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Article

FDA-Approved Drugs with Potent In Vitro Antiviral Activity against Severe Acute Respiratory Syndrome Coronavirus 2

1
Center of Scientific Excellence for Influenza Viruses, National Research Centre, Giza 12622, Egypt
2
Organic & Medicinal Chemistry Department, Faculty of Pharmacy, University of Sadat City, Menoufia 32897, Egypt
3
Department of Biochemistry & Molecular Biology, Drexel University College of Medicine, Philadelphia, PA 19102, USA
4
Department of Microbiology and Immunology, Zagazig University, Zagazig 44519, Egypt
5
Pharmaceutics Department, National Organization for Drug Control and Research, Giza 12654, Egypt
6
Department of Epidemiology, Human Genetics, and Environmental Sciences, University of Texas, Houston, TX 77030, USA
7
Human Link, Baabda 1109, Lebanon
*
Authors to whom correspondence should be addressed.
Contributed equally to this work.
Pharmaceuticals 2020, 13(12), 443; https://0-doi-org.brum.beds.ac.uk/10.3390/ph13120443
Received: 22 October 2020 / Revised: 30 November 2020 / Accepted: 1 December 2020 / Published: 4 December 2020
(This article belongs to the Special Issue COVID-19 in Pharmaceuticals)
(1) Background: Drug repositioning is an unconventional drug discovery approach to explore new therapeutic benefits of existing drugs. Currently, it emerges as a rapid avenue to alleviate the COVID-19 pandemic disease. (2) Methods: Herein, we tested the antiviral activity of anti-microbial and anti-inflammatory Food and Drug Administration (FDA)-approved drugs, commonly prescribed to relieve respiratory symptoms, against Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2), the viral causative agent of the COVID-19 pandemic. (3) Results: Of these FDA-approved antimicrobial drugs, Azithromycin, Niclosamide, and Nitazoxanide showed a promising ability to hinder the replication of a SARS-CoV-2 isolate, with IC50 of 0.32, 0.16, and 1.29 µM, respectively. We provided evidence that several antihistamine and anti-inflammatory drugs could partially reduce SARS-CoV-2 replication in vitro. Furthermore, this study showed that Azithromycin can selectively impair SARS-CoV-2 replication, but not the Middle East Respiratory Syndrome Coronavirus (MERS-CoV). A virtual screening study illustrated that Azithromycin, Niclosamide, and Nitazoxanide bind to the main protease of SARS-CoV-2 (Protein data bank (PDB) ID: 6lu7) in binding mode similar to the reported co-crystalized ligand. Also, Niclosamide displayed hydrogen bond (HB) interaction with the key peptide moiety GLN: 493A of the spike glycoprotein active site. (4) Conclusions: The results suggest that Piroxicam should be prescribed in combination with Azithromycin for COVID-19 patients. View Full-Text
Keywords: SARS-CoV-2; COVID-19; antiviral; virtual screening; drug repurposing SARS-CoV-2; COVID-19; antiviral; virtual screening; drug repurposing
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MDPI and ACS Style

Mostafa, A.; Kandeil, A.; A. M. M. Elshaier, Y.; Kutkat, O.; Moatasim, Y.; Rashad, A.A.; Shehata, M.; Gomaa, M.R.; Mahrous, N.; Mahmoud, S.H.; GabAllah, M.; Abbas, H.; Taweel, A.E.; Kayed, A.E.; Kamel, M.N.; Sayes, M.E.; Mahmoud, D.B.; El-Shesheny, R.; Kayali, G.; Ali, M.A. FDA-Approved Drugs with Potent In Vitro Antiviral Activity against Severe Acute Respiratory Syndrome Coronavirus 2. Pharmaceuticals 2020, 13, 443. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13120443

AMA Style

Mostafa A, Kandeil A, A. M. M. Elshaier Y, Kutkat O, Moatasim Y, Rashad AA, Shehata M, Gomaa MR, Mahrous N, Mahmoud SH, GabAllah M, Abbas H, Taweel AE, Kayed AE, Kamel MN, Sayes ME, Mahmoud DB, El-Shesheny R, Kayali G, Ali MA. FDA-Approved Drugs with Potent In Vitro Antiviral Activity against Severe Acute Respiratory Syndrome Coronavirus 2. Pharmaceuticals. 2020; 13(12):443. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13120443

Chicago/Turabian Style

Mostafa, Ahmed, Ahmed Kandeil, Yaseen A. M. M. Elshaier, Omnia Kutkat, Yassmin Moatasim, Adel A. Rashad, Mahmoud Shehata, Mokhtar R. Gomaa, Noura Mahrous, Sara H. Mahmoud, Mohamed GabAllah, Hisham Abbas, Ahmed E. Taweel, Ahmed E. Kayed, Mina N. Kamel, Mohamed E. Sayes, Dina B. Mahmoud, Rabeh El-Shesheny, Ghazi Kayali, and Mohamed A. Ali 2020. "FDA-Approved Drugs with Potent In Vitro Antiviral Activity against Severe Acute Respiratory Syndrome Coronavirus 2" Pharmaceuticals 13, no. 12: 443. https://0-doi-org.brum.beds.ac.uk/10.3390/ph13120443

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