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...

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Main Authors: Murad N. Abualhasan, Motasem Y. Al- Masri, Rufaida Manasara, Lana Yadak, Nael S. Abu-Hasan
Format: Article
Language:English
Published: Hindawi Limited 2020-01-01
Series:Scientifica
Online Access:http://dx.doi.org/10.1155/2020/9817502
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spelling doaj-9c6484d56f25478c9ee425222a1b71b82020-11-25T03:29:10ZengHindawi LimitedScientifica2090-908X2020-01-01202010.1155/2020/98175029817502Anti-Inflammatory and Anticoagulant Activities of Synthesized NSAID Prodrug EstersMurad N. Abualhasan0Motasem Y. Al- Masri1Rufaida Manasara2Lana Yadak3Nael S. Abu-Hasan4Faculty of Medicine and Health Sciences, Department of Pharmacy, An-Najah National University, Nablus, State of PalestineFaculty of Science, Department of Biology, An-Najah National University, Nablus, State of PalestineFaculty of Medicine and Health Sciences, Department of Pharmacy, An-Najah National University, Nablus, State of PalestineFaculty of Medicine and Health Sciences, Department of Pharmacy, An-Najah National University, Nablus, State of PalestineFaculty of Science, Department of Biology, An-Najah National University, Nablus, State of PalestineParacetamol 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.http://dx.doi.org/10.1155/2020/9817502
collection DOAJ
language English
format Article
sources DOAJ
author Murad N. Abualhasan
Motasem Y. Al- Masri
Rufaida Manasara
Lana Yadak
Nael S. Abu-Hasan
spellingShingle Murad N. Abualhasan
Motasem Y. Al- Masri
Rufaida Manasara
Lana Yadak
Nael S. Abu-Hasan
Anti-Inflammatory and Anticoagulant Activities of Synthesized NSAID Prodrug Esters
Scientifica
author_facet Murad N. Abualhasan
Motasem Y. Al- Masri
Rufaida Manasara
Lana Yadak
Nael S. Abu-Hasan
author_sort Murad N. Abualhasan
title Anti-Inflammatory and Anticoagulant Activities of Synthesized NSAID Prodrug Esters
title_short 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_sort anti-inflammatory and anticoagulant activities of synthesized nsaid prodrug esters
publisher Hindawi Limited
series Scientifica
issn 2090-908X
publishDate 2020-01-01
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.
url http://dx.doi.org/10.1155/2020/9817502
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AT lanayadak antiinflammatoryandanticoagulantactivitiesofsynthesizednsaidprodrugesters
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