Towards the Development of Dual Hypouricemic and Anti-inflammatory Candidates: Design, Synthesis, Stability Studies and Biological Evaluation of Some Mutual Ester Prodrugs of Febuxostat-NSAIDs

Rashad, Aya Y; Daabees, Hoda G.; Elagawany, Mohamed; Shahin, Mohamed A.; Moneim, Ahmed E. Abdel; Rostom, Sherif A. F.

doi:10.1016/j.bioorg.2023.106502

Cited by 8 publications

(1 citation statement)

References 46 publications

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“…The cardiovascular implications of febuxostat extend beyond its primary function of managing hyperuricemia and gout. Notably, the medication has demonstrated a favorable cardiovascular safety profile, making it a compelling candidate for further exploration in the field of cardiac care [27].…”

Section: Cardiovascular Healthmentioning

confidence: 99%

Celebrating Versatility: Febuxostat’s Multifaceted Therapeutic Application

Kraev,

Geneva-Popova,

Hristov

et al. 2023

Life

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Febuxostat, initially developed as a xanthine oxidase inhibitor to address hyperuricemia in gout patients, has evolved into a versatile therapeutic agent with multifaceted applications. This review provides a comprehensive overview of febuxostat’s mechanism of action, its effectiveness in gout management, its cardiovascular safety profile, renal and hepatic effects, musculoskeletal applications, safety considerations, and emerging research prospects. Febuxostat’s primary mechanism involves selective inhibition of xanthine oxidase, resulting in reduced uric acid production. Its pharmacokinetics require personalized dosing strategies based on individual characteristics. In gout management, febuxostat offers a compelling alternative, effectively lowering uric acid levels, relieving symptoms, and supporting long-term control, especially for patients intolerant to allopurinol. Recent studies have demonstrated its cardiovascular safety, and it exhibits minimal hepatotoxicity, making it suitable for those with liver comorbidities. Febuxostat’s potential nephroprotective effects and kidney stone prevention properties are noteworthy, particularly for gout patients with renal concerns. Beyond gout, its anti-inflammatory properties hint at applications in musculoskeletal conditions and a broader spectrum of clinical contexts, including metabolic syndrome. Emerging research explores febuxostat’s roles in cardiovascular health, neurological disorders, rheumatoid arthritis, and cancer therapy, driven by its anti-inflammatory and antioxidative properties. Future directions include personalized medicine, combination therapies, mechanistic insights, and ongoing long-term safety monitoring, collectively illuminating the promising landscape of febuxostat’s multifaceted therapeutic potential.

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Section: Cardiovascular Healthmentioning

confidence: 99%

Celebrating Versatility: Febuxostat’s Multifaceted Therapeutic Application

Kraev,

Geneva-Popova,

Hristov

et al. 2023

Life

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5‐N,N‐Diarylaminothiazoles with Electron‐Accepting Groups: Synthesis, Photophysical Properties, and Their Application for the Detection of Hydrazine Hydrate

Murai,

Tanaka,

Takekoshi

et al. 2023

Eur J Org Chem

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Abstract5‐N,N‐diarylaminothiazoles containing cyano and nitro groups were synthesized using the Pd‐catalyzed Buchwald‐Hartwig amination reaction with good yields. The cyano group in the resultant thiazole was reduced to a formyl group. This was then subjected to the Knoevenagel condensation reaction, leading to the formation of thiazoles with a dicyanovinyl group. The nitro group in the thiazole was reduced to an amino group, which was subsequently reacted with triphosgene, yielding a thiazole with an isocyanate group. These thiazoles, with their electron‐accepting properties, demonstrated absorption and emission spectra at longer wavelengths. Notably, the thiazole containing the dicyanovinyl group displayed a red emission. Tests for the detection of hydrazine, a hazardous volatile organic compound, were conducted using the synthesized thiazoles. The results showed that the dicyanovinyl group effectively responded to hydrazine hydrate, evidenced by changes in the absorption and emission spectra. This change in color was also visibly detectable to the naked eye.

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