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

Çağla Begüm Apaydın; Gozde Hasbal Çelikok; Tuğba Yılmaz Özden

Makale detayları

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

Yazarlar:

Çağla Begüm Apaydın | Gozde Hasbal Çelikok | Tuğba Yılmaz Özden

Yayıncı:

Ankara University

Ana Başlıklar:

Farmasotik Kimya

Dergi:

Ankara Üniversitesi Eczacılık Fakültesi Dergisi Vol.49 Issue 1, pp.12-20

Belge Tipi:

Makale

Yayın Tarihi:

1/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001333042

pISSN:

1015-3918

Anahtar kelimeler:

Özet:

 Objective: A novel class of spirothiazolidinone derivatives were designed, synthesized, and assessed as possible acetylcholinesterase AChE and butyrylcholinesterase BuChE inhibitors for Alzheimers 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 Ellmans 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 39.531.94 µM, while compound 4b exhibited the most potential against BuChE, with an IC50 value of 95.971.79 µM.

 Objective: A novel class of spirothiazolidinone derivatives were designed, synthesized, and assessed as possible acetylcholinesterase AChE and butyrylcholinesterase BuChE inhibitors for Alzheimers 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 Ellmans 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 39.531.94 µM, while compound 4b exhibited the most potential against BuChE, with an IC50 value of 95.971.79 µM.

 Objective: A novel class of spirothiazolidinone derivatives were designed, synthesized, and assessed as possible acetylcholinesterase AChE and butyrylcholinesterase BuChE inhibitors for Alzheimers 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 Ellmans 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 39.531.94 µM, while compound 4b exhibited the most potential against BuChE, with an IC50 value of 95.971.79 µM.

 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 AChEye karşı IC50 değeri 39.531.94 µM olan 4e ve BuChEye karşı IC50 değeri 95.971.79 µM olan 4b bileşikleri olarak kaydedilmiştir.

Makale detayları

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

Yazarlar:

Çağla Begüm Apaydın | Gozde Hasbal Çelikok | Tuğba Yılmaz Özden

Yayıncı:

Ankara University

Ana Başlıklar:

Farmasotik Kimya

Dergi:

Ankara Üniversitesi Eczacılık Fakültesi Dergisi Vol.49 Issue 1, pp.12-20

Belge Tipi:

Makale

Yayın Tarihi:

1/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001333042

pISSN:

1015-3918

Acetylcholinesterase

butyrylcholinesterase

ibuprofen

spirothiazolidinone

synthesisAsetilkolinesteraz

butirilkolinesteraz

ibuprofen

sentez

spirotiyazolidinon

Sayı

Makale detayları

Yazarlar: Çağla Begüm Apaydın | Gozde Hasbal Çelikok | Tuğba Yılmaz Özden

Yayıncı: Ankara University

Ana Başlıklar: Farmasotik Kimya

Dergi: Ankara Üniversitesi Eczacılık Fakültesi Dergisi Vol.49 Issue 1, pp.12-20

Belge Tipi: Makale

Yayın Tarihi: 1/2025

Belge Dili: İngilizce

Document ID (Org No.): 2001333042

pISSN: 1015-3918

Sayı

Yazarlar:

Çağla Begüm Apaydın | Gozde Hasbal Çelikok | Tuğba Yılmaz Özden

Yayıncı:

Ankara University

Ana Başlıklar:

Farmasotik Kimya

Dergi:

Ankara Üniversitesi Eczacılık Fakültesi Dergisi Vol.49 Issue 1, pp.12-20

Belge Tipi:

Makale

Yayın Tarihi:

1/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001333042

pISSN:

1015-3918