Synthesis and Pharmacological Evaluation of 5-Pyrrolidinylquinoxalines as a Novel Class of Peripherally Restricted κ-Opioid Receptor Agonists

2014 ◽  
Vol 57 (15) ◽  
pp. 6845-6860 ◽  
Author(s):  
Christian Bourgeois ◽  
Elena Werfel ◽  
Fabian Galla ◽  
Kirstin Lehmkuhl ◽  
Héctor Torres-Gómez ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Receptor Agonists ◽  
Pharmacological Evaluation ◽  
Opioid Receptor Agonists

Synthesis and pharmacological evaluation of conformationally restricted κ-opioid receptor agonists

MedChemComm ◽  
2016 ◽  
Vol 7 (12) ◽  
pp. 2368-2380 ◽  
Author(s):  
Yvonne Wenker ◽  
Michael Soeberdt ◽  
Constantin Daniliuc ◽  
Sonja Ständer ◽  
Dirk Schepmann ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Fine Tuning ◽  
Receptor Agonists ◽  
Conformationally Restricted ◽  
Pharmacological Evaluation ◽  
Pharmacokinetic Properties ◽  
Opioid Receptor Agonists

Additional N- and O-atoms in the bicyclic scaffold increase polarity and allow fine tuning of pharmacodynamic and pharmacokinetic properties of novel κ agonists.

scholarly journals Enantiomerically Pure Quinoline‐Based κ‐Opioid Receptor Agonists: Chemoenzymatic Synthesis and Pharmacological Evaluation

ChemMedChem ◽  
2020 ◽  
Vol 15 (15) ◽  
pp. 1408-1420
Author(s):  
Benedikt Martin ◽  
Dirk Schepmann ◽  
Freddy A. Bernal ◽  
Thomas J. Schmidt ◽  
Tao Che ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Chemoenzymatic Synthesis ◽  
Enantiomerically Pure ◽  
Receptor Agonists ◽  
Pharmacological Evaluation ◽  
Opioid Receptor Agonists

scholarly journals Cover Feature: Synthesis and Assessment of Fused β‐Carboline Derivatives as Kappa Opioid Receptor Agonists (12/2021)

ChemMedChem ◽  
2021 ◽  
Vol 16 (12) ◽  
pp. 1834-1834
Author(s):  
Veena D. Yadav ◽  
Lalan Kumar ◽  
Poonam Kumari ◽  
Sakesh Kumar ◽  
Maninder Singh ◽  
...  
Keyword(s):  
Opioid Receptor ◽  
Kappa Opioid Receptor ◽  
Kappa Opioid ◽  
Receptor Agonists ◽  
Opioid Receptor Agonists
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