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dc.contributor.authorRobinson, Sarel J.
dc.contributor.authorPetzer, Jacobus P.
dc.contributor.authorTerre'Blanche, Gisella
dc.contributor.authorPetzer, Anél
dc.contributor.authorVan der Walt, Mietha M.
dc.contributor.authorBergh, Jacobus J.
dc.contributor.authorLourens, Anna C.U.
dc.date.accessioned2016-08-22T09:51:19Z
dc.date.available2016-08-22T09:51:19Z
dc.date.issued2015
dc.identifier.citationRobinson, S.J. et al. 2015. 2-Aminopyrimidines as dual adenosine A1/A2A antagonists. European journal of medicinal chemistry, 104:177-188. [https://doi.org/10.1016/j.ejmech.2015.09.035]en_US
dc.identifier.issn0223-5234
dc.identifier.issn1768-3254 (Online)
dc.identifier.urihttp://hdl.handle.net/10394/18353
dc.identifier.urihttps://doi.org/10.1016/j.ejmech.2015.09.035
dc.identifier.urihttps://www.sciencedirect.com/science/article/pii/S0223523415302798
dc.description.abstractIn this study thirteen 2-aminopyrimidine derivatives were synthesised and screened as potential antagonists of adenosine A1 and A2A receptors in order to further investigate the structure activity relationships of this class of compounds. 4-(5-Methylfuran-2-yl)-6-[3-(piperidine-1-carbonyl)phenyl]pyrimidin-2-amine (8m) was identified as a compound with high affinities for both receptors, with an A2AKi value of 6.34 nM and an A1Ki value of 9.54 nM. The effect of selected compounds on the viability of cultured cells was assessed and preliminary results indicate low cytotoxicity. In vivo efficacy at A2A receptors was illustrated for compounds 8k and 8m since these compounds attenuated haloperidol-induced catalepsy in rats. A molecular docking study revealed that the interactions between the synthesised compounds and the adenosine A2A binding site most likely involve Phe168 and Asn253, interactions which are similar for structurally related adenosine A2A receptor antagonistsen_US
dc.description.sponsorshipNorth-West University, Medical Research Council (MRC) and the National Research Foundation (UID 76308)en_US
dc.language.isoenen_US
dc.publisherElsevieren_US
dc.subjectParkinson's diseaseen_US
dc.subjectAdenosine A2A antagonisten_US
dc.subjectAdenosine A1 antagonisten_US
dc.subject2-Aminopyrimidineen_US
dc.title2-Aminopyrimidines as dual adenosine A1/A2A antagonistsen_US
dc.typeArticleen_US
dc.contributor.researchID20367414 - Robinson, Sarel Johannes
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus
dc.contributor.researchID10206280 - Terre'Blanche, Gisella
dc.contributor.researchID12264954 - Petzer, Anél
dc.contributor.researchID13035134 - Van der Walt, Mietha Magdalena
dc.contributor.researchID10057072 - Bergh, Jacobus Johannes
dc.contributor.researchID10948724 - Lourens, Anna Catharina U.


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