(E)-3-Heteroarylidenechroman-4-ones as potent and selective monoamine oxidase-B inhibitors
详细信息 查看全文
- 作者：Nicoletta Desideria ; nicoletta.desideri@uniroma1.it" class="auth_mail" title="E-mail the corresponding author ; Luca Proietti Monacoa ; Rossella Fioravantia ; Mariangela Biavaa ; Matilde Yá ; ñ ; ezb ; Stefano Alcaroc ; Francesco Ortusoc
- 关键词：Monoamine oxidases ; Selective hMAO-B inhibitors ; Chroman-4-ones ; Homoisoflavonoids ; Docking studies
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：19 July 2016
- 年：2016
- 卷：117
- 期：Complete
- 页码：292-300
- 全文大小：1363 K
文摘
- •
A series of (E)-3-heteroarylidenechroman-4-ones was synthesized.
- •
The compounds were evaluated in vitro as inhibitors of both human MAO isoforms.
- •
All the compounds were found to be selective hMAO-B inhibitors.
- •
The most active compound showed MAO-B inhibitory activity in the nanomolar range.
- •
Docking and molecular dynamics simulations proposed the binding mode of the best compound.