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Anti-Inflammatory and Anticoagulant Activities of Synthesized NSAID Prodrug Esters
Paracetamol with ibuprofen or with naproxen are frequently prescribed by doctors in combination. It was found that patients using a combination of NSAID like acetaminophen and ibuprofen experienced less pain. Patients are more compliant if these two drugs are combined in an ester form and given in o...
Autores principales: | , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Hindawi
2020
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7271289/ https://www.ncbi.nlm.nih.gov/pubmed/33093967 http://dx.doi.org/10.1155/2020/9817502 |
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author | Abualhasan, Murad N. Al- Masri, Motasem Y. Manasara, Rufaida Yadak, Lana Abu-Hasan, Nael S. |
author_facet | Abualhasan, Murad N. Al- Masri, Motasem Y. Manasara, Rufaida Yadak, Lana Abu-Hasan, Nael S. |
author_sort | Abualhasan, Murad N. |
collection | PubMed |
description | Paracetamol with ibuprofen or with naproxen are frequently prescribed by doctors in combination. It was found that patients using a combination of NSAID like acetaminophen and ibuprofen experienced less pain. Patients are more compliant if these two drugs are combined in an ester form and given in one dosage form. The esterified prodrugs are hydrolyzed in humans to their active forms. In this study, two esters of paracetamol combined with ibuprofen and naproxen were synthesized as prodrugs. The physiochemical properties of these products were identified. Moreover, the bioactivities of these prodrugs were tested for its anti-inflammatory and anticoagulant activities. The results showed an improved COX inhibition and anticoagulant activity compared with their parent drugs. The synthesized drugs are expected to improve patient's compliance in terms of administration frequency and will have better pharmacokinetic properties with fewer side effects. |
format | Online Article Text |
id | pubmed-7271289 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2020 |
publisher | Hindawi |
record_format | MEDLINE/PubMed |
spelling | pubmed-72712892020-10-21 Anti-Inflammatory and Anticoagulant Activities of Synthesized NSAID Prodrug Esters Abualhasan, Murad N. Al- Masri, Motasem Y. Manasara, Rufaida Yadak, Lana Abu-Hasan, Nael S. Scientifica (Cairo) Research Article Paracetamol with ibuprofen or with naproxen are frequently prescribed by doctors in combination. It was found that patients using a combination of NSAID like acetaminophen and ibuprofen experienced less pain. Patients are more compliant if these two drugs are combined in an ester form and given in one dosage form. The esterified prodrugs are hydrolyzed in humans to their active forms. In this study, two esters of paracetamol combined with ibuprofen and naproxen were synthesized as prodrugs. The physiochemical properties of these products were identified. Moreover, the bioactivities of these prodrugs were tested for its anti-inflammatory and anticoagulant activities. The results showed an improved COX inhibition and anticoagulant activity compared with their parent drugs. The synthesized drugs are expected to improve patient's compliance in terms of administration frequency and will have better pharmacokinetic properties with fewer side effects. Hindawi 2020-05-23 /pmc/articles/PMC7271289/ /pubmed/33093967 http://dx.doi.org/10.1155/2020/9817502 Text en Copyright © 2020 Murad N. Abualhasan et al. http://creativecommons.org/licenses/by/4.0/ This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. |
spellingShingle | Research Article Abualhasan, Murad N. Al- Masri, Motasem Y. Manasara, Rufaida Yadak, Lana Abu-Hasan, Nael S. Anti-Inflammatory and Anticoagulant Activities of Synthesized NSAID Prodrug Esters |
title | Anti-Inflammatory and Anticoagulant Activities of Synthesized NSAID Prodrug Esters |
title_full | Anti-Inflammatory and Anticoagulant Activities of Synthesized NSAID Prodrug Esters |
title_fullStr | Anti-Inflammatory and Anticoagulant Activities of Synthesized NSAID Prodrug Esters |
title_full_unstemmed | Anti-Inflammatory and Anticoagulant Activities of Synthesized NSAID Prodrug Esters |
title_short | Anti-Inflammatory and Anticoagulant Activities of Synthesized NSAID Prodrug Esters |
title_sort | anti-inflammatory and anticoagulant activities of synthesized nsaid prodrug esters |
topic | Research Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7271289/ https://www.ncbi.nlm.nih.gov/pubmed/33093967 http://dx.doi.org/10.1155/2020/9817502 |
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