阿莫地喹类似物的设计、合成及其抗sars - cov -2活性

IF 1.5 4区医学 Q4 CHEMISTRY, MEDICINAL

Chemical & pharmaceutical bulletin Pub Date : 2025-01-01 DOI:10.1248/cpb.c24-00647

Shin Aoki, Tomohiro Tanaka, Kenta Yokoi, Azusa Kanbe, Tomoe Morita, Mayuka Nii, Hidetoshi Satoh, Masaki Kakihana, Shotaro Otaki, Saki Sekiguchi, Koki Nakamura, Toshifumi Tojo, Masanori Baba, Mika Okamoto

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引用次数: 0

摘要

由新型冠状病毒严重急性呼吸综合征冠状病毒2型（SARS-CoV-2）引起的2019年冠状病毒病大流行仍是全球严重关切的问题。虽然已经开发出一些有效的疫苗，但只有少数抗sars - cov -2药物被批准用于临床。本研究以抗疟药阿莫地喹的化学结构为基础，设计合成了新的抗sars - cov -2药物。因此，我们已经确定了具有二氨基悬垂氨基酚基团功能化的amodiaquine类似物，具有高水平的抗sars - cov -2活性和低水平的毒性。

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Design, Synthesis, and Anti-SARS-CoV-2 Activity of Amodiaquine Analogs.

The pandemic of coronavirus disease 2019, caused by the new coronavirus severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2), remains a serious concern worldwide. Although some effective vaccines have been developed, only a few anti-SARS-CoV-2 drugs have been approved for their clinical use. In this study, we designed and synthesized new anti-SARS-CoV-2 drugs based on the chemical structure of amodiaquine, which is known as an antimalarial drug. Consequently, we have identified amodiaquine analogs functionalized with dialkylamino-pendant aminophenol moieties that possess a high level of anti-SARS-CoV-2 activity with a low level of toxicity.

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来源期刊

Chemical & pharmaceutical bulletin 医学-化学综合

CiteScore

3.20

自引率

5.90%

发文量

132

审稿时长

1.7 months

期刊介绍： The CPB covers various chemical topics in the pharmaceutical and health sciences fields dealing with biologically active compounds, natural products, and medicines, while BPB deals with a wide range of biological topics in the pharmaceutical and health sciences fields including scientific research from basic to clinical studies. For details of their respective scopes, please refer to the submission topic categories below. Topics: Organic chemistry In silico science Inorganic chemistry Pharmacognosy Health statistics Forensic science Biochemistry Pharmacology Pharmaceutical care and science Medicinal chemistry Analytical chemistry Physical pharmacy Natural product chemistry Toxicology Environmental science Molecular and cellular biology Biopharmacy and pharmacokinetics Pharmaceutical education Chemical biology Physical chemistry Pharmaceutical engineering Epidemiology Hygiene Regulatory science Immunology and microbiology Clinical pharmacy Miscellaneous.