ArticlePNAS nexus2025
An orally available P1'-5-fluorinated M
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Article in PNAS nexus, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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9citing papers in PubMed
–field-weighted citation impact
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
9 citing papers in PubMed.
- Insights into the complexity of SARS-CoV-2 MJournal of enzyme inhibition and medicinal chemistry · 2026Article
- Slowly exchanging bound states of SARS-CoV-2 3CLStructural dynamics (Melville, N.Y.) · 2026Article
- Characterization of the Cross-Resistance of SARS-CoV‑2 Main Protease Inhibitors, Ibuzatrelvir, Ensitrelvir, and Nirmatrelvir.ACS pharmacology & translational science · 2026Article
- Impact of Single Halogen Atom Substitutions on Antiviral Profile of Inhibitors Targeting SARS-CoV‑2 Main Protease.ACS omega · 2026Article
- Design and Synthesis of Novel Spiropyridine Derivatives as Promising Anti-inflammatory and Gene-targeting Agents Against COVID-19.Current pharmaceutical design · 2026Article
- SARS-CoV‑2 Papain-Like Protease Inhibitors Based on Naphthalen-1-ylethanamine and Halogenated Benzene Moieties.ACS omega · 2025Article
- Azapeptide-Based SARS-CoV-2 Main Protease Inhibitors: Design, Synthesis, Enzyme Inhibition, Structural Determination, and Antiviral Activity.Journal of medicinal chemistry · 2025Article
- SARS-CoV‑2 Main Protease Inhibitors Containing 5‑Substituted Benzothiazole-2-carbonyl Moieties at the P1' Site and Their Derivatives.ACS omega · 2025Article
- Glycosylated 18β-glycyrrhetinic acid derivatives as promising inhibitors of the SARS-CoV-2 main protease.RSC advances · 2025Article
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
28 authors.
Nobuyo Higashi-KuwataDepartment of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan.ORCID https://orcid.org/0000-0002-9404-3532
Haydar BulutExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, NIH, Bethesda, MD 20892, USA.ORCID https://orcid.org/0000-0003-0262-6296
Hironori HayashiDepartment of Infectious Diseases, International Research Institute of Disaster Science, Tohoku University, Aoba-ku, Sendai 980-8575, Japan.ORCID https://orcid.org/0000-0002-5892-0040
Kohei TsujiDepartment of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan.ORCID https://orcid.org/0000-0003-4773-8793
Hiromi Ogata-AokiDepartment of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan.ORCID https://orcid.org/0000-0002-9290-911X
Maki KisoDivision of Virology, Institute of Medical Science, University of Tokyo, Minato-ku, Tokyo 108-8639, Japan.ORCID https://orcid.org/0009-0004-3645-0967
Nobutoki TakamuneDepartment of Environmental and Molecular Health Sciences, Faculty of Life Sciences, Kumamoto University, 5-1 Oe-honmachi, Chuo-ku, Kumamoto 862-0973, Japan.ORCID https://orcid.org/0000-0001-7173-240X
Naoki KishimotoDepartment of Environmental and Molecular Health Sciences, Faculty of Life Sciences, Kumamoto University, 5-1 Oe-honmachi, Chuo-ku, Kumamoto 862-0973, Japan.ORCID https://orcid.org/0000-0002-9401-8118
Shin-Ichiro HattoriDepartment of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan.ORCID https://orcid.org/0000-0002-5637-3397
Takahiro IshiiDepartment of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan.ORCID https://orcid.org/0000-0003-1664-6191
Takuya KobayakawaDepartment of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan.ORCID https://orcid.org/0000-0001-9786-2608
Kenta NakanoDepartment of Laboratory Animal Medicine, National Center for Global Health and Medicine Research Institute, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan.ORCID https://orcid.org/0000-0003-2617-1468
Yukiko ShimizuDepartment of Laboratory Animal Medicine, National Center for Global Health and Medicine Research Institute, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan.ORCID https://orcid.org/0000-0003-2120-3993
Debananda DasExperimental Retrovirology Section, HIV and AIDS Malignancy Branch, National Cancer Institute, NIH, Bethesda, MD 20892, USA.ORCID https://orcid.org/0000-0001-9943-5888
Junji SaruwatariDivision of Pharmacology and Therapeutics, Graduate School of Pharmaceutical Sciences, Kumamoto University, Chuo-ku, Kumamoto 862-0973, Japan.ORCID https://orcid.org/0000-0001-6266-1347
Kazuya HasegawaStructural Biology Division, Japan Synchrotron Radiation Research Institute, 1-1-1 Kouto, Sayo, Hyogo 679-5198, Japan.ORCID https://orcid.org/0000-0003-0331-1624
Kazutaka MurayamaGraduate School of Biomedical Engineering, Tohoku University, Miyagi 980-8579, Japan.ORCID https://orcid.org/0000-0003-1749-4038
Yoshikazu SukenagaDepartment of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan.ORCID https://orcid.org/0000-0001-8479-3842
Yuki TakamatsuDepartment of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan.ORCID https://orcid.org/0000-0001-7967-1576
Kazuhisa YoshimuraTokyo Metropolitan Institute of Public Health, Shinjuku-ku, Tokyo 169-0073, Japan.
Manabu AokiDepartment of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan.ORCID https://orcid.org/0000-0001-7089-831X
Yuri FurusawaDivision of Virology, Institute of Medical Science, University of Tokyo, Minato-ku, Tokyo 108-8639, Japan.ORCID https://orcid.org/0000-0002-7489-7303
Tadashi OkamuraDepartment of Laboratory Animal Medicine, National Center for Global Health and Medicine Research Institute, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan.ORCID https://orcid.org/0000-0001-8457-1561
Seiya YamayoshiDivision of Virology, Institute of Medical Science, University of Tokyo, Minato-ku, Tokyo 108-8639, Japan.ORCID https://orcid.org/0000-0001-7768-5157
Yoshihiro KawaokaDivision of Virology, Institute of Medical Science, University of Tokyo, Minato-ku, Tokyo 108-8639, Japan.ORCID https://orcid.org/0000-0001-5061-8296
Shogo MisumiDepartment of Environmental and Molecular Health Sciences, Faculty of Life Sciences, Kumamoto University, 5-1 Oe-honmachi, Chuo-ku, Kumamoto 862-0973, Japan.ORCID https://orcid.org/0000-0002-9465-4720
Hirokazu TamamuraDepartment of Medicinal Chemistry, Institute of Biomaterials and Bioengineering, Tokyo Medical and Dental University, Chiyoda-ku, Tokyo 101-0062, Japan.ORCID https://orcid.org/0000-0003-2788-2579
Hiroaki MitsuyaDepartment of Refractory Viral Diseases, National Center for Global Health and Medicine Research Institute, 1-21-1 Toyama, Shinjuku-ku, Tokyo 162-8655, Japan.ORCID https://orcid.org/0000-0001-9274-3853
Funding
No grant is acknowledged in the PubMed record.
Abstract
We identified a 5-fluoro-benzothiazole-containing small molecule, TKB272, through fluorine-scanning of the benzothiazole moiety, which more potently inhibits the enzymatic activity of SARS-CoV-2's main protease (M
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COVID-19fluorine-scanninggenetic barrierMpro inhibitorSARS-CoV-2
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