ArticleBioorganic & medicinal chemistry letters2021
Application of niclosamide and analogs as small molecule inhibitors of Zika virus and SARS-CoV-2 infection.
Article in Bioorganic & medicinal chemistry letters, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed.
- An Open Label, Cross-Over Phase 1 Study to Determine the Safety, Tolerability and Pharmacokinetics of Multiple Oral Doses of Niclosamide Under Fed and Fasted Conditions in Healthy Volunteers.Journal of clinical medicine · 2026Article
- Discovery of Niclosamide Analogs with Potent Mitochondrial Uncoupling Activity and Reduced Mitochondrial Inhibition-Associated Toxicity.ACS medicinal chemistry letters · 2026Article
- Successive paired electrochemical late-stage modification of niclosamide a common anthelmintic drug. A green protocol for the synthesis of new drug-like molecules.RSC advances · 2025Article
- Harnessing Nanohybridized Niclosamide for Precision Mpox Therapeutics.Advanced healthcare materials · 2025Review
- On the origins of SARS-CoV-2 main protease inhibitors.RSC medicinal chemistry · 2024Review
- Revisiting Niclosamide Formulation Approaches - a Pathway Toward Drug Repositioning.Drug design, development and therapy · 2024Review
- Microwave-assisted chemoselective synthesis and photophysical properties of 2-arylazo-biphenyl-4-carboxamides from hydrazonals.RSC advances · 2023Article
- Therapeutic potential of salicylamide derivatives for combating viral infections.Medicinal research reviews · 2023Review
- Use of physiological based pharmacokinetic modeling for cross-species prediction of pharmacokinetic and tissue distribution profiles of a novel niclosamide prodrug.Frontiers in pharmacology · 2023Article
- Niclosamide-loaded nanoparticles disrupt Candida biofilms and protect mice from mucosal candidiasis.PLoS biology · 2022Article
- Design, synthesis and biological evaluations of niclosamide analogues against SARS-CoV-2.European journal of medicinal chemistry · 2022Article
- Efficacy of Ceftazidime and Cefepime in the Management of COVID-19 Patients: Single Center Report from Egypt.Antibiotics (Basel, Switzerland) · 2021Article
- Nitro-Deficient Niclosamide Confers Reduced Genotoxicity and Retains Mitochondrial Uncoupling Activity for Cancer Therapy.International journal of molecular sciences · 2021Article
- Screening Potential Drugs for COVID-19 Based on Bound Nuclear Norm Regularization.Frontiers in genetics · 2021Article
Corrections and comments
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Authors and funding
24 authors.
Funding
Abstract
Zika virus has emerged as a potential threat to human health globally. A previous drug repurposing screen identified the approved anthelminthic drug niclosamide as a small molecule inhibitor of Zika virus infection. However, as antihelminthic drugs are generally designed to have low absorption when dosed orally, the very limited bioavailability of niclosamide will likely hinder its potential direct repurposing as an antiviral medication. Here, we conducted SAR studies focusing on the anilide and salicylic acid regions of niclosamide to improve physicochemical properties such as microsomal metabolic stability, permeability and solubility. We found that the 5-bromo substitution in the salicylic acid region retains potency while providing better drug-like properties. Other modifications in the anilide region with 2'-OMe and 2'-H substitutions were also advantageous. We found that the 4'-NO
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