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dc.contributor.authorJanse van Rensburg, Helena D.
dc.contributor.authorLegoabe, Lesetja J.
dc.contributor.authorTerre'Blanche, Gisella
dc.date.accessioned2020-06-11T12:02:26Z
dc.date.available2020-06-11T12:02:26Z
dc.date.issued2020
dc.identifier.citationJanse van Rensburg, H.D. et al. 2020. Synthesis and structure activity relationships of chalcone based benzocycloalkanone derivatives as adenosine a 1 and/or a 2a receptor antagonists. Drug research, 70(6):243-256. [https://doi.org/10.1055/a-1146-2996]en_US
dc.identifier.issn2194-9379
dc.identifier.urihttp://hdl.handle.net/10394/34760
dc.identifier.urihttps://www.thieme-connect.com/products/ejournals/abstract/10.1055/a-1146-2996
dc.identifier.urihttps://doi.org/10.1055/a-1146-2996
dc.description.abstractAdenosine A1 and/or A2A receptor antagonists hold promise for the potential treatment of neurological conditions, such as Parkinson’s disease. Herein, a total of seventeen benzocycloalkanone derivatives were synthesised and evaluated for affinity towards adenosine receptors (A1 and A2A AR). The obtained results allowed for the conclusion that affinity and/or selectivity of the 2-benzylidene-1-indanone and -tetralone derivatives toward A1 and/or A2A ARs may be modulated by the nature of the substituents (either -OH, -OCH3 or morpholine) attached at position C4 of the 1-indanone core and C5 of the 1-tetralone core as well as the meta (C3’) and/or para (C4’) position(s) on ring B. Several compounds (2a–b, 3b–c and 4a–b) possessed affinity for the A1 and/or A2A AR below 10 µM. Additionally, compounds 2a, 3b and 4a were A1 AR antagonists. These results, once again, confirmed the importance of C4 methoxy-group substitution on ring A in combination with meta (C3’) and/or para (C4’) hydroxyl-group substitution ring B of the 2-benzylidene-1-indanone scaffold leading to drug-like compounds 1h and 1j with affinity in the nanomolar-rangeen_US
dc.language.isoenen_US
dc.publisherThiemeen_US
dc.subject2-Benzylidene-1-tetralone derivativesen_US
dc.subject2-Benzylidene-1-indanone derivativesen_US
dc.subjectAcid catalysed aldol condensation reactionen_US
dc.subjectNeurological conditionsen_US
dc.titleSynthesis and structure activity relationships of chalcone based benzocycloalkanone derivatives as adenosine a 1 and/or a 2a receptor antagonistsen_US
dc.typeArticleen_US
dc.contributor.researchID12902608 - Legoabe, Lesetja Jan
dc.contributor.researchID10206280 - Terre'Blanche, Gisella
dc.contributor.researchID23551917 - Janse van Rensburg, Helena Dorothea


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