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.

A library of 1,2,3-triazole-substituted oleanolic acid derivatives as anticancer agents: design, synthesis, and biological evaluation

2015 ◽  
Vol 13 (5) ◽  
pp. 1507-1514 ◽  
Author(s):  
Gaofei Wei ◽  
Weijing Luan ◽  
Shuai Wang ◽  
Shanshan Cui ◽  
Fengran Li ◽  
...  
Keyword(s):  
Oleanolic Acid ◽  
Anticancer Agents ◽  
Cycloaddition Reaction ◽  
Biological Evaluation ◽  
Dipolar Cycloaddition ◽  
Design Synthesis ◽  
Triazole Derivatives ◽  
Synthesis And Biological Evaluation

A series of novel oleanolic acid coupled 1,2,3-triazole derivatives have been designed and synthesized by employing a Cu(i) catalyzed Huisgen 1,3-dipolar cycloaddition reaction.

Design, Synthesis, and Biological Evaluation of New Indole-Acrylamide-1,2,3-Triazole Derivatives as Potential α-Glucosidase Inhibitors

2020 ◽  
pp. 1-9
Author(s):  
Seyed Esmaeil Sadat-Ebrahimi ◽  
Hiva Babania ◽  
Maryam Mohammadi-Khanaposhtani ◽  
Mohammad Sadegh Asgari ◽  
Somayeh Mojtabavi ◽  
...  
Keyword(s):  
Biological Evaluation ◽  
Design Synthesis ◽  
Triazole Derivatives ◽  
Glucosidase 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.

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