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ID: ALA5260834

Journal: Eur J Med Chem

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

Authors: Turnaturi R, Montenegro L, Marrazzo A, Parenti R, Pasquinucci L, Parenti C.

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.

CiteXplore: 29908442

DOI: 10.1016/j.ejmech.2018.06.017