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FDA-Approved Oximes and Their Significance in Medicinal Chemistry

Despite the scientific advancements, organophosphate (OP) poisoning continues to be a major threat to humans, accounting for nearly one million poisoning cases every year leading to at least 20,000 deaths worldwide. Oximes represent the most important class in medicinal chemistry, renowned for their...

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Autores principales: Dhuguru, Jyothi, Zviagin, Eugene, Skouta, Rachid
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8779982/
https://www.ncbi.nlm.nih.gov/pubmed/35056123
http://dx.doi.org/10.3390/ph15010066
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author Dhuguru, Jyothi
Zviagin, Eugene
Skouta, Rachid
author_facet Dhuguru, Jyothi
Zviagin, Eugene
Skouta, Rachid
author_sort Dhuguru, Jyothi
collection PubMed
description Despite the scientific advancements, organophosphate (OP) poisoning continues to be a major threat to humans, accounting for nearly one million poisoning cases every year leading to at least 20,000 deaths worldwide. Oximes represent the most important class in medicinal chemistry, renowned for their widespread applications as OP antidotes, drugs and intermediates for the synthesis of several pharmacological derivatives. Common oxime based reactivators or nerve antidotes include pralidoxime, obidoxime, HI-6, trimedoxime and methoxime, among which pralidoxime is the only FDA-approved drug. Cephalosporins are β-lactam based antibiotics and serve as widely acclaimed tools in fighting bacterial infections. Oxime based cephalosporins have emerged as an important class of drugs with improved efficacy and a broad spectrum of anti-microbial activity against Gram-positive and Gram-negative pathogens. Among the several oxime based derivatives, cefuroxime, ceftizoxime, cefpodoxime and cefmenoxime are the FDA approved oxime-based antibiotics. Given the pharmacological significance of oximes, in the present paper, we put together all the FDA-approved oximes and discuss their mechanism of action, pharmacokinetics and synthesis.
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spelling pubmed-87799822022-01-22 FDA-Approved Oximes and Their Significance in Medicinal Chemistry Dhuguru, Jyothi Zviagin, Eugene Skouta, Rachid Pharmaceuticals (Basel) Review Despite the scientific advancements, organophosphate (OP) poisoning continues to be a major threat to humans, accounting for nearly one million poisoning cases every year leading to at least 20,000 deaths worldwide. Oximes represent the most important class in medicinal chemistry, renowned for their widespread applications as OP antidotes, drugs and intermediates for the synthesis of several pharmacological derivatives. Common oxime based reactivators or nerve antidotes include pralidoxime, obidoxime, HI-6, trimedoxime and methoxime, among which pralidoxime is the only FDA-approved drug. Cephalosporins are β-lactam based antibiotics and serve as widely acclaimed tools in fighting bacterial infections. Oxime based cephalosporins have emerged as an important class of drugs with improved efficacy and a broad spectrum of anti-microbial activity against Gram-positive and Gram-negative pathogens. Among the several oxime based derivatives, cefuroxime, ceftizoxime, cefpodoxime and cefmenoxime are the FDA approved oxime-based antibiotics. Given the pharmacological significance of oximes, in the present paper, we put together all the FDA-approved oximes and discuss their mechanism of action, pharmacokinetics and synthesis. MDPI 2022-01-04 /pmc/articles/PMC8779982/ /pubmed/35056123 http://dx.doi.org/10.3390/ph15010066 Text en © 2022 by the authors. 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/).
spellingShingle Review
Dhuguru, Jyothi
Zviagin, Eugene
Skouta, Rachid
FDA-Approved Oximes and Their Significance in Medicinal Chemistry
title FDA-Approved Oximes and Their Significance in Medicinal Chemistry
title_full FDA-Approved Oximes and Their Significance in Medicinal Chemistry
title_fullStr FDA-Approved Oximes and Their Significance in Medicinal Chemistry
title_full_unstemmed FDA-Approved Oximes and Their Significance in Medicinal Chemistry
title_short FDA-Approved Oximes and Their Significance in Medicinal Chemistry
title_sort fda-approved oximes and their significance in medicinal chemistry
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8779982/
https://www.ncbi.nlm.nih.gov/pubmed/35056123
http://dx.doi.org/10.3390/ph15010066
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