Structure Optimization of Aloperine Derivatives as HIV-1 Entry Inhibitors.

Journal Article (Journal Article)

As a step toward developing novel anti-HIV agents, we have identified a class of quinolizidines, including aloperine, that inhibit HIV at 1-5 μM by blocking viral entry. In this study, we have optimized the structure of aloperine and derived compounds with markedly improved activity. Our structural optimization has yielded an aloperine derivative 19 with approximately a 15-fold increase in anti-HIV-1 activity. Our mechanism of action study reveals that compound 19 does not inhibit binding of HIV-1 to receptors but arrests the virus from fusion with the membrane. Binding of the compound to HIV-1gp120 might be responsible for its anti-HIV-1 entry activity.

Full Text

Duke Authors

Cited Authors

  • Dang, Z; Xie, H; Zhu, L; Zhang, Q; Li, Z; Huang, L; Chen, C-H

Published Date

  • November 9, 2017

Published In

Volume / Issue

  • 8 / 11

Start / End Page

  • 1199 - 1203

PubMed ID

  • 29152054

Pubmed Central ID

  • PMC5683702

International Standard Serial Number (ISSN)

  • 1948-5875

Digital Object Identifier (DOI)

  • 10.1021/acsmedchemlett.7b00376

Language

  • eng

Conference Location

  • United States