities. This suggests that the S=O group can compensate for the lack of a basic nitrogen atom, which is typically considered an essential pharmacophore in opioid ligands.
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