PMID- 29908442
OWN - NLM
STAT- MEDLINE
DCOM- 20180813
LR  - 20231213
IS  - 1768-3254 (Electronic)
IS  - 0223-5234 (Linking)
VI  - 155
DP  - 2018 Jul 15
TI  - Benzomorphan skeleton, a versatile scaffold for different targets: A 
      comprehensive review.
PG  - 492-502
LID - S0223-5234(18)30508-7 [pii]
LID - 10.1016/j.ejmech.2018.06.017 [doi]
AB  - 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 (sigma1R), sigma 2 receptor (sigma2R), 
      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.
CI  - Copyright (c) 2018 Elsevier Masson SAS. All rights reserved.
FAU - Turnaturi, Rita
AU  - Turnaturi R
AD  - Department of Drug Sciences, Medicinal Chemistry Section, University of Catania, 
      Viale A. Doria, 6, 95100, Catania, Italy. Electronic address: 
      rita.turnaturi@unict.it.
FAU - Montenegro, Lucia
AU  - Montenegro L
AD  - Department of Drug Sciences, Pharmaceutical Technology Section, University of 
      Catania, Viale A. Doria 6, 95125, Catania, Italy.
FAU - Marrazzo, Agostino
AU  - Marrazzo A
AD  - Department of Drug Sciences, Medicinal Chemistry Section, University of Catania, 
      Viale A. Doria, 6, 95100, Catania, Italy.
FAU - Parenti, Rosalba
AU  - Parenti R
AD  - Department of Biomedical and Biotechnological Sciences, Physiology Section, 
      University of Catania, Catania, Italy.
FAU - Pasquinucci, Lorella
AU  - Pasquinucci L
AD  - Department of Drug Sciences, Medicinal Chemistry Section, University of Catania, 
      Viale A. Doria, 6, 95100, Catania, Italy.
FAU - Parenti, Carmela
AU  - Parenti C
AD  - Department of Drug Sciences, Pharmacology Section, University of Catania, Viale 
      A. Doria, 6, 95100, Catania, Italy.
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20180607
PL  - France
TA  - Eur J Med Chem
JT  - European journal of medicinal chemistry
JID - 0420510
RN  - 0 (Analgesics, Opioid)
RN  - 0 (Benzomorphans)
RN  - 0 (NAV1.2 Voltage-Gated Sodium Channel)
RN  - 0 (Receptors, N-Methyl-D-Aspartate)
RN  - 0 (Receptors, sigma)
RN  - 0 (sigma-2 receptor)
SB  - IM
MH  - Analgesics, Opioid/chemical synthesis/chemistry/*pharmacology
MH  - Animals
MH  - Benzomorphans/chemical synthesis/chemistry/*pharmacology
MH  - Dose-Response Relationship, Drug
MH  - Humans
MH  - Molecular Structure
MH  - NAV1.2 Voltage-Gated Sodium Channel/*metabolism
MH  - Receptors, N-Methyl-D-Aspartate/*antagonists & inhibitors
MH  - Receptors, sigma/*antagonists & inhibitors
MH  - Structure-Activity Relationship
MH  - Sigma-1 Receptor
OTO - NOTNLM
OT  - Antiviral
OT  - NMDA
OT  - Neuroprotection
OT  - Opioid
OT  - Sigma receptor
OT  - Sodium channel
EDAT- 2018/06/17 06:00
MHDA- 2018/08/14 06:00
CRDT- 2018/06/17 06:00
PHST- 2017/12/11 00:00 [received]
PHST- 2018/03/23 00:00 [revised]
PHST- 2018/06/06 00:00 [accepted]
PHST- 2018/06/17 06:00 [pubmed]
PHST- 2018/08/14 06:00 [medline]
PHST- 2018/06/17 06:00 [entrez]
AID - S0223-5234(18)30508-7 [pii]
AID - 10.1016/j.ejmech.2018.06.017 [doi]
PST - ppublish
SO  - Eur J Med Chem. 2018 Jul 15;155:492-502. doi: 10.1016/j.ejmech.2018.06.017. Epub 
      2018 Jun 7.