Jessica A. Downs-Bowen

1′-Cyanocytidine-5′-isobutyryl is a potent SARS-CoV-2 inhibitor in culture and infected Syrian hamsters

Franck Amblard, Mahesh Kasthuri, Julia C. LeCher, Sijia Tao et autres

The severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) and COVID-19 epidemic is relatively under control due to the rapid development and deployment of vaccines and a few drugs. However, challenges persist, as new variants and issues with vaccine durability may compromise their …

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Cannabinoid-Inspired Inhibitors of the SARS-CoV-2 Coronavirus 2′-O-Methyltransferase (2′-O-MTase) Non-Structural Protein (Nsp10–16)

Menny M. Benjamin, George S. Hanna, Cody F. Dickinson, Yeun‐Mun Choo et autres

The design and synthesis of antiviral compounds were guided by computationally predicted data against highly conserved non-structural proteins (Nsps) of the SARS-CoV-2 coronavirus. Chromenephenylmethanone-1 (CPM-1), a novel biphenylpyran (BPP), was selected from a unique natural product library based on in silico docking …

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Why Certain Repurposed Drugs Are Unlikely to Be Effective Antivirals to Treat SARS-CoV-2 Infections

Selwyn J. Hurwitz, Ramyani De, Julia C. LeCher, Jessica A. Downs-Bowen et autres

Most repurposed drugs have proved ineffective for treating COVID-19. We evaluated median effective and toxic concentrations (EC50, CC50) of 49 drugs, mostly from previous clinical trials, in Vero cells. Ratios of reported unbound peak plasma concentrations, (Cmax)/EC50, were used to predict the …

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Synthesis and biological evaluation of novel peptidomimetic inhibitors of the coronavirus 3C-like protease

Franck Amblard, Julia C. LeCher, Ramyani De, Shaoman Zhou et autres

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Synthesis and evaluation of highly potent HBV capsid assembly modulators (CAMs)

Franck Amblard, Zhe Chen, JOHN R. WISEMAN, Shaoman Zhou et autres

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Synthesis of 4′-Substituted Carbocyclic Uracil Derivatives and Their Monophosphate Prodrugs as Potential Antiviral Agents

Nicolas Biteau, Sarah Amichai, Niloufar Azadi, Ramyani De et autres

Over the past decades, both 4'-modified nucleoside and carbocyclic nucleoside analogs have been under the spotlight as several compounds from either family showed anti-HIV, HCV, RSV or SARS-CoV-2 activity. Herein, we designed compounds combining these two features and report the synthesis of …

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Botanical inhibitors of SARS-CoV-2 viral entry: a phylogenetic perspective

Caitlin J. Risener, Sunmin Woo, Tharanga Samarakoon, Marco Caputo et autres

Abstract Throughout the SARS-CoV-2 pandemic, the use of botanical dietary supplements in the United States has increased, yet their safety and efficacy against COVID-19 remains underexplored. The Quave Natural Product Library is a phylogenetically diverse collection of botanical and fungal natural product …

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Discovery of a 2′-Fluoro,2′-Bromouridine Phosphoramidate Prodrug Exhibiting Anti-Yellow Fever Virus Activity in Culture and in Mice

Julia C. LeCher, Keivan Zandi, Vivian Vasconcelos Costa, Franck Amblard et autres

Yellow fever virus (YFV) is a potentially lethal, zoonotic, blood-borne flavivirus transmitted to humans and non-human primates by mosquitoes. Owing to multiple deadly epidemics, the WHO classifies YFV as a "high impact, high threat disease" with resurgent epidemic potential. At present, there …

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Synthesis of Novel N4-Hydrocytidine Analogs as Potential Anti-SARS-CoV-2 Agents

Franck Amblard, Julia C. LeCher, Ramyani De, Chengwei Li et autres

Coronavirus disease 2019 (COVID-19) is an emerging global pandemic with severe morbidity and mortality caused by the severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). Molnupiravir, an ester prodrug form of N4-hydroxycytidine (NHC), was recently emergency-use approved for the treatment of early SARS-CoV-2 …

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Identification of Botanical Viral Entry Inhibitors for SARS‐CoV‐2

Caitlin J. Risener, Sunmin Woo, Tharamangala Samarakoon, Marco Caputo et autres

The examination of biodiversity across the world has historically been a critical part of drug development and led to the discovery of common medications for many medical issues including pain management, cancer, heart disease, and infections. During the SARS‐CoV‐2 pandemic, the use …

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Comparison of anti-SARS-CoV-2 activity and intracellular metabolism of remdesivir and its parent nucleoside

Sijia Tao, Keivan Zandi, Leda Bassit, Yee Tsuey Ong et autres

Remdesivir, a monophosphate prodrug of nucleoside analog GS-441524, is widely used for the treatment of moderate to severe COVID-19. It has been suggested to use GS-441524 instead of remdesivir in the clinic and in new inhalation formulations. Thus, we compared the anti-SARS-CoV-2 …

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Repurposing Nucleoside Analogs for Human Coronaviruses

Keivan Zandi, Franck Amblard, Katie Musall, Jessica A. Downs-Bowen et autres

Coronavirus disease 2019 (COVID-19) is a serious illness caused by severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2 or CoV-2). Some reports claimed certain nucleoside analogs to be active against CoV-2 and thus needed confirmation. Here, we evaluated a panel of compounds and …

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