Benzomorphan scaffold for opioid analgesics and pharmacological tools development: A comprehensive review

European Journal of Medicinal Chemistry
Rita TurnaturiL Pasquinucci

Abstract

Benzomorphan, derived by morphine skeleton simplification, has been the subject of exploration in medicinal chemistry for the development of new drugs and pharmacological tools to explore opioid pharmacology in vitro and in vivo. Building upon these evidences, the design and synthesis of benzomorphan-based compounds, appropriately modified at the basic nitrogen and/or the phenolic hydroxyl (8-OH) group, represent a valid and versatile strategy to obtain analgesics. In this review, to improve the body of information in this field, we report structure activity-relationships (SARs) of benzomorphan-based compounds analysing data literature of last 25 years. Collectively, SARs data highlighted that the benzomorphan nucleus represents a template in the achievement of a specific functional profile, by modifying N-substituent or 8-OH group.

Citations

Mar 17, 2018·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Rita TurnaturiLorella Pasquinucci
Feb 29, 2020·Archives of Toxicology·Svetoslav SlavovRichard D Beger
Nov 6, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Helmut SchmidhammerMariana Spetea
Jul 20, 2021·Chirality·José A GálvezMaría D Díaz-de-Villegas
Jul 25, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Lorella PasquinucciRita Turnaturi
May 22, 2020·ACS Medicinal Chemistry Letters·Lorella PasquinucciRita Turnaturi

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