Cargando…

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...

Descripción completa

Detalles Bibliográficos
Autores principales: Abualhasan, Murad N., Al- Masri, Motasem Y., Manasara, Rufaida, Yadak, Lana, Abu-Hasan, Nael S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Hindawi 2020
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
_version_ 1783542065290805248
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
work_keys_str_mv AT abualhasanmuradn antiinflammatoryandanticoagulantactivitiesofsynthesizednsaidprodrugesters
AT almasrimotasemy antiinflammatoryandanticoagulantactivitiesofsynthesizednsaidprodrugesters
AT manasararufaida antiinflammatoryandanticoagulantactivitiesofsynthesizednsaidprodrugesters
AT yadaklana antiinflammatoryandanticoagulantactivitiesofsynthesizednsaidprodrugesters
AT abuhasannaels antiinflammatoryandanticoagulantactivitiesofsynthesizednsaidprodrugesters