Divergent synthesis and biological evaluation of 2-(trifluoromethyl)pyridines as virulence-attenuating inverse agonists targeting PqsR

2021 ◽  
Vol 226 ◽  
pp. 113797
Author(s):  
Christian Schütz ◽  
Amir Hodzic ◽  
Mostafa Hamed ◽  
Ahmed S. Abdelsamie ◽  
Andreas M. Kany ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Inverse Agonists ◽  
Synthesis And Biological Evaluation

Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation. Part 1

2010 ◽  
Vol 20 (4) ◽  
pp. 1448-1452 ◽  
Author(s):  
John S. Debenham ◽  
Christina B. Madsen-Duggan ◽  
Richard B. Toupence ◽  
Thomas F. Walsh ◽  
Junying Wang ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Inverse Agonists ◽  
Cannabinoid 1 Receptor ◽  
Synthesis And Biological Evaluation

scholarly journals Piperazine- and Piperidine-Containing Thiazolo[5,4-d]pyrimidine Derivatives as New Potent and Selective Adenosine A2A Receptor Inverse Agonists

2020 ◽  
Vol 13 (8) ◽  
pp. 161
Author(s):  
Flavia Varano ◽  
Daniela Catarzi ◽  
Erica Vigiani ◽  
Fabrizio Vincenzi ◽  
Silvia Pasquini ◽  
...  
Keyword(s):  
Tumor Development ◽  
Biological Evaluation ◽  
Pyrimidine Derivatives ◽  
A2a Adenosine Receptor ◽  
Inverse Agonists ◽  
A2a Receptor ◽  
Potential Therapeutic Role ◽  
Adenosine A2a ◽  
Synthesis And Biological Evaluation

The therapeutic use of A2A adenosine receptor (AR) antagonists for the treatment of neurodegenerative disorders, such as Parkinson and Alzheimer diseases, is a very promising approach. Moreover, the potential therapeutic role of A2A AR antagonists to avoid both immunoescaping of tumor cells and tumor development is well documented. Herein, we report on the synthesis and biological evaluation of a new set of piperazine- and piperidine- containing 7-amino-2-(furan-2-yl)thiazolo[5,4-d]pyrimidine derivatives designed as human A2A AR antagonists/inverse agonists. Binding and potency data indicated that a good number of potent and selective hA2A AR inverse agonists were found. Amongst them, the 2-(furan-2-yl)-N5-(2-(4-phenylpiperazin-1-yl)ethyl)thiazolo[5,4-d]pyrimidine-5,7-diamine 11 exhibited the highest A2A AR binding affinity (Ki = 8.62 nM) as well as inverse agonist potency (IC50 = 7.42 nM). In addition, bioinformatics prediction using the web tool SwissADME revealed that 8, 11, and 19 possessed good drug-likeness profiles.

Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation

2009 ◽  
Vol 19 (9) ◽  
pp. 2591-2594 ◽  
Author(s):  
John S. Debenham ◽  
Christina B. Madsen-Duggan ◽  
Junying Wang ◽  
Xinchun Tong ◽  
Julie Lao ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Inverse Agonists ◽  
Cannabinoid 1 Receptor ◽  
Synthesis And Biological Evaluation

Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine RORγt Inverse Agonists

ChemMedChem ◽  
2016 ◽  
Vol 11 (24) ◽  
pp. 2640-2648 ◽  
Author(s):  
Samuel Hintermann ◽  
Christine Guntermann ◽  
Henri Mattes ◽  
David A. Carcache ◽  
Juergen Wagner ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Inverse Agonists ◽  
Synthesis And Biological Evaluation
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