December 1, 2025ChemistrySelectOpen Access

New, Melatonin Receptors Selective 2‐Phenyl/C5‐Substituted Ν ‐Acylated Tryptamines

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Discussion

Indole analogues demonstrate selectivity and affinity for MT2 receptors, suggesting potential therapeutic applications.

Higher selectivity observed for MT2 receptors, with compounds 8a-10a displaying significant binding affinity, correlating to distinct chemical modifications.
Compounds showed the best efficacy at the MT2 receptor, with notable modifications impacting affinity and selectivity across the series.
Synthesis involved cyclization and functionalization of 2-phenylindoles to improve receptor targeting through specific structural changes.
Study highlights the importance of C3-side chain length and C2 phenyl substitution in developing selective melatonin receptor agonists.

Sakellaropoulou et al. (2025) studied this question.

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