The active metabolite of leflunomide, A77 1726, increases proliferation of human synovial fibroblasts in presence of IL-1β and TNF-α

Magne, David; Mézin, Françoise; Palmer, Gaby; Guerne, Pierre‐André

doi:10.1007/s00011-006-5196-x

Cited by 8 publications

(4 citation statements)

References 34 publications

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“…This approach was next applied to the production of the active metabolite of Leflunomide,20 which was approved for commercialisation under the name Teriflunomide (trade name Aubagio) by the FDA in 2012 for the treatment of multiple sclerosis 21. Indeed, the treatment of 5‐methyl‐4‐isoxazolecarboxylic acid with CDI followed by mixing with 4‐(trifluoromethyl)aniline hydrochloride during 5 h and then with water during 5 min produced Leflunomide as a fine suspension in water (Scheme ).…”

Section: Resultsmentioning

confidence: 99%

Comprehensive Study of the Organic‐Solvent‐Free CDI‐Mediated Acylation of Various Nucleophiles by Mechanochemistry

Métro

Bonnamour

Reidon

et al. 2015

Chemistry A European J

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Acylation reactions are ubiquitous in the synthesis of natural products and biologically active compounds. Unfortunately, these reactions often require the use of large quantities of volatile and/or toxic solvents, either for the reaction, purification or isolation of the products. Herein we describe and discuss the possibility of completely eliminating the use of organic solvents for the synthesis, purification and isolation of products resulting from the acylation of amines and other nucleophiles. Thus, utilisation of N,N'-carbonyldiimidazole (CDI) allows efficient coupling between carboxylic acids and various nucleophiles under solvent-free mechanical agitation, and water-assisted grinding enables both the purification and isolation of pure products. Critical parameters such as the physical state and water solubility of the products, milling material, type of agitation (vibratory or planetary) as well as contamination from wear are analysed and discussed. In addition, original organic-solvent-free conditions are proposed to overcome the limitations of this approach. The calculations of various green metrics are included, highlighting the particularly low environmental impact of this strategy.

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Section: Resultsmentioning

confidence: 99%

Comprehensive Study of the Organic‐Solvent‐Free CDI‐Mediated Acylation of Various Nucleophiles by Mechanochemistry

Métro

Bonnamour

Reidon

et al. 2015

Chemistry A European J

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“…In another study; IL-36 receptor is expressed in human synovial fibroblast and human articular chondrocytes but there was no increase in IL36β levels in the inflamed human and mouse joints. Serum IL-36β levels were also similar in healthy controls with rheumatoid arthritis, osteoarthritis 29 . In another study which compared RA and psoriatic arthritis showed that IL-36α is expressed at similar levels in the synovium while psoriatic arthritis synovium expressed less IL-36Ra compared with RA.…”

Section: Discussionmentioning

confidence: 62%

Serum Levels of Interleukin-36 Alpha and Interleukin-36 Receptor Antagonist In Behcet’s Syndrome

Ünsal

Çerçi

Açıkgöz

et al. 2021

Aktuelle Rheumatologie

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Background Behcet’s syndrome (BS) is a systemic vasculitic disorder. This study aimed to investigate the levels of serum IL-36α and IL-36Ra in patients with BS. Material and Methods A total of 80 subjects (60 BS patients and 20 healthy controls [HC]) were included. Results The median IL-36α level was 0.11 ng/ml in the BS group and 0.09 ng/ml in the HC group (p=0.058). The mean IL-36Ra level was 13.62 pg/ml in the BS group and 13.26 pg/ml in the HC group (p=0.348). Serum IL-36Ra levels of the active group were significantly higher (p=0.037). Patients with oral ulcers and central nervous system involvement had higher serum IL36Ra levels. In the BS group, a positive correlation was found between serum IL-36Ra and CRP. In a multivariate analysis, the IL-36Ra level (OR=1.067; 95% CI=1.001–1.137; p=0.045) was independently associated with disease activity. Conclusion According to these findings, it is not clear whether such a slight difference is clinically significant, but they suggest that the IL-36 cytokine family may play a role in the course of the disease.

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“…Препарат является ингибитором митохондриального фермента дигидроортатдегидрогеназы (ДГО-ДГ), который необходим для синтеза пиримидина. Таким образом, под действием препарата снижается репликация аутореактивных лимфоцитов [34].…”

Section: терифлуномидunclassified

COVID-19 Features in Patients with Multiple Sclerosis: Main Approaches to Their Management, Treatment, and Vaccination

Malko

Бисага

Топузова

et al. 2023

Annals of Clinical and Experimental Neurology

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The COVID-19 pandemic calls for correct and evidence-based decisions regarding management and treatment of patients with multiple sclerosis. Information on researches, clinical cases, and recommendations for treatment of such patients during the pandemic should be classified. We report COVID-19 features in patients with multiple sclerosis, risk factors for infection and development of severe disease. We also describe management strategies for multiple sclerosis: from relapse treatment to the selection of disease-modifying therapies focusing on patients safety. We analyze the latest observational and comparative studies, clinical cases of multiple sclerosis patients vaccination and demyelinating disease onset after COVID-19 or vaccination.

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The active metabolite of leflunomide, A77 1726, increases proliferation of human synovial fibroblasts in presence of IL-1β and TNF-α

Abstract: A77 1726 displays proliferative effects in presence of IL-1beta and TNF-alpha. Further elucidation of involved mechanisms may prove useful for the utilization of leflunomide, the development of related compounds or elaboration of new therapeutic strategies.

Cited by 8 publications

References 34 publications

Comprehensive Study of the Organic‐Solvent‐Free CDI‐Mediated Acylation of Various Nucleophiles by Mechanochemistry

Comprehensive Study of the Organic‐Solvent‐Free CDI‐Mediated Acylation of Various Nucleophiles by Mechanochemistry

Serum Levels of Interleukin-36 Alpha and Interleukin-36 Receptor Antagonist In Behcet’s Syndrome

COVID-19 Features in Patients with Multiple Sclerosis: Main Approaches to Their Management, Treatment, and Vaccination

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