BIOMAT Database Logo BIOMAT Database Logo

[Design, synthesis and evaluation of 5-aminobenzimidazolone derivatives as acetylcholinesterase inhibitors]. 2015

Zheng-yue Ma, and Jun-jie Li, and Jun-tao Chen, and Yun-feng Tian, and Ying-chao Zhang, and Yu-qing Cao

The target compounds were prepared from 5-aminobenzimidazolone by two steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The AChE inhibitory activity of compound 4d is the best of them, and its IC50 value is equal to 7.2 μmol·L(-1), which is better than that of rivastigmine; moreover the 4d had no inhibitory activities to BuChE. Therefore, the inhibitory activities of 5-aminobenzimidazolone derivatives to acetylcholinesterase are worth further researching.

UI MeSH Term Description Entries
D002800 Cholinesterase Inhibitors Drugs that inhibit cholinesterases. The neurotransmitter ACETYLCHOLINE is rapidly hydrolyzed, and thereby inactivated, by cholinesterases. When cholinesterases are inhibited, the action of endogenously released acetylcholine at cholinergic synapses is potentiated. Cholinesterase inhibitors are widely used clinically for their potentiation of cholinergic inputs to the gastrointestinal tract and urinary bladder, the eye, and skeletal muscles; they are also used for their effects on the heart and the central nervous system. Acetylcholinesterase Inhibitor,Acetylcholinesterase Inhibitors,Anti-Cholinesterase,Anticholinesterase,Anticholinesterase Agent,Anticholinesterase Agents,Anticholinesterase Drug,Cholinesterase Inhibitor,Anti-Cholinesterases,Anticholinesterase Drugs,Anticholinesterases,Cholinesterase Inhibitors, Irreversible,Cholinesterase Inhibitors, Reversible,Agent, Anticholinesterase,Agents, Anticholinesterase,Anti Cholinesterase,Anti Cholinesterases,Drug, Anticholinesterase,Drugs, Anticholinesterase,Inhibitor, Acetylcholinesterase,Inhibitor, Cholinesterase,Inhibitors, Acetylcholinesterase,Inhibitors, Cholinesterase,Inhibitors, Irreversible Cholinesterase,Inhibitors, Reversible Cholinesterase,Irreversible Cholinesterase Inhibitors,Reversible Cholinesterase Inhibitors
D000068836 Rivastigmine A carbamate-derived reversible CHOLINESTERASE INHIBITOR that is selective for the CENTRAL NERVOUS SYSTEM and is used for the treatment of DEMENTIA in ALZHEIMER DISEASE and PARKINSON DISEASE. (S)-N-Ethyl-3-((1-dimethyl-amino)ethyl)-N-methylphenylcarbamate,ENA 713,ENA-713,Exelon,Rivastigmine Hydrogen Tartrate,RivastigmineTartrate,SDZ ENA 713,713, ENA,713, SDZ ENA,ENA 713, SDZ,ENA713,Hydrogen Tartrate, Rivastigmine,Tartrate, Rivastigmine Hydrogen
D000110 Acetylcholinesterase An enzyme that catalyzes the hydrolysis of ACETYLCHOLINE to CHOLINE and acetate. In the CNS, this enzyme plays a role in the function of peripheral neuromuscular junctions. EC 3.1.1.7. Acetylcholine Hydrolase,Acetylthiocholinesterase,Hydrolase, Acetylcholine
D001562 Benzimidazoles Compounds with a BENZENE fused to IMIDAZOLES.
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D015195 Drug Design The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include PHARMACOKINETICS, dosage analysis, or drug administration analysis. Computer-Aided Drug Design,Computerized Drug Design,Drug Modeling,Pharmaceutical Design,Computer Aided Drug Design,Computer-Aided Drug Designs,Computerized Drug Designs,Design, Pharmaceutical,Drug Design, Computer-Aided,Drug Design, Computerized,Drug Designs,Drug Modelings,Pharmaceutical Designs
D048448 Phenylcarbamates Phenyl esters of carbamic acid or of N-substituted carbamic acids. Structures are similar to PHENYLUREA COMPOUNDS with a carbamate in place of the urea. Phenyl-Carbamates,Phenyl Carbamates

Related Publications

Zheng-yue Ma, and Jun-jie Li, and Jun-tao Chen, and Yun-feng Tian, and Ying-chao Zhang, and Yu-qing Cao
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors.
February 2009, European journal of medicinal chemistry,
Zheng-yue Ma, and Jun-jie Li, and Jun-tao Chen, and Yun-feng Tian, and Ying-chao Zhang, and Yu-qing Cao
Design, synthesis and pharmacological evaluation of chalcone derivatives as acetylcholinesterase inhibitors.
November 2014, Bioorganic & medicinal chemistry,
Zheng-yue Ma, and Jun-jie Li, and Jun-tao Chen, and Yun-feng Tian, and Ying-chao Zhang, and Yu-qing Cao
Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors.
March 2009, European journal of medicinal chemistry,
Zheng-yue Ma, and Jun-jie Li, and Jun-tao Chen, and Yun-feng Tian, and Ying-chao Zhang, and Yu-qing Cao
Design, synthesis and evaluation of 2-(2-oxoethyl)pyrimidine-5-carboxamide derivatives as acetylcholinesterase inhibitors.
September 2022, Bioorganic & medicinal chemistry letters,
Zheng-yue Ma, and Jun-jie Li, and Jun-tao Chen, and Yun-feng Tian, and Ying-chao Zhang, and Yu-qing Cao
Design, synthesis and evaluation of isaindigotone derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors.
July 2008, Bioorganic & medicinal chemistry letters,
Zheng-yue Ma, and Jun-jie Li, and Jun-tao Chen, and Yun-feng Tian, and Ying-chao Zhang, and Yu-qing Cao
Design, synthesis, and biological evaluation of acetophenone derivatives as dual binding acetylcholinesterase inhibitors.
May 2013, Die Pharmazie,
Zheng-yue Ma, and Jun-jie Li, and Jun-tao Chen, and Yun-feng Tian, and Ying-chao Zhang, and Yu-qing Cao
Design, synthesis, and evaluation of indanone derivatives as acetylcholinesterase inhibitors and metal-chelating agents.
July 2012, Bioorganic & medicinal chemistry letters,
Zheng-yue Ma, and Jun-jie Li, and Jun-tao Chen, and Yun-feng Tian, and Ying-chao Zhang, and Yu-qing Cao
Design, synthesis, biological evaluation, and molecular modeling of coumarin-piperazine derivatives as acetylcholinesterase inhibitors.
November 2013, Archiv der Pharmazie,
Zheng-yue Ma, and Jun-jie Li, and Jun-tao Chen, and Yun-feng Tian, and Ying-chao Zhang, and Yu-qing Cao
Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.
September 2005, Bioorganic & medicinal chemistry letters,
Zheng-yue Ma, and Jun-jie Li, and Jun-tao Chen, and Yun-feng Tian, and Ying-chao Zhang, and Yu-qing Cao
Design, synthesis and evaluation of new 4-arylthiazole-2-amine derivatives as acetylcholinesterase inhibitors.
March 2020, Bioorganic & medicinal chemistry letters,
Copied contents to your clipboard!