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Journals / Ankara Üniversitesi Eczacılık Fakültesi Dergisi / 2026 / Cilt: 49 Sayı: 1

SYNTHESIS, CHARACTERIZATION AND CHOLINESTERASE INHIBITORY EFFECTS OF IBUPROFEN-BASED SPIROTHIAZOLIDINONES

İBUPROFEN TÜREVİ SPİROTHİAZOLİDİNONLARIN SENTEZİ, KARAKTERİZASYONU VE KOLİNESTERAZ İNHİBİTÖR ETKİLERİ

Çağla Begüm Apaydın(ISTANBUL UNIVERSITY, FACULTY OF PHARMACY)0000-0001-6703-9389
Gozde Hasbal Çelikok(ISTANBUL UNIVERSITY)0000-0002-0216-7635
Tuğba Yılmaz Özden(ISTANBUL UNIVERSITY)0000-0003-4426-4502
Pages
12–20
Publication Date
2025-01-20
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

Result and Discussion: According to the inhibition data, compound 4e demonstrated the most promising activity against AChE, with an IC50 value of 39.53±1.94 µM, while compound 4b exhibited the most potential against BuChE, with an IC50 value of 95.97±1.79 µM.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:Objective: A novel class of spirothiazolidinone derivatives were designed, synthesized, and assessed as possible acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors for Alzheimer's disease therapy.
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Key Findings & Data:IR, 1H NMR, 13C NMR, LC-MS and elemental analysis techniques have all been used to clarify the chemical structures of the compounds.
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Conclusion & Impact:Result and Discussion: According to the inhibition data, compound 4e demonstrated the most promising activity against AChE, with an IC50 value of 39.53±1.94 µM, while compound 4b exhibited the most potential against BuChE, with an IC50 value of 95.97±1.79 µM.
🔬Design:Araştırma Makalesi
📍Scope:Comprehensive Sample
⚙️Variables:Asetilkolinesteraz · butirilkolinesteraz · ibuprofen

Abstract

Objective: A novel class of spirothiazolidinone derivatives were designed, synthesized, and assessed as possible acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitors for Alzheimer's disease therapy. Material and Method: In this study, novel spirocyclic compounds were synthesized by one-pot reaction. IR, 1H NMR, 13C NMR, LC-MS and elemental analysis techniques have all been used to clarify the chemical structures of the compounds. AChE and BuChE inhibitory effects of compounds (4a-e and, 5a-e) were assayed according to Ellman’s method using galantamine as reference. Result and Discussion: According to the inhibition data, compound 4e demonstrated the most promising activity against AChE, with an IC50 value of 39.53±1.94 µM, while compound 4b exhibited the most potential against BuChE, with an IC50 value of 95.97±1.79 µM.

Özet

Amaç: Alzheimer hastalığına karşı potansiyel asetilkolinesteraz (AChE) ve butirilkolinesteraz (BuChE) inhibitörleri olarak bir seri yeni spirotiyazolidinon türevi tasarlanmış, sentezlenmiş ve inhibisyon etkileri değerlendirilmiştir. Gereç ve Yöntem: Bu çalışmadan kazanılan yeni spiro bileşikler tek kap yöntemi ile sentez edilmiştir. Bileşiklerin kimyasal yapılarını aydınlatmak için IR, 1H NMR, 13C NMR, LC-MS ve elementel analiz yöntemleri kullanılmıştır. Bileşiklerin (4a-e ve 5a-e), AChE ve BuChE enzimleri üzerindeki inhibisyon etkileri galantamin referans olarak kullanılarak Ellman yöntemine göre analiz edilmiştir. Sonuç ve Tartışma: İnhibisyon sonuçlarına göre, en umut verici bileşik AChE'ye karşı IC50 değeri 39.53±1.94 µM olan 4e ve BuChE'ye karşı IC50 değeri 95.97±1.79 µM olan 4b bileşikleri olarak kaydedilmiştir.

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Cite This Article

Apaydın, Ç. B., Çelikok, G. H., Özden, T. Y. (2025). SYNTHESIS, CHARACTERIZATION AND CHOLINESTERASE INHIBITORY EFFECTS OF IBUPROFEN-BASED SPIROTHIAZOLIDINONES. Ankara Üniversitesi Eczacılık Fakültesi Dergisi, Cilt: 49 Sayı: 1, 12–20. https://doi.org/10.33483/jfpau.1493082

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