68280-18-2Relevant academic research and scientific papers
Multivalent butyrylcholinesterase inhibitor discovered by exploiting dynamic combinatorial chemistry
Zhao, Shuang,Xu, Jintao,Zhang, Shixin,Han, Maochun,Wu, Yao,Li, Yusi,Hu, Lei
, (2021)
In this study, we report the generation of a polymer-based dynamic combinatorial library (DCL) incorporating exchangeable side chains using acylhydrazone formation reaction. In combination with tetrameric butyrylcholinesterase (BChE), the most potent binding side chain was identified, and the information obtained was further used for the synthesis of a multivalent BChE inhibitor. In the in vitro biological evaluation, this multivalent inhibitor exhibited not only better inhibitory effect than the commercial reference but also high selectivity on BChE over acetylcholinesterase (AChE).
Structure–activity relationship investigation of benzamide and picolinamide derivatives containing dimethylamine side chain as acetylcholinesterase inhibitors
Gao, Xiao-hui,Liu, Lin-bo,Liu, Hao-ran,Tang, Jing-jing,Kang, Lu,Wu, Hongnian,Cui, Peiwu,Yan, Jianye
, p. 110 - 114 (2017/12/01)
A series of benzamide and picolinamide derivatives containing dimethylamine side chain (4a–4c and 7a–7i) were synthesised and evaluated for acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activity in vitro. Structure–activity relat
N-Methylanilide and N-methylbenzamide derivatives as phosphodiesterase 10A (PDE10A) inhibitors
Kilburn, John Paul,Kehler, Jan,Langgard, Morten,Erichsen, Mette N.,Leth-Petersen, Sebastian,Larsen, Mogens,Christoffersen, Claus Tornby,Nielsen, Jacob
, p. 6053 - 6062 (2013/09/23)
PDE10A is a recently identified phosphodiesterase with a quite remarkable localization since the protein is abundant only in brain tissue. Based on this unique localization, research has focused extensively on using PDE10A modulators as a novel therapeutic approach for dysfunction in the basal ganglia circuit including Parkinson's disease, Huntington's disease, schizophrenia, addiction and obsessive compulsive disorder. Medicinal chemistry efforts identified the N-methyl-N-[4-(quinolin-2-ylmethoxy)-phenyl]-isonicotinamide (8) as a nanomolar PDE10A inhibitor. A subsequent Lead-optimization program identified analogous N-methylanilides and their corresponding N-methylbenzamides (29) as potent PDE10A inhibitors, concurrently some interesting and unexpected binding modes were identified.
