Challenges Based on Antiplasmodial and Antiviral Activities of 7-Chloro-4-aminoquinoline Derivatives

ChemMedChem. 2023 Apr 3;18(7):e202200586. doi: 10.1002/cmdc.202200586. Epub 2023 Feb 8.

Abstract

We report the structural functionalization of the terminal amino group of N1 -(7-chloroquinolin-4-yl) butane-1,4-diamine, leading to a series of 7-chloro-4-aminoquinoline derivatives, and their evaluation as potent anti-malarial and anti-viral agents. Some compounds exhibited promising anti-malarial effects against the Plasmodium falciparum 3D7 (chloroquine-sensitive) and Dd2 (chloroquine-resistant) strains. In addition, these compounds were assayed in vitro against influenza A virus (IAV) and severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Compound 5 h, bearing an N-mesityl thiourea group, displayed pronounced anti-infectious effects against malaria, IAV, and SARS-CoV-2. These results provide new insights into drug discovery for the prevention or treatment of malaria and virus co-infection.

Keywords: Anti-SARS-CoV-2; Anti-influenza virus; Anti-malaria; Chloroquine; Co-infection.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antimalarials* / chemistry
  • Antiviral Agents / pharmacology
  • Antiviral Agents / therapeutic use
  • COVID-19*
  • Chloroquine / pharmacology
  • Humans
  • Malaria* / drug therapy
  • Plasmodium falciparum
  • SARS-CoV-2

Substances

  • Antimalarials
  • 7-chloro-4-aminoquinoline
  • Antiviral Agents
  • Chloroquine