SYNTHESIS OF NEW CHLOROQUINE DERIVATIVES FOR BIOLOGICAL STUDIES | ||
| Al-Azhar Journal of Pharmaceutical Sciences | ||
| Volume 70, Issue 2, September 2024, Pages 103-119 PDF (1.34 M) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ajps.2024.429774 | ||
| Authors | ||
| Mohamed Elsebaei* 1; Abdullah Y. Saad2; Abdelrahman S. Mayhoub3; Korany A. Ali4 | ||
| 1Department of Pharmaceutical Organic Chemistry, College of Pharmacy(boys), Al-Azhar University, Cairo 11884, Egypt. | ||
| 2Department of Pharmaceutical Organic Chemistry, College of Pharmacy, Al-Azhar University, Cairo, 11884, Egypt | ||
| 31Department of Pharmaceutical Organic Chemistry, College of Pharmacy, Al-Azhar University, Cairo, 11884, Egypt & Nanoscience Program, University of Science and Technology, Zewail City of Science and Technology, Giza, Egypt | ||
| 4Center of Excellence, Advanced Material & Nanotechnology Group, National Research Centre, &Applied Organic Chemistry Department, National Research Centre, 12622 Dokki, Giza, Egypt | ||
| Abstract | ||
| This study focused on the development of novel chloroquine derivatives as potential antiviral agents against SARS-CoV-2. By modifying the 7-position of chloroquine using Sonogashira and Buchwald cross-coupling reactions, a series of compounds were synthesized. In vitro evaluations identified several derivatives with promising antiviral activity, with compound 9d exhibiting strong inhibitory effects and a favorable selectivity index. These results suggest that the derivatives provide a promising basis for further optimization and development as antiviral drugs. This work highlights the potential of structural modifications to improve the effectiveness of chloroquine derivatives. Given the ongoing challenges of COVID-19, these novel compounds deserve further investigation to determine their mechanisms of action and therapeutic value. This study provides important insights into antiviral drug development and highlights the need for continued efforts to optimize existing drug scaffolds in the fight against emerging viral threats. | ||
| Keywords | ||
| Chloroquine; COVID-19; Sonogashira cross-coupling; Buchwald cross-coupling; Antiviral agent | ||
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