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

Author:

Mizuta Satoshi1ORCID,Mosaddeque Farhana2,Tun Mya Myat Ngwe3,Teklemichael Awet Alem4,Taniguchi Mayumi4,Hosokawa Masashi5,Yamaguchi Tomoko1,Makau Juliann6,Huy Nguyen Tien27,Mizukami Shusaku4,Nishida Noriyuki8,Morita Kouichi39,Hirayama Kenji27

Affiliation:

1. Center for Bioinformatics and Molecular Medicine Nagasaki University 1-14 Bunkyo 852-8521 Nagasaki Japan

2. Department of Immunogenetics Institute of Tropical Medicine (NEKKEN) Nagasaki University 1-12-4 Sakamoto 852-8523 Nagasaki Japan

3. Department of Virology Institute of Tropical Medicine (NEKKEN) Nagasaki University 1-12-4 Sakamoto 852-8523 Nagasaki Japan

4. Department of Immune Regulation Shionogi Global Infectious Diseases Division Nagasaki University 1-12-4 Sakamoto 852-8523 Nagasaki Japan

5. School of Medicine Nagasaki University 1-12-4 Sakamoto 852-8523 Nagasaki Japan

6. Center for Virus Research Kenya Medical Research Institute 54840-00200 Nairobi Kenya

7. School of Tropical Medicine and Global Health Nagasaki University 1-12-4 Sakamoto 852-8102> Nagasaki Japan

8. Department of Molecular Microbiology and Immunology Nagasaki University 1-12-4 Sakamoto 852-8102 Nagasaki Japan

9. Dejima Infectious Disease Research Alliance Nagasaki University Nagasaki 852-8523 Japan

Abstract

AbstractWe 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.

Funder

Japan Agency for Medical Research and Development

Publisher

Wiley

Subject

Organic Chemistry,General Pharmacology, Toxicology and Pharmaceutics,Molecular Medicine,Drug Discovery,Biochemistry,Pharmacology

Reference56 articles.

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