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Thiamine analogues as inhibitors of pyruvate dehydrogenase and discovery of a thiamine analogue with non-thiamine related antiplasmodial activity

A series of derivatives of a triazole analogue of thiamine has been synthesised. When tested as inhibitors of porcine pyruvate dehydrogenase, the benzoyl ester derivatives proved to be potent thiamine pyrophosphate (TPP) competitive inhibitors, with the affinity of the most potent analogue (K(i) = 5...

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Detalles Bibliográficos
Autores principales: Chan, Alex H. Y., Fathoni, Imam, Ho, Terence C. S., Saliba, Kevin J., Leeper, Finian J.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: RSC 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9298186/
https://www.ncbi.nlm.nih.gov/pubmed/35919337
http://dx.doi.org/10.1039/d2md00085g