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dc.contributor.authorJanse van Rensburg, Helena Dorothea
dc.contributor.authorLegoabe, Lesetja J.
dc.contributor.authorTerre'Blanche, Gisella
dc.contributor.authorVan der Walt, Mietha M.
dc.date.accessioned2019-01-28T08:40:37Z
dc.date.available2019-01-28T08:40:37Z
dc.date.issued2019
dc.identifier.citationJanse van Rensburg, H.D. et al. 2019. 2-Benzylidene-1-indanone analogues as dual adenosine A1/A2a receptor antagonists for the potential treatment of neurological conditions. Drug research, 69(07):382-391. [https://doi.org/10.1055/a-0808-3993]en_US
dc.identifier.issn2194-9379 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/31757
dc.identifier.urihttps://www.thieme-connect.com/products/ejournals/abstract/10.1055/a-0808-3993
dc.identifier.urihttps://doi.org/10.1055/a-0808-3993
dc.description.abstractPrevious studies explored 2-benzylidine-1-tetralone derivatives as innovative adenosine A1 and A2A receptor antagonists for alternative non-dopaminergic treatment of Parkinson’s disease. This study’s aim is to investigate structurally related 2-benzylidene-1-indanones with substitutions on ring A and B as novel, potent and selective adenosine A1 and A2A receptor blockers. 2-Benzylidene-1-indanone derivatives were synthesised via acid catalysed aldol condensation reactions and evaluated via radioligand binding assays to ascertain structure activity relationships to govern A1 and A2A AR affinity. The results indicated that hydroxy substitution at C4 of ring A and meta (3’), or para (4’) substitution on ring B of the 2-benzylidene-1-indanone scaffold (2c) is preferred over substitution at C5 (2d) or C6 (2e) of ring A for adenosine A1 receptor activity and selectivity in the micromolar range. Furthermore, substitution at the meta (3’) position of ring B with chlorine lead to the highly potent and selective adenosine A2A receptor antagonist, compound 2 h. Compound 2c and the 2q behaved as adenosine A1 receptor antagonists in the performed GTP shift assays. In view of these findings, compounds 2c, 2 h, 2q and 2p are potent and selective adenosine A1 and A2A receptor antagonists for the potential treatment of neurological conditionsen_US
dc.language.isoenen_US
dc.publisherThiemeen_US
dc.subjectParkinson’s diseaseen_US
dc.subjectAlzheimer’s diseaseen_US
dc.subject4–Hydroxy–2–benzylidene–1–indanonesen_US
dc.subjectAdenosine antagonistsen_US
dc.title2-Benzylidene-1-indanone analogues as dual adenosine A1/A2a receptor antagonists for the potential treatment of neurological conditionsen_US
dc.typeArticleen_US
dc.contributor.researchID12902608 - Legoabe, Lesetja Jan
dc.contributor.researchID13035134 - Van der Walt, Mietha Magdalena
dc.contributor.researchID10206280 - Terre'Blanche, Gisella
dc.contributor.researchID23551917 - Janse van Rensburg, Helena Dorothea


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