Syntheses and Glycosidase Inhibitory Activities, and in Silico Docking Studies of Pericosine E Analogs Methoxy-Substituted at C6.
Mar Drugs
; 18(4)2020 Apr 20.
Article
em En
| MEDLINE
| ID: mdl-32326065
ABSTRACT
Inspired by the significant ï¡-glucosidase inhibitory activities of (+)- and (-)-pericosine E, we herein designed and synthesized 16 analogs of these marine natural products bearing a methoxy group instead of a chlorine atom at C6. Four of these compounds exhibited moderate ï¡-glucosidase inhibitory activities, which were weaker than those of the corresponding chlorine-containing species. The four compounds could be prepared by coupling reactions utilizing the (-)-pericosine B moiety. An additional in silico docking simulation suggested that the reason of reduced activity of the C6-methoxylated analogs might be an absence of hydrogen bonding between a methoxy group with the surrounding amino acid residues in the active site in ï¡-glucosidase.
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01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ácido Chiquímico
/
Inibidores de Glicosídeo Hidrolases
Idioma:
En
Revista:
Mar Drugs
Ano de publicação:
2020
Tipo de documento:
Article