Synthesis and pharmacological evaluation of enantiomerically pure endo-configured KOR agonists with 2 azabicyclo[3.2.1]octane scaffold

2021 ◽  
Author(s):  
Bernhard Wuensch ◽  
Hendrik Jonas ◽  
Daniele Aiello ◽  
Bastian Frehland ◽  
Kirstin Lehmkuhl ◽  
...  
Keyword(s):  
Bioactive Conformation ◽  
Enantiomerically Pure ◽  
Conformationally Restricted ◽  
Pharmacological Evaluation

Conformationally restricted bicyclic KOR agonists 10 with an endo configured amino moiety were synthesized to analyze the bioactive conformation of conformationally flexible KOR agonists such as 2-5. A seven-step, chiral...

scholarly journals Conformationally restricted benzothienoazepine respiratory syncytial virus inhibitors: their synthesis, structural analysis and biological activities

MedChemComm ◽  
2018 ◽  
Vol 9 (3) ◽  
pp. 583-589 ◽  
Author(s):  
Euan A. F. Fordyce ◽  
S. Fraser Hunt ◽  
Damien Crepin ◽  
Stuart T. Onions ◽  
Guillaume F. Parra ◽  
...  
Keyword(s):  
Respiratory Syncytial Virus ◽  
Structural Analysis ◽  
Biological Activities ◽  
Bioactive Conformation ◽  
Conformationally Restricted ◽  
Syncytial Virus

Study of atropisomerism around RSV inhibitors allows identification of bioactive conformation.

scholarly journals Design, synthesis and pharmacological evaluation of conformationally restricted N-arylsulfonyl-3-aminoalkoxy indoles as a potential 5-HT6 receptor ligands

2011 ◽  
Vol 26 (3) ◽  
pp. 341-349 ◽  
Author(s):  
Ramakrishna V.S. Nirogia ◽  
Ramasastri Kambhampati ◽  
Anand V. Daulatabad ◽  
Parandhama Gudla ◽  
Mohammad Shaikh ◽  
...  
Keyword(s):  
Receptor Ligands ◽  
Design Synthesis ◽  
Conformationally Restricted ◽  
Pharmacological Evaluation

Synthesis and pharmacological evaluation of conformationally restricted phenothiazine analogues

1982 ◽  
Vol 25 (1) ◽  
pp. 5-9 ◽  
Author(s):  
Cor J. Grol ◽  
Durk Dijkstra ◽  
Wim Schunselaar ◽  
Ben H. C. Westerink ◽  
Arnold R. Martin
Keyword(s):  
Conformationally Restricted ◽  
Pharmacological Evaluation

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.

Sign in / Sign up

Export Citation Format

Share Document