A Small Molecule That In Vitro Neutralizes Infection of SARS-CoV-2 and Its Most Infectious Variants, Delta, and Omicron

The COVID-19 pandemic has underscored the urgent need to develop highly potent and safe medications that are complementary to the role of vaccines. Specifically, it has exhibited the need for orally bioavailable broad-spectrum antivirals that are able to be quickly deployed against newly emerging vi...

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Published in:	Biomedicines Vol. 11; no. 3; p. 916
Main Authors:	Reyes-Alcaraz, Arfaxad, Qasim, Hanan, Merlinsky, Elizabeth, Fox, Glenn, Islam, Tasneem, Medina, Bryan, Schwartz, Robert J, Craft, Jr, John W, McConnell, Bradley K
Format:	Journal Article
Language:	English
Published:	Switzerland MDPI AG 01-03-2023 MDPI
Subjects:	Antiviral agents Brief Report Coronaviruses COVID-19 COVID-19 vaccines Delta Disease transmission Infections Omicron Plasmids Proteins SARS-CoV-2 spike protein Severe acute respiratory syndrome coronavirus 2 Viruses United States United States > US COVID-19 SARS-CoV-2 spike protein Omicron Delta
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Abstract	The COVID-19 pandemic has underscored the urgent need to develop highly potent and safe medications that are complementary to the role of vaccines. Specifically, it has exhibited the need for orally bioavailable broad-spectrum antivirals that are able to be quickly deployed against newly emerging viral pathogens. The Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV2) and its variants Delta and Omicron are still a major threat to patients of all ages. In this brief report, we describe that the small molecule CD04872SC was able to neutralize SARS-CoV2 infection with a half-maximal effective concentration (EC50) = 248 μM. Serendipitously, we also were able to observe that CD04872SC inhibited the infection of the SARS-CoV-2 variants; Delta (EC50 = 152 μM) and Omicron (EC50 = 308 μM). These properties may define CD04872SC as a potential broad-spectrum candidate lead for the development of treatments for COVID-19.
AbstractList	The COVID-19 pandemic has underscored the urgent need to develop highly potent and safe medications that are complementary to the role of vaccines. Specifically, it has exhibited the need for orally bioavailable broad-spectrum antivirals that are able to be quickly deployed against newly emerging viral pathogens. The Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV2) and its variants Delta and Omicron are still a major threat to patients of all ages. In this brief report, we describe that the small molecule CD04872SC was able to neutralize SARS-CoV2 infection with a half-maximal effective concentration (EC50) = 248 μM. Serendipitously, we also were able to observe that CD04872SC inhibited the infection of the SARS-CoV-2 variants; Delta (EC50 = 152 μM) and Omicron (EC50 = 308 μM). These properties may define CD04872SC as a potential broad-spectrum candidate lead for the development of treatments for COVID-19.
Audience	Academic
Author	Reyes-Alcaraz, Arfaxad Medina, Bryan Islam, Tasneem Qasim, Hanan Fox, Glenn Schwartz, Robert J Merlinsky, Elizabeth Craft, Jr, John W McConnell, Bradley K
AuthorAffiliation	2 Rogers State University, 1701 W. Will Rogers Blvd., Claremore, OK 74017, USA 3 Department of Biology and Biochemistry, University of Houston, Houston, TX 77204, USA 1 Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, USA; areyesa2@central.uh.edu (A.R.-A.)
AuthorAffiliation_xml	– name: 1 Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, USA; areyesa2@central.uh.edu (A.R.-A.) – name: 3 Department of Biology and Biochemistry, University of Houston, Houston, TX 77204, USA – name: 2 Rogers State University, 1701 W. Will Rogers Blvd., Claremore, OK 74017, USA
Author_xml	– sequence: 1 givenname: Arfaxad surname: Reyes-Alcaraz fullname: Reyes-Alcaraz, Arfaxad organization: Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, USA – sequence: 2 givenname: Hanan surname: Qasim fullname: Qasim, Hanan organization: Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, USA – sequence: 3 givenname: Elizabeth surname: Merlinsky fullname: Merlinsky, Elizabeth organization: Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, USA – sequence: 4 givenname: Glenn surname: Fox fullname: Fox, Glenn organization: Rogers State University, 1701 W. Will Rogers Blvd., Claremore, OK 74017, USA – sequence: 5 givenname: Tasneem orcidid: 0009-0000-3786-9621 surname: Islam fullname: Islam, Tasneem organization: Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, USA – sequence: 6 givenname: Bryan orcidid: 0000-0002-4502-1222 surname: Medina fullname: Medina, Bryan organization: Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, USA – sequence: 7 givenname: Robert J surname: Schwartz fullname: Schwartz, Robert J organization: Department of Biology and Biochemistry, University of Houston, Houston, TX 77204, USA – sequence: 8 givenname: John W surname: Craft, Jr fullname: Craft, Jr, John W organization: Department of Biology and Biochemistry, University of Houston, Houston, TX 77204, USA – sequence: 9 givenname: Bradley K surname: McConnell fullname: McConnell, Bradley K organization: Department of Pharmacological and Pharmaceutical Sciences, College of Pharmacy, University of Houston, Houston, TX 77204, USA
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SubjectTerms	Antiviral agents Brief Report Coronaviruses COVID-19 COVID-19 vaccines Delta Disease transmission Infections Omicron Plasmids Proteins SARS-CoV-2 spike protein Severe acute respiratory syndrome coronavirus 2 Viruses
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Title	A Small Molecule That In Vitro Neutralizes Infection of SARS-CoV-2 and Its Most Infectious Variants, Delta, and Omicron
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