학술논문
Novel glycosyl prodrug of RXP03 as MMP-11 prodrug: design, synthesis and virtual screening.
Document Type
Article
Source
Subject
*PRODRUGS
*LEAD compounds
*PHOSPHINIC acid
*BLOOD-brain barrier
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Language
ISSN
2661-801X
Abstract
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. [ABSTRACT FROM AUTHOR]