Synthesis of Novel Esters of Mefenamic Acid with Pronounced Anti-nociceptive Effects and a Proposed Activity on GABA, Opioid and Glutamate Receptors

Ayoub, Rami; Jarrar, Qais; Ali, Dalia Khalil; Moshawih, Said; Jarrar, Yazun; Hakim, Muhammad Nazrul; Zakaria, Zuhaina

doi:10.1016/j.ejps.2021.105865

Cited by 8 publications

(6 citation statements)

References 47 publications

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“…Therefore, the recent trend in MFA development is to reduce its CNS toxicity by masking the carboxylic acid moiety. A previous study demonstrated that binding MFA with alpha-tocopherol reduced the CNS toxicity by increasing the latency to the convulsions (15). In this study, the potential risk of CNS toxicity of HEMA was evaluated in comparison to that of MFA.…”

Section: Acetic Acid-induced Writhing Response Testmentioning

confidence: 99%

“…Structurally, the hydroxyethyl moiety of HEMA binds via an ester bond to the carboxylic acid group of MFA, which is responsible for the development of seizure in MFA treatment (15). The ester bond of HEMA showed strong resistance to enzymatic degradation and exhibited high stability in the plasma and various buffer solutions (16,17).…”

Section: The Toxicity and Therapeutic …mentioning

confidence: 99%

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The Toxicity and Therapeutic Efficacy of Mefenamic Acid and its Hydroxyethyl Ester in Mice: In Vivo Comparative Study: A promising Drug Derivative

Adel

Jarrar

Ayoub

et al. 2022

Jordan j. pharm. sci.

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Background: Hydroxyethyl Ester of Mefenamic acid (HEMA), which is an available derivative of mefenamic acid (MFA) in the literature, was shown to exert a strong resistance to enzymatic hydrolysis in various buffer solutions as well as in the plasma. However, there are no studies yet that investigate the biological effects of HEMA as a possible active drug in-vivo. This study provides an in-vivo investigation of the efficacy and toxicity of HEMA in comparison to those of a related drug, MFA, that has a similar chemical structure. Methods: Acute toxicity evaluations were conducted in various groups of mice following administration of high equimolar doses of HEMA and MFA and were measured at various parameters including the percentage of catalepsy, seizure score, percentage of clonic-tonic seizure and death, grimace scale score (GSS) and locomotor activity. In addition, the anti-inflammatory and anti-nociceptive effects of HEMA were evaluated in the carrageenan-induced paw edema test and acetic acid-induced writhing test, respectively. Results: The findings of this study revealed that the percentage of catalepsy, clonic-tonic seizure and death as well as seizure and grimace scale scores were lower in mice treated with HEMA than those treated with equimolar doses of MFA. In addition, treatment with HEMA caused a comparable anti-inflammatory activity in the carrageenan-induced paw edema test and a significantly (p<0.05) higher anti-nociceptive effect in the acetic acid-induced writhing test than that of MFA. Conclusion: Results obtained from this study may indicate that HEMA has superior therapeutic advantages for the management of acute and inflammatory events with a less potential risk of neuromuscular adverse effects.

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Section: Acetic Acid-induced Writhing Response Testmentioning

confidence: 99%

Section: The Toxicity and Therapeutic …mentioning

confidence: 99%

The Toxicity and Therapeutic Efficacy of Mefenamic Acid and its Hydroxyethyl Ester in Mice: In Vivo Comparative Study: A promising Drug Derivative

Adel

Jarrar

Ayoub

et al. 2022

Jordan j. pharm. sci.

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“…According to (Ayoub et al, 2021) Agrarian reform in forest areas is a policy to achieve justice related to assets and access whose sources come from forest areas through the PTKH settlement scheme in accordance with the direction of Presidential Regulation No. 88 of 2017.…”

Section: Land Policy For Agrarian Reform Objects (Tora) In the 2015-2...mentioning

confidence: 99%

Implementation of Land Tenure Settlement in Forest Area as a Land Object of Agrarian Reform in Central Sulawesi Province

Hasibuan¹,

Rachman²

2022

IJRIAS

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The allocation and utilization of forest resources is closely related to forest land tenure policies. Problems related to overlapping claims to forest areas are basically related to the existence of various products that can be utilized from forest resources and other potential natural resources. This encourages various parties to "participate" in the utilization and use of forest areas, which in the end gives rise to disputes or disagreements over resources that lead to forest resource conflicts. The research focus is on the Implementation of Land Settlement in Forest Areas (PTKH) in Central Sulawesi Province. The study used a qualitative approach through field observations and in-depth interviews. Data analysis was carried out qualitatively-descriptively. The results show that Agrarian Reform is a constitutional mandate to provide a sense of justice in order to create prosperity for the people, and resolve forest area problems and conflicts. Completion of the ongoing control and use of land in forest areas through PTKH activities to provide a sense of justice in order to create prosperity for the people, and resolve forest area problems and conflicts. The implementation of PTKH is in the form of legalizing assets through the release of forest areas and legalizing access through social forestry licensing in Central Sulawesi Province with recommendations for settlement patterns for changing boundaries (asset rights) and social forestry licensing patterns (access rights).

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“…In drug chemistry, Mefenamic acid is known as anthranilic acid derivatives brand of nonsteroidal anti-inflammatory drugs (NSAID) that inhibits the synthesis of pain-causing prostaglandins and is useful as pain reliever [1,2]. The unique structure of mefenamic acid synthetically leads to a large number of the derivatives class of (NSAID), which based on pharmacological findings represent their interference with prostaglandin biosynthesis.…”

Section: Introductionmentioning

confidence: 99%

Untitled

2023

J. Med. Chem. Sci.

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Synthesis of Novel Esters of Mefenamic Acid with Pronounced Anti-nociceptive Effects and a Proposed Activity on GABA, Opioid and Glutamate Receptors

Cited by 8 publications

References 47 publications

The Toxicity and Therapeutic Efficacy of Mefenamic Acid and its Hydroxyethyl Ester in Mice: In Vivo Comparative Study: A promising Drug Derivative

The Toxicity and Therapeutic Efficacy of Mefenamic Acid and its Hydroxyethyl Ester in Mice: In Vivo Comparative Study: A promising Drug Derivative

Implementation of Land Tenure Settlement in Forest Area as a Land Object of Agrarian Reform in Central Sulawesi Province

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