Literature DB >> 29908442

Benzomorphan skeleton, a versatile scaffold for different targets: A comprehensive review.

Rita Turnaturi1, Lucia Montenegro2, Agostino Marrazzo3, Rosalba Parenti4, Lorella Pasquinucci3, Carmela Parenti5.   

Abstract

Despite the fact that the benzomorphan skeleton has mainly been employed in medicinal chemistry for the development of opioid analgesics, it is a versatile structure. Its stereochemistry, as well as opportune modifications at the phenolic hydroxyl group and at the basic nitrogen, play a pivotal role addressing the benzomorphan-based compounds to a specific target. In this review, we describe the structure activity-relationships (SARs) of benzomorphan-based compounds acting at sigma 1 receptor (σ1R), sigma 2 receptor (σ2R), voltage-dependent sodium channel, N-Methyl-d-Aspartate (NMDA) receptor-channel complex and other targets. Collectively, the SARs data have highlighted that the benzomorphan nucleus could be regarded as a useful template for the synthesis of drug candidates for different targets.
Copyright © 2018 Elsevier Masson SAS. All rights reserved.

Entities:  

Keywords:  Antiviral; NMDA; Neuroprotection; Opioid; Sigma receptor; Sodium channel

Mesh:

Substances:

Year:  2018        PMID: 29908442     DOI: 10.1016/j.ejmech.2018.06.017

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN: 0223-5234            Impact factor:   6.514


  3 in total

1.  Novel N-Substituted Benzomorphan-Based Compounds: From MOR-Agonist/DOR-Antagonist to Biased/Unbiased MOR Agonists.

Authors:  Lorella Pasquinucci; Carmela Parenti; M Carmen Ruiz-Cantero; Zafiroula Georgoussi; Paschalina Pallaki; Enrique J Cobos; Emanuele Amata; Agostino Marrazzo; Orazio Prezzavento; Emanuela Arena; Maria Dichiara; Loredana Salerno; Rita Turnaturi
Journal:  ACS Med Chem Lett       Date:  2020-01-28       Impact factor: 4.345

2.  Structural and Molecular Insight into Piperazine and Piperidine Derivatives as Histamine H3 and Sigma-1 Receptor Antagonists with Promising Antinociceptive Properties.

Authors:  Katarzyna Szczepańska; Sabina Podlewska; Maria Dichiara; Davide Gentile; Vincenzo Patamia; Niklas Rosier; Denise Mönnich; Ma Carmen Ruiz Cantero; Tadeusz Karcz; Dorota Łażewska; Agata Siwek; Steffen Pockes; Enrique J Cobos; Agostino Marrazzo; Holger Stark; Antonio Rescifina; Andrzej J Bojarski; Emanuele Amata; Katarzyna Kieć-Kononowicz
Journal:  ACS Chem Neurosci       Date:  2021-12-15       Impact factor: 4.418

3.  Novel N-normetazocine Derivatives with Opioid Agonist/Sigma-1 Receptor Antagonist Profile as Potential Analgesics in Inflammatory Pain.

Authors:  Rita Turnaturi; Santina Chiechio; Lorella Pasquinucci; Salvatore Spoto; Giuliana Costanzo; Maria Dichiara; Silvia Piana; Margherita Grasso; Emanuele Amata; Agostino Marrazzo; Carmela Parenti
Journal:  Molecules       Date:  2022-08-12       Impact factor: 4.927

  3 in total

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