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dc.contributor.authorPrins, Louis H.A.en_US
dc.contributor.authorPetzer, Jacobus P.en_US
dc.contributor.authorMalan, Sarel F.en_US
dc.identifier.citationPrins, L.H.A. et al. 2009. Synthesis and in vitro evaluation of pteridine analogues as monoamine oxidase B and nitric oxice synthase inhibitors. Bioorganic & medicinal chemistry, 17(21):7523-7530. []en_US
dc.identifier.issn1464-3391 (Online)
dc.description.abstractMonoamine oxidase B (MAO-B) and nitric oxide synthase (NOS) have both been implicated in the pathology of neurodegenerative diseases. In an attempt to design dual-target-directed drugs that inhibit both these enzymes, a series of pteridine-2,4-dione analogues were synthesised. The compounds were found to be relatively weak NOS inhibitors but showed promising MAO-B activity with 6-amino-5-[(E)-3-(3-chloro-phenyl)-prop-2-en-(E)-ylideneamino]-1,3-dimethyl-1H-pyrimidine-2,4-dione and 6-[(E)-2-(3-chloro-phenyl)-vinyl]-1,3-dimethyl-1H-pteridine-2,4-dione inhibiting MAO-B with IC(50) values of 0.602 and 0.314 microM, respectively. The pteridine-2,4-dione analogues thus show promise as scaffolds for the development of potent reversible MAO-B inhibitors and as observed in earlier studies, the most potent inhibitors were obtained with 3-chlorostyryl substitution.
dc.subjectMonoamine oxidase B
dc.subjectNitric oxide synthase
dc.subjectDual-target-directed ligands
dc.titleSynthesis and in vitro evaluation of pteridine analogues as monoamine oxidase B and nitric oxice synthase inhibitorsen_US
dc.contributor.researchID10727388 - Petzer, Jacobus Petrus
dc.contributor.researchID10199667 - Malan, Sarel Francois
dc.contributor.researchID12256129 - Prins, Louis Hendrik Albertus

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