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Modification on the O-glucoside of Sergliflozin-A: A new strategy for SGLT2 inhibitor design.
- Source :
-
Bioorganic & Medicinal Chemistry Letters . May2016, Vol. 26 Issue 9, p2170-2173. 4p. - Publication Year :
- 2016
-
Abstract
- Poor pharmacokinetic stability is one of the issues of O -glucoside SGLT2 inhibitors in clinical trials, hence C -glucoside inhibitors have been developed and extensively applied. Herein, we provided an alternative approach to improve the pharmacokinetic stability of such inhibitors. Nine derivatives of Sergliflozin-A with modifications on the O -glucoside fragment were prepared, among which the 4- O -methyl derivative exhibited similar pharmacodynamics potency in excreted glucose urine test. Most attractively, significantly increased pharmacokinetic stability was observed for 4- O -methyl derivative of O -glucosides. This work proved that modification on the O -glucoside fragment could be a promising approach to the future SGLT2 inhibitor design. [ABSTRACT FROM AUTHOR]
- Subjects :
- *GLUCOSIDES
*PHARMACOKINETICS
*DRUG design
*CHEMICAL derivatives
*CLINICAL trials
Subjects
Details
- Language :
- English
- ISSN :
- 0960894X
- Volume :
- 26
- Issue :
- 9
- Database :
- Academic Search Index
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Publication Type :
- Academic Journal
- Accession number :
- 114483376
- Full Text :
- https://doi.org/10.1016/j.bmcl.2016.03.065