Synthesis and biological evaluation of potential bisubstrate inhibitors of protein farnesyltransferase. Design and synthesis of functionalized imidazoles

2007 ◽  
Vol 5 (20) ◽  
pp. 3299 ◽  
Author(s):  
Renata Marcia de Figueiredo ◽  
Laëtitia Coudray ◽  
Joëlle Dubois
Keyword(s):  
Biological Evaluation ◽  
Protein Farnesyltransferase ◽  
Design And Synthesis ◽  
Bisubstrate Inhibitors ◽  
Synthesis And Biological Evaluation

Synthesis and Biological Evaluation of Potent Bisubstrate Inhibitors of the Enzyme CatecholO-Methyltransferase (COMT) Lacking a Nitro Group

2006 ◽  
Vol 89 (9) ◽  
pp. 1856-1887 ◽  
Author(s):  
Ralph Paulini ◽  
Christian Lerner ◽  
François Diederich ◽  
Roland Jakob-Roetne ◽  
Gerhard Zürcher ◽  
...  
Keyword(s):  
Nitro Group ◽  
Biological Evaluation ◽  
Bisubstrate Inhibitors ◽  
Synthesis And Biological Evaluation

scholarly journals Design, Synthesis and Biological Evaluation of Novel SARS-CoV-2 3CLpro Covalent Inhibitors

2021 ◽  
Author(s):  
Julia Stille ◽  
Jevgenijs Tjutrins ◽  
Guanyu Wang ◽  
Felipe A. Venegas ◽  
Christopher Hennecker ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Antiviral Drugs ◽  
Design Synthesis ◽  
Design And Synthesis ◽  
Promising Target ◽  
Starting Point ◽  
Covalent Inhibitors ◽  
Screening Platform ◽  
And Function ◽  
Synthesis And Biological Evaluation

Severe diseases such as the ongoing COVID-19 pandemic, as well as the previous SARS and MERS outbreaks, are the result of coronavirus infections and have demonstrated the urgent need for antiviral drugs to combat these deadly viruses. Due to its essential role in viral replication and function, 3CLpro> has been identified as a promising target for the development of antiviral drugs. Previously reported SARS-CoV 3CLpro non-covalent inhibitors were used as a starting point for the development of covalent inhibitors of SARS-CoV-2 3CLpro. We report herein our efforts in design and synthesis which led to submicromolar covalent inhibitors when the enzymatic activity of the viral protease was used as a screening platform.

scholarly journals Design, Synthesis and Biological Evaluation of Novel SARS-CoV-2 3CLpro Covalent Inhibitors

2020 ◽  
Author(s):  
Julia Stille ◽  
Jevgenijs Tjutrins ◽  
Guanyu Wang ◽  
Felipe A. Venegas ◽  
Christopher Hennecker ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Antiviral Drugs ◽  
Design Synthesis ◽  
Design And Synthesis ◽  
Promising Target ◽  
Starting Point ◽  
Covalent Inhibitors ◽  
Screening Platform ◽  
And Function ◽  
Synthesis And Biological Evaluation

Severe diseases such as the ongoing COVID-19 pandemic, as well as the previous SARS and MERS outbreaks, are the result of coronavirus infections and have demonstrated the urgent need for antiviral drugs to combat these deadly viruses. Due to its essential role in viral replication and function, 3CLpro has been identified as a promising target for the development of antiviral drugs. Previously reported SARS-CoV 3CLpro non-covalent inhibitors were used as a starting point for the development of covalent inhibitors of SARS-CoV-2 3CLpro. We report herein our efforts in design and synthesis which led to submicromolar covalent inhibitors when the enzymatic activity of the viral protease was used as a screening platform.

scholarly journals Design, synthesis and biological evaluation of tacrine-1,2,3-triazole derivatives as potent cholinesterase inhibitors

MedChemComm ◽  
2018 ◽  
Vol 9 (1) ◽  
pp. 149-159 ◽  
Author(s):  
Gaochan Wu ◽  
Yun Gao ◽  
Dongwei Kang ◽  
Boshi Huang ◽  
Zhipeng Huo ◽  
...  
Keyword(s):  
Cholinesterase Inhibitors ◽  
Biological Evaluation ◽  
Dipolar Cycloaddition ◽  
Design Synthesis ◽  
Triazole Derivatives ◽  
Design And Synthesis ◽  
Cuaac Reaction ◽  
Synthesis And Biological Evaluation

We report herein the design and synthesis of a series of 11 novel tacrine-1,2,3-triazole derivatives via a Cu(i)-catalyzed alkyne–azide 1,3-dipolar cycloaddition (CuAAC) reaction.

scholarly journals Design, Synthesis and Biological Evaluation of Novel Anthraniloyl-AMP Mimics as PQS Biosynthesis Inhibitors Against Pseudomonas aeruginosa Resistance

Molecules ◽  
2020 ◽  
Vol 25 (13) ◽  
pp. 3103
Author(s):  
Shekh Sabir ◽  
Sujatha Subramoni ◽  
Theerthankar Das ◽  
David StC. Black ◽  
Scott A. Rice ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Biofilm Formation ◽  
Adenosine Monophosphate ◽  
Biological Evaluation ◽  
Bacterial Biofilms ◽  
Design Synthesis ◽  
Signaling Systems ◽  
Design And Synthesis ◽  
Bacterial Aggregation ◽  
Synthesis And Biological Evaluation

The Pseudomonas quinolone system (PQS) is one of the three major interconnected quorum sensing signaling systems in Pseudomonas aeruginosa. The virulence factors PQS and HHQ activate the transcription regulator PqsR (MvfR), which controls several activities in bacteria, including biofilm formation and upregulation of PQS biosynthesis. The enzyme anthraniloyl-CoA synthetase (PqsA) catalyzes the first and critical step in the biosynthesis of quinolones; therefore, it is an attractive target for the development of anti-virulence therapeutics against Pseudomonas resistance. Herein, we report the design and synthesis of novel triazole nucleoside-based anthraniloyl- adenosine monophosphate (AMP) mimics. These analogues had a major impact on the morphology of bacterial biofilms and caused significant reduction in bacterial aggregation and population density. However, the compounds showed only limited inhibition of PQS and did not exhibit any effect on pyocyanin production.

Synthesis and biological evaluation of a new series of N-ylides as protein farnesyltransferase inhibitors

2013 ◽  
Vol 23 (21) ◽  
pp. 5887-5892 ◽  
Author(s):  
Cristina-Maria Abuhaie ◽  
Alina Ghinet ◽  
Amaury Farce ◽  
Joëlle Dubois ◽  
Benoît Rigo ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Farnesyltransferase Inhibitors ◽  
Protein Farnesyltransferase ◽  
Synthesis And Biological Evaluation
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