Results 41 to 50 of about 1,008 (155)

Synthesis and Opioid Receptor Binding Affinities of 2-Substituted and 3-Aminomorphinans: Ligands for μ, κ, and δ Opioid Receptors

open access: yes, 2016
The phenolic group of the potent μ and κ opioid morphinan agonist/antagonists cyclorphan and butorphan was replaced by phenylamino and benzylamino groups including compounds with para-substituents in the benzene ring.
Jean M. Bidlack (1313052)   +4 more
core   +1 more source

High‐Throughput Drug Derivatization and Bioassay by Desorption Electrospray Ionization Mass Spectrometry

open access: yesChemPlusChem, Volume 90, Issue 6, June 2025.
Accelerated drug derivatization in microdroplets combined with high‐throughput desorption electrospray ionization mass spectrometry provides rapid reaction screening and label‐free bioassay results, which can expedite drug discovery. Adapting high‐throughput (HT) synthetic methods to the modification of drugs and to testing of their bioactivity should ...
Jyotirmoy Ghosh   +3 more
wiley   +1 more source

Characterization of Opioid Agonist Morphine Derivatives with Emphasis on Medicinal Chemistry

open access: yesChemMedChem, Volume 20, Issue 4, February 16, 2025.
The aim of synthesizing new opioid compounds is to produce drugs that are more potent, less addictive, and have fewer side effects, such as respiratory depression and constipation. To achieve this, we evaluated the basicity, lipophilicity, and permeability of 30 opioid compounds, including 11 newly synthesized ones, to better understand the ...
Alaa Malik   +7 more
wiley   +1 more source

Effect of a 6-Cyano Substituent in 14-Oxygenated N-Methylmorphinans on Opioid Receptor Binding and Antinociceptive Potency

open access: yes, 2016
In a continued effort to find new substitution patterns in morphinans that would produce strong antinociception while inducing lesser side effects, 4,5-oxygen bridge-opened 6-cyano-substituted N-methylmorphinans (1−3) were synthesized.
Mario D. Aceto (2384371)   +5 more
core   +1 more source

Phenol (bio)isosteres in drug design and development

open access: yesArchiv der Pharmazie, Volume 358, Issue 1, January 2025.
This review explores the pivotal role of phenol bioisosteres in drug design, highlighting their potential to overcome the limitations of phenolic compounds, such as poor bioavailability and rapid metabolism. By examining diverse bioisosteric replacements, from benzimidazolones to quinolinones, it is demonstrated how these modifications enhance drug ...
Calvin Dunker   +2 more
wiley   +1 more source

The Application of Metallated Enamines to the Synthesis of Morphine Alkaloids [PDF]

open access: yes, 1982
Metallated enamines have been used to prepare a number of morphine-based analgesics, including efficient entry to the 4a-phenylisoquinolines and morphinans.
Mitch, Charles Howard
core   +1 more source

Synthetic analgesics.

open access: yes, 1966
1. Diphenylpropylamines / by P. A. J. Janssen2A. Morphinans / by J. Hellerbach, O. Schnider, H. Besendorf e. a.2B. 6.7-Benzomorphans / by N. B. Eddy and E. L. May.Pt.
Janssen, Paul Adriaan Jan,Baron,1926-2003(viaf)32253568   +5 more
core  

Morphinan alkaloids from the leaves of Alphonsea cylindrica and their antibacterial properties

open access: yes, 2023
A phytochemical study has been carried out on CH (2) Cl (2) extract of Alphonsea cylindrica leaves, resulting in the isolation of three new morphinan alkaloids. They are kinomenine ( 1 ), N -methylkinomenine ( 2 ), and hydroxymethylkinomenine ( 3 ).
Tan, Siow-Ping   +4 more
core   +1 more source

Isoquinoline Alkaloids from the Leaves of Dehaasia Hainanensis

open access: yes, 2008
This study was aimed at investigating the alkaloids present in the leaves of Dehaasia hainanensis. Thirteen isoquinolines were isolated and characterized. Of these, four aporphines [(+)-laurolitsine, (+)-corydine, (+)- laurotetanine and (+)-lindcarpine],
CHEN, CHIEN-KUANG;CHEN, CHUNG-HSIUNG;LEE, SHOEI-SHENG   +1 more
core  

Formal Synthesis of (+/-) Morphine via an Oxy-cope/Claisen/Ene Reaction Cascade

open access: yes, 2012
For years now, opium alkaloids and morphinans have been attractive synthetic targets for numerous organic chemists due to their important biological activity and interesting molecular architecture.
Marcotte, Joel
core   +1 more source

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