Ebselen and Analogues: Pharmacological Properties and Synthetic Strategies for Their Preparation

Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities. It was the subject of several clinical trials and it is currently in c...

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Published inMolecules (Basel, Switzerland) Vol. 26; no. 14; p. 4230
Main Authors Santi, Claudio, Scimmi, Cecilia, Sancineto, Luca
Format Journal Article
LanguageEnglish
Published Switzerland MDPI AG 12.07.2021
MDPI
Subjects
Animals
Anti-Infective Agents - pharmacology
Antimicrobial agents
Antioxidants - pharmacology
antiviral
Antiviral Agents - pharmacology
Azoles - chemical synthesis
Azoles - chemistry
Azoles - pharmacology
Biomimetics - methods
bipolar disorders
Clinical trials
Coronaviruses
COVID-19
Cyclooxygenase Inhibitors - pharmacology
ebselen
Enzymes
Glutathione Peroxidase - metabolism
Glutathione Peroxidase - pharmacology
hearing loss
Humans
Isoindoles
Molecular Structure
Neuroprotective Agents - pharmacology
Organic chemistry
Organoselenium Compounds - chemical synthesis
Organoselenium Compounds - chemistry
Organoselenium Compounds - pharmacology
Potassium
Review
Selenium
Selenium - chemistry
Selenoproteins - chemical synthesis
Selenoproteins - pharmacology
selenorganic compounds
Severe acute respiratory syndrome coronavirus 2
Viral infections
bipolar disorders
ebselen
selenorganic compounds
hearing loss
antiviral
selenium chemistry
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Abstract Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities. It was the subject of several clinical trials and it is currently in clinical evaluation for the treatment of COVID-19 patients. Given our interest in the synthesis and pharmacological evaluation of selenorganic derivatives with this review, we aimed to collect all the papers focused on the biological evaluation of ebselen and its close analogues, covering the timeline between 2016 and most of 2021. Our analysis evidences that, even if it lacks specificity when tested in vitro, being able to bind to every reactive cysteine, it proved to be always well tolerated in vivo, exerting no sign of toxicity whatever the administered doses. Besides, looking at the literature, we realized that no review article dealing with the synthetic approaches for the construction of the benzo[d][1,2]-selenazol-3(2H)-one scaffold is available; thus, a section of the present review article is completely devoted to this specific topic.
AbstractList Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities. It was the subject of several clinical trials and it is currently in clinical evaluation for the treatment of COVID-19 patients. Given our interest in the synthesis and pharmacological evaluation of selenorganic derivatives with this review, we aimed to collect all the papers focused on the biological evaluation of ebselen and its close analogues, covering the timeline between 2016 and most of 2021. Our analysis evidences that, even if it lacks specificity when tested in vitro, being able to bind to every reactive cysteine, it proved to be always well tolerated in vivo, exerting no sign of toxicity whatever the administered doses. Besides, looking at the literature, we realized that no review article dealing with the synthetic approaches for the construction of the benzo[ ][1,2]-selenazol-3(2 )-one scaffold is available; thus, a section of the present review article is completely devoted to this specific topic.
Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities. It was the subject of several clinical trials and it is currently in clinical evaluation for the treatment of COVID-19 patients. Given our interest in the synthesis and pharmacological evaluation of selenorganic derivatives with this review, we aimed to collect all the papers focused on the biological evaluation of ebselen and its close analogues, covering the timeline between 2016 and most of 2021. Our analysis evidences that, even if it lacks specificity when tested in vitro, being able to bind to every reactive cysteine, it proved to be always well tolerated in vivo, exerting no sign of toxicity whatever the administered doses. Besides, looking at the literature, we realized that no review article dealing with the synthetic approaches for the construction of the benzo[ d ][1,2]-selenazol-3(2 H )-one scaffold is available; thus, a section of the present review article is completely devoted to this specific topic.
Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities. It was the subject of several clinical trials and it is currently in clinical evaluation for the treatment of COVID-19 patients. Given our interest in the synthesis and pharmacological evaluation of selenorganic derivatives with this review, we aimed to collect all the papers focused on the biological evaluation of ebselen and its close analogues, covering the timeline between 2016 and most of 2021. Our analysis evidences that, even if it lacks specificity when tested in vitro, being able to bind to every reactive cysteine, it proved to be always well tolerated in vivo, exerting no sign of toxicity whatever the administered doses. Besides, looking at the literature, we realized that no review article dealing with the synthetic approaches for the construction of the benzo[d][1,2]-selenazol-3(2H)-one scaffold is available; thus, a section of the present review article is completely devoted to this specific topic.Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities. It was the subject of several clinical trials and it is currently in clinical evaluation for the treatment of COVID-19 patients. Given our interest in the synthesis and pharmacological evaluation of selenorganic derivatives with this review, we aimed to collect all the papers focused on the biological evaluation of ebselen and its close analogues, covering the timeline between 2016 and most of 2021. Our analysis evidences that, even if it lacks specificity when tested in vitro, being able to bind to every reactive cysteine, it proved to be always well tolerated in vivo, exerting no sign of toxicity whatever the administered doses. Besides, looking at the literature, we realized that no review article dealing with the synthetic approaches for the construction of the benzo[d][1,2]-selenazol-3(2H)-one scaffold is available; thus, a section of the present review article is completely devoted to this specific topic.
Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several papers have appeared in literature claiming its biological activities. It was the subject of several clinical trials and it is currently in clinical evaluation for the treatment of COVID-19 patients. Given our interest in the synthesis and pharmacological evaluation of selenorganic derivatives with this review, we aimed to collect all the papers focused on the biological evaluation of ebselen and its close analogues, covering the timeline between 2016 and most of 2021. Our analysis evidences that, even if it lacks specificity when tested in vitro, being able to bind to every reactive cysteine, it proved to be always well tolerated in vivo, exerting no sign of toxicity whatever the administered doses. Besides, looking at the literature, we realized that no review article dealing with the synthetic approaches for the construction of the benzo[d][1,2]-selenazol-3(2H)-one scaffold is available; thus, a section of the present review article is completely devoted to this specific topic.
Author Scimmi, Cecilia
Santi, Claudio
Sancineto, Luca
AuthorAffiliation Group of Catalysis and Green Organic Chemistry, Department of Pharmaceutical Sciences, University of Perugia Via del Liceo 1, 06122 Perugia, Italy; claudio.santi@unipg.it (C.S.); cecilia.scimmi@studenti.unipg.it (C.S.)
AuthorAffiliation_xml – name: Group of Catalysis and Green Organic Chemistry, Department of Pharmaceutical Sciences, University of Perugia Via del Liceo 1, 06122 Perugia, Italy; claudio.santi@unipg.it (C.S.); cecilia.scimmi@studenti.unipg.it (C.S.)
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BackLink https://www.ncbi.nlm.nih.gov/pubmed/34299505$$D View this record in MEDLINE/PubMed
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Issue 14
Keywords bipolar disorders
ebselen
selenorganic compounds
hearing loss
antiviral
selenium chemistry
Language English
License https://creativecommons.org/licenses/by/4.0
Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/).
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Snippet Ebselen is the leader of selenorganic compounds, and starting from its identification as mimetic of the key antioxidant enzyme glutathione peroxidase, several...
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SubjectTerms Animals
Anti-Infective Agents - pharmacology
Antimicrobial agents
Antioxidants - pharmacology
antiviral
Antiviral Agents - pharmacology
Azoles - chemical synthesis
Azoles - chemistry
Azoles - pharmacology
Biomimetics - methods
bipolar disorders
Clinical trials
Coronaviruses
COVID-19
Cyclooxygenase Inhibitors - pharmacology
ebselen
Enzymes
Glutathione Peroxidase - metabolism
Glutathione Peroxidase - pharmacology
hearing loss
Humans
Isoindoles
Molecular Structure
Neuroprotective Agents - pharmacology
Organic chemistry
Organoselenium Compounds - chemical synthesis
Organoselenium Compounds - chemistry
Organoselenium Compounds - pharmacology
Potassium
Review
Selenium
Selenium - chemistry
Selenoproteins - chemical synthesis
Selenoproteins - pharmacology
selenorganic compounds
Severe acute respiratory syndrome coronavirus 2
Viral infections
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Title Ebselen and Analogues: Pharmacological Properties and Synthetic Strategies for Their Preparation
URI https://www.ncbi.nlm.nih.gov/pubmed/34299505
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Volume 26
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