Fullerene derivatives as inhibitors of the SARS-CoV-2 main protease

Daiki Katagishi; Daisuke Yasuda; Kyoko Takahashi; Shigeo Nakamura; Tadahiko Mashino; Tomoyuki Ohe

doi:10.1016/j.bmcl.2022.129121

Fullerene derivatives as inhibitors of the SARS-CoV-2 main protease

Daiki Katagishi, Daisuke Yasuda, Kyoko Takahashi, Shigeo Nakamura, Tadahiko Mashino, Tomoyuki Ohe

School of Pharmaceutical Sciences

Research output: Contribution to journal › Article › peer-review

Abstract

COVID-19 is an ongoing worldwide pandemic. Even today, there is a need for the development of effective therapeutic agents. SARS-CoV-2 is known as the causative virus of COVID-19, and its main protease is one of the enzymes essential for its growth and is considered a drug discovery target. In this study, we evaluated the inhibitory activities of a variety of fullerene derivatives, including newly synthesized derivatives, against the main protease of SARS-CoV-2. As a result, the malonic acid-type fullerene derivatives showed the strongest inhibitory activity.

Original language	English
Article number	129121
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	80
DOIs	https://doi.org/10.1016/j.bmcl.2022.129121
Publication status	Published - 2023 Jan 15

Keywords

COVID-19
Fullerene
Main protease
SARS-CoV-2

ASJC Scopus subject areas

Biochemistry
Molecular Medicine
Molecular Biology
Pharmaceutical Science
Drug Discovery
Clinical Biochemistry
Organic Chemistry

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10.1016/j.bmcl.2022.129121

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title = "Fullerene derivatives as inhibitors of the SARS-CoV-2 main protease",

abstract = "COVID-19 is an ongoing worldwide pandemic. Even today, there is a need for the development of effective therapeutic agents. SARS-CoV-2 is known as the causative virus of COVID-19, and its main protease is one of the enzymes essential for its growth and is considered a drug discovery target. In this study, we evaluated the inhibitory activities of a variety of fullerene derivatives, including newly synthesized derivatives, against the main protease of SARS-CoV-2. As a result, the malonic acid-type fullerene derivatives showed the strongest inhibitory activity.",

keywords = "COVID-19, Fullerene, Main protease, SARS-CoV-2",

author = "Daiki Katagishi and Daisuke Yasuda and Kyoko Takahashi and Shigeo Nakamura and Tadahiko Mashino and Tomoyuki Ohe",

note = "Funding Information: This work was supported by JST SPRING (Grant Number JPMJSP2123), the Keio University Doctorate Student Grant-in-Aid Program from Ushioda Memorial Fund, the Platform Project for Supporting Drug Discovery and Life Science Research (Basis for Supporting Innovative Drug Discovery and Life Science Research) from AMED (Grant Number JP21am0101089) and JSPS KAKENHI (Grant Number 21K18881). Publisher Copyright: {\textcopyright} 2022 Elsevier Ltd",

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doi = "10.1016/j.bmcl.2022.129121",

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AU - Katagishi, Daiki

AU - Yasuda, Daisuke

AU - Takahashi, Kyoko

AU - Nakamura, Shigeo

AU - Mashino, Tadahiko

AU - Ohe, Tomoyuki

N1 - Funding Information: This work was supported by JST SPRING (Grant Number JPMJSP2123), the Keio University Doctorate Student Grant-in-Aid Program from Ushioda Memorial Fund, the Platform Project for Supporting Drug Discovery and Life Science Research (Basis for Supporting Innovative Drug Discovery and Life Science Research) from AMED (Grant Number JP21am0101089) and JSPS KAKENHI (Grant Number 21K18881). Publisher Copyright: © 2022 Elsevier Ltd

PY - 2023/1/15

Y1 - 2023/1/15

N2 - COVID-19 is an ongoing worldwide pandemic. Even today, there is a need for the development of effective therapeutic agents. SARS-CoV-2 is known as the causative virus of COVID-19, and its main protease is one of the enzymes essential for its growth and is considered a drug discovery target. In this study, we evaluated the inhibitory activities of a variety of fullerene derivatives, including newly synthesized derivatives, against the main protease of SARS-CoV-2. As a result, the malonic acid-type fullerene derivatives showed the strongest inhibitory activity.

AB - COVID-19 is an ongoing worldwide pandemic. Even today, there is a need for the development of effective therapeutic agents. SARS-CoV-2 is known as the causative virus of COVID-19, and its main protease is one of the enzymes essential for its growth and is considered a drug discovery target. In this study, we evaluated the inhibitory activities of a variety of fullerene derivatives, including newly synthesized derivatives, against the main protease of SARS-CoV-2. As a result, the malonic acid-type fullerene derivatives showed the strongest inhibitory activity.

KW - COVID-19

KW - Fullerene

KW - Main protease

KW - SARS-CoV-2

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ER -

Fullerene derivatives as inhibitors of the SARS-CoV-2 main protease

Abstract

Keywords

ASJC Scopus subject areas

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