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• W3010712023 abstract "Abstract Annelated purinedione derivatives have been shown to act as possible multiple‐target ligands, addressing adenosine receptors and monoaminooxidases. In this study, based on our previous results, novel annelated pyrimido‐ and diazepino[2,1‐ f ]purinedione derivatives were designed as dual‐target‐directed ligands combining A 2A adenosine receptor (AR) antagonistic activity with blocking monoamine oxidase B. A library of 19 novel compounds was synthesized and biologically evaluated in radioligand binding studies at AR subtypes and for their ability to inhibit MAO‐B. This allowed 9‐(2‐chloro‐6‐fluorobenzyl)‐3‐ethyl‐1‐methyl‐6,7,8,9‐tetrahydropyrimido[2,1‐ f ]purine‐2,4(1 H ,3 H )‐dione ( 13 e ; K i human A 2A AR: 264 nM and IC 50 human MAO‐B: 243 nM) to be identified as the most potent dual‐acting ligand from this series. ADMET parameters were estimated in vitro, and analysis of the structure‐activity relationships was complemented by molecular‐docking studies based on previously published X‐ray structures of the protein targets. Such dual‐acting ligands, by selectively blocking A 2A AR, accompanied by the inhibition of dopamine metabolizing enzyme MAO‐B, might provide symptomatic and neuroprotective effects in, among others, the treatment of Parkinson disease" @default.
• W3010712023 created "2020-03-23" @default.
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• W3010712023 date "2020-04-06" @default.
• W3010712023 modified "2023-10-16" @default.
• W3010712023 title "Novel, Dual Target‐Directed Annelated Xanthine Derivatives Acting on Adenosine Receptors and Monoamine Oxidase B" @default.
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• W3010712023 doi "https://doi.org/10.1002/cmdc.201900717" @default.
• W3010712023 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/32162782" @default.
• W3010712023 hasPublicationYear "2020" @default.
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