Elongation of the side chain by linear alkyl groups increases the potency of salacinol, a potent α-glucosidase inhibitor from the Ayurvedic traditional medicine "Salacia," against human intestinal maltase.
Animals
Dose-Response Relationship, Drug
Glycoside Hydrolase Inhibitors
/ chemical synthesis
Humans
Intestines
/ enzymology
Medicine, Ayurvedic
Molecular Conformation
Rats
Salacia
/ chemistry
Structure-Activity Relationship
Sugar Alcohols
/ chemical synthesis
Sulfates
/ chemical synthesis
alpha-Glucosidases
/ metabolism
Kotalanol
SAR study
Salacia
Salacinol
α-Glucosidase inhibitor
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
01 02 2021
01 02 2021
Historique:
received:
27
10
2020
revised:
10
12
2020
accepted:
12
12
2020
pubmed:
22
12
2020
medline:
23
7
2021
entrez:
21
12
2020
Statut:
ppublish
Résumé
Four chain-extended analogs (12a-12d) and two related de-O-sulfonated analogs (13a and 13c) by introducing alkyl groups (a: R = C
Identifiants
pubmed: 33347966
pii: S0960-894X(20)30862-3
doi: 10.1016/j.bmcl.2020.127751
pii:
doi:
Substances chimiques
Glycoside Hydrolase Inhibitors
0
Sugar Alcohols
0
Sulfates
0
salacinol
0
alpha-Glucosidases
EC 3.2.1.20
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
127751Informations de copyright
Copyright © 2020. Published by Elsevier Ltd.