Abdou, Moaz M. and Ötvös, Ferenc and Dong, Dewen and Matziari, Magdalini (2023) Novel glycosyl prodrug of RXP03 as MMP-11 prodrug: design, synthesis and virtual screening. BMC CHEMISTRY, 17 (1). No.-167. ISSN 2661-801X
|
Text
s13065-023-01075-1-2.pdf Download (2MB) | Preview |
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.
| Item Type: | Article |
|---|---|
| Additional Information: | Funding Agency and Grant Number: Egyptian Petroleum Research Institute Funding text: The authors are greatly thankful to the Egyptian Petroleum Research Institute (EPRI) for research facilities. |
| Uncontrolled Keywords: | Prodrug, RXP03, Phosphinic ester, Matrix metalloproteases, Molecular docking, Permeability enhancer |
| Subjects: | Q Science / természettudomány > QD Chemistry / kémia |
| SWORD Depositor: | MTMT SWORD |
| Depositing User: | MTMT SWORD |
| Date Deposited: | 20 Feb 2024 08:33 |
| Last Modified: | 20 Feb 2024 08:33 |
| URI: | https://real.mtak.hu/id/eprint/188580 |
Actions (login required)
 |
Edit Item |
