Novel glycosyl prodrug of RXP03 as MMP-11 prodrug: design, synthesis and virtual screening

Like most phosphinic acids, the potent and selective RXP03 inhibitor of different MMPs exhibited moderate absorption and low bioavailability, which impaired its use. In an unprecedented attempt, we present an interesting synthetic approach to a new class of phosphinate prodrug, glycosyl ester of RXP...

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Detalles Bibliográficos
Autores principales: Abdou, Moaz M., Ötvös, Ferenc, Dong, Dewen, Matziari, Magdalini
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer International Publishing 2023
Materias:
Research
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10675898/
https://www.ncbi.nlm.nih.gov/pubmed/38007463
http://dx.doi.org/10.1186/s13065-023-01075-1
Descripción
Sumario:Like most phosphinic acids, the potent and selective RXP03 inhibitor of different MMPs exhibited moderate absorption and low bioavailability, which impaired its use. In an unprecedented attempt, we present an interesting synthetic approach to a new class of phosphinate prodrug, glycosyl ester of RXP03, to provide a potentially improved blood–brain barrier (BBB) behavior compared to the former lead compound RXP03. To validate this speculation, a predictive study for permeability enhancer of glycosyl ester of RXP03 showed encouraging insights to improve drug delivery across biological barriers.

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