Matches in SemOpenAlex for { <https://semopenalex.org/work/W4386464370> ?p ?o ?g. }
- W4386464370 endingPage "13707" @default.
- W4386464370 startingPage "13707" @default.
- W4386464370 abstract "Chronic inflammation plays an important role in the development of neurodegenerative diseases, such as Parkinson’s disease (PD). In the present study, we synthesized 25 novel xanthine derivatives with variable substituents at the N1-, N3- and C8-position as adenosine receptor antagonists with potential anti-inflammatory activity. The compounds were investigated in radioligand binding studies at all four human adenosine receptor subtypes, A1, A2A, A2B and A3. Compounds showing nanomolar A2A and dual A1/A2A affinities were obtained. Three compounds, 19, 22 and 24, were selected for further studies. Docking and molecular dynamics simulation studies indicated binding poses and interactions within the orthosteric site of adenosine A1 and A2A receptors. In vitro studies confirmed the high metabolic stability of the compounds, and the absence of toxicity at concentrations of up to 12.5 µM in various cell lines (SH-SY5Y, HepG2 and BV2). Compounds 19 and 22 showed anti-inflammatory activity in vitro. In vivo studies in mice investigating carrageenan- and formalin-induced inflammation identified compound 24 as the most potent anti-inflammatory derivative. Future studies are warranted to further optimize the compounds and to explore their therapeutic potential in neurodegenerative diseases." @default.
- W4386464370 created "2023-09-06" @default.
- W4386464370 creator A5006200304 @default.
- W4386464370 creator A5008883576 @default.
- W4386464370 creator A5015494539 @default.
- W4386464370 creator A5017915434 @default.
- W4386464370 creator A5028320053 @default.
- W4386464370 creator A5034879913 @default.
- W4386464370 creator A5043866947 @default.
- W4386464370 creator A5055214820 @default.
- W4386464370 creator A5058209925 @default.
- W4386464370 creator A5067048725 @default.
- W4386464370 creator A5071406940 @default.
- W4386464370 creator A5073968516 @default.
- W4386464370 creator A5081072732 @default.
- W4386464370 creator A5083947932 @default.
- W4386464370 creator A5092824811 @default.
- W4386464370 date "2023-09-05" @default.
- W4386464370 modified "2023-10-17" @default.
- W4386464370 title "Anti-Inflammatory Activities of 8-Benzylaminoxanthines Showing High Adenosine A2A and Dual A1/A2A Receptor Affinity" @default.
- W4386464370 cites W149769536 @default.
- W4386464370 cites W1593543865 @default.
- W4386464370 cites W173818528 @default.
- W4386464370 cites W1970723735 @default.
- W4386464370 cites W1976499671 @default.
- W4386464370 cites W1978656200 @default.
- W4386464370 cites W1981819970 @default.
- W4386464370 cites W1985588649 @default.
- W4386464370 cites W1995850373 @default.
- W4386464370 cites W2015619448 @default.
- W4386464370 cites W2015811644 @default.
- W4386464370 cites W2020773808 @default.
- W4386464370 cites W2086476589 @default.
- W4386464370 cites W2089232549 @default.
- W4386464370 cites W2097775366 @default.
- W4386464370 cites W2129153475 @default.
- W4386464370 cites W2153228625 @default.
- W4386464370 cites W2262538191 @default.
- W4386464370 cites W2401188729 @default.
- W4386464370 cites W2596244944 @default.
- W4386464370 cites W2736015721 @default.
- W4386464370 cites W2790568799 @default.
- W4386464370 cites W2800384110 @default.
- W4386464370 cites W2881629212 @default.
- W4386464370 cites W2939604020 @default.
- W4386464370 cites W2954500169 @default.
- W4386464370 cites W2993082108 @default.
- W4386464370 cites W3006012411 @default.
- W4386464370 cites W3036892182 @default.
- W4386464370 cites W3042580583 @default.
- W4386464370 cites W3087722966 @default.
- W4386464370 cites W3124243234 @default.
- W4386464370 cites W3124355188 @default.
- W4386464370 cites W3137988929 @default.
- W4386464370 cites W3183993513 @default.
- W4386464370 cites W3199532305 @default.
- W4386464370 cites W4206481149 @default.
- W4386464370 cites W4211215713 @default.
- W4386464370 cites W4214833982 @default.
- W4386464370 cites W4308834563 @default.
- W4386464370 cites W4313488897 @default.
- W4386464370 doi "https://doi.org/10.3390/ijms241813707" @default.
- W4386464370 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/37762006" @default.
- W4386464370 hasPublicationYear "2023" @default.
- W4386464370 type Work @default.
- W4386464370 citedByCount "0" @default.
- W4386464370 crossrefType "journal-article" @default.
- W4386464370 hasAuthorship W4386464370A5006200304 @default.
- W4386464370 hasAuthorship W4386464370A5008883576 @default.
- W4386464370 hasAuthorship W4386464370A5015494539 @default.
- W4386464370 hasAuthorship W4386464370A5017915434 @default.
- W4386464370 hasAuthorship W4386464370A5028320053 @default.
- W4386464370 hasAuthorship W4386464370A5034879913 @default.
- W4386464370 hasAuthorship W4386464370A5043866947 @default.
- W4386464370 hasAuthorship W4386464370A5055214820 @default.
- W4386464370 hasAuthorship W4386464370A5058209925 @default.
- W4386464370 hasAuthorship W4386464370A5067048725 @default.
- W4386464370 hasAuthorship W4386464370A5071406940 @default.
- W4386464370 hasAuthorship W4386464370A5073968516 @default.
- W4386464370 hasAuthorship W4386464370A5081072732 @default.
- W4386464370 hasAuthorship W4386464370A5083947932 @default.
- W4386464370 hasAuthorship W4386464370A5092824811 @default.
- W4386464370 hasBestOaLocation W43864643701 @default.
- W4386464370 hasConcept C150903083 @default.
- W4386464370 hasConcept C159110408 @default.
- W4386464370 hasConcept C170493617 @default.
- W4386464370 hasConcept C185592680 @default.
- W4386464370 hasConcept C202751555 @default.
- W4386464370 hasConcept C203014093 @default.
- W4386464370 hasConcept C207001950 @default.
- W4386464370 hasConcept C2776914184 @default.
- W4386464370 hasConcept C2776991684 @default.
- W4386464370 hasConcept C2778491162 @default.
- W4386464370 hasConcept C2778938600 @default.
- W4386464370 hasConcept C41685203 @default.
- W4386464370 hasConcept C55493867 @default.
- W4386464370 hasConcept C67847695 @default.
- W4386464370 hasConcept C67907053 @default.