Random Chemistry as a New Tool for the Generation of Small Compound Libraries:  Development of a New Acetylcholinesterase Inhibitor

Journal of Medicinal Chemistry
2005.0

Abstract

Random chemistry, the serendipitous generation of small compound libraries by gamma-irradiation of source compounds, presents a methodology providing reassembled and rearranged structures. The gamma-irradiation was applied to generate new acetylcholinesterase (AChE) inhibitors. The bioassay-guided fractionation as a deconvolution strategy was employed to analyze gained product mixture. The structure of the new highly potent AChE inhibitor, 9-amino-5,6,7,8-tetrahydroacridin-4yl)methanol (1), was elucidated by NMR spectroscopy and ESI (tandem) mass spectrometry.

Knowledge Graph

Similar Paper

Random Chemistry as a New Tool for the Generation of Small Compound Libraries:  Development of a New Acetylcholinesterase Inhibitor
Journal of Medicinal Chemistry 2005.0
Synthesis, biological assessment and molecular modeling of 14-aryl-10,11,12,14-tetrahydro-9H-benzo[5,6]chromeno[2,3-b]quinolin-13-amines
Bioorganic & Medicinal Chemistry Letters 2011.0
Synthesis and AChE inhibitory activity of new chiral tetrahydroacridine analogues from terpenic cyclanones
European Journal of Medicinal Chemistry 2010.0
A Structure-Based Design Approach to the Development of Novel, Reversible AChE Inhibitors
Journal of Medicinal Chemistry 2001.0
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors
European Journal of Medicinal Chemistry 2009.0
Design, synthesis, docking study and biological evaluation of some novel tetrahydrochromeno [3′,4′:5,6]pyrano[2,3-b]quinolin-6(7H)-one derivatives against acetyl- and butyrylcholinesterase
European Journal of Medicinal Chemistry 2013.0
Acetylcholinesterase Inhibitors:  Synthesis and Structure−Activity Relationships of ω-[N-Methyl-N-(3-alkylcarbamoyloxyphenyl)- methyl]aminoalkoxyheteroaryl Derivatives
Journal of Medicinal Chemistry 1998.0
Discovery of new acetylcholinesterase inhibitors with small core structures through shape-based virtual screening
Bioorganic & Medicinal Chemistry Letters 2015.0
Acetylcholinesterase inhibitory dimeric indole derivatives from the marine actinomycetes Rubrobacter radiotolerans
Fitoterapia 2015.0
Dispiropyrrolidinyl-piperidone embedded indeno[1,2-b]quinoxaline heterocyclic hybrids: Synthesis, cholinesterase inhibitory activity and their molecular docking simulation
Bioorganic & Medicinal Chemistry 2019.0