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Abstract
We have recently reported that N-alkyl and N-acyl naltrindole (NTI) derivatives showed activities for the δ opioid receptor (DOR) ranging widely from full inverse agonists to full agonists. We newly designed sulfonamide-type NTI derivatives in order to investigate the effects of the N-substituent on the functional activities because the side chain and S=O part in the sulfonamide moiety located in spatially different positions compared with those in the alkylamine and amide moieties. Among the tested compounds, cyclopropylsulfonamide 9f (SYK-839) was the most potent full inverse agonist for the DOR, whereas phenethylsulfonamide 9e (SYK-901) showed full DOR agonist activity with moderate potency. These NTI derivatives are expected to be useful compounds for investigation of the molecular mechanism inducing these functional activities.
Highlights
The ligands interacting with receptors have long been classified into agonists and antagonists.it is widely accepted that there are agonists, neutral antagonists, and inverse agonists.Agonists interact with receptors in the active state to induce physiological activities, whereas inverse agonists, which bind to receptors in the inactive state, can suppress the constitutive activities of receptors
It is evoked the idea that the C=O moiety might compensate for the interaction between the protonated interesting to consider whether the moieties in sulfonamide-type derivatives, which were nitrogen and the receptor
We previously reported the synthesis of of 5
Summary
The ligands interacting with receptors have long been classified into agonists and antagonists. 1) are expected to be useful compounds to elucidate the binding modes of these structures and to on the conformational changes of the DOR that induce functional activities agonists to investigate the effects of the N-substituents on the conformational changes from of theinverse. We were interested in sulfonamideorientation of the sidechain, property of the nitrogen atom the sulfonamide type NTI derivatives, becausebut notalso onlythe thechemical orientation of the sidechain, and theinchemical property moiety differs from those of tertiary alkyl or amide-type compounds. We will report the of the nitrogen atom in the sulfonamide moiety differs from those of tertiary alkyl or amide-type synthesis of sulfonamide-type derivatives and the evaluation of their opioid activities.
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