| Autor: |
Yoshihide Usami, Megumi Higuchi, Koji Mizuki, Mizuki Yamamoto, Mao Kanki, Chika Nakasone, Yuya Sugimoto, Makio Shibano, Yoshihiro Uesawa, Junko Nagai, Hiroki Yoneyama, Shinya Harusawa |
| Jazyk: |
angličtina |
| Rok vydání: |
2020 |
| Předmět: |
|
| Zdroj: |
Marine Drugs, Vol 18, Iss 4, p 221 (2020) |
| Druh dokumentu: |
article |
| ISSN: |
1660-3397 |
| DOI: |
10.3390/md18040221 |
| Popis: |
Inspired by the significant α-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 α-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 α-glucosidase. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
|
