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Synthesis and in vitro evaluation of pteridine analogues as monoamine oxidase B and nitric oxice synthase inhibitors

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dc.contributor.author Petzer, Jacobus P. en_US
dc.contributor.author Prins, Louis H.A. en_US
dc.contributor.author Malan, Sarel F. en_US
dc.date.accessioned 2010-08-04T15:36:09Z
dc.date.available 2010-08-04T15:36:09Z
dc.date.issued 2009 en_US
dc.identifier.citation Prins, L.H.A. et al. 2009. Synthesis and in vitro evaluation of pteridine analogues as monoamine oxidase B and nitric oxice synthase inhibitors. Bioorganic and medicinal chemistry, 17(21):7523-7530. [http://www.journals.elsevier.com/bioorganic-and-medicinal-chemistry/] en_US
dc.identifier.uri http://hdl.handle.net/10394/3383
dc.description.abstract Monoamine 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.description.uri http://dx.doi.org/10.1016/j.bmc.2009.09.019
dc.title Synthesis and in vitro evaluation of pteridine analogues as monoamine oxidase B and nitric oxice synthase inhibitors en_US
dc.contributor.researchID 10727388 - Petzer, Jacobus Petrus
dc.contributor.researchID 10199667 - Malan, Sarel Francois


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