Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme

Gülce Taşkor Önel; Burçin Türkmenoğlu; Şule Gürsoy; Esra Dilek; Azime Berna Özçelik; Mehtap Uysal

Makale detayları

Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme

Yazarlar:

Gülce Taşkor Önel | Burçin Türkmenoğlu | Şule Gürsoy | Esra Dilek | Azime Berna Özçelik | Mehtap Uysal

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmaceutical Biochemistry | Pharmaceutical Chemistry

Dergi:

Journal of Research in Pharmacy Vol.26 Issue 5, pp.1461-1471

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001347564

pISSN:

2630-6344

Anahtar kelimeler:

Özet:

 Alzheimers disease is a neurological disease characterized by the destruction of brain cells. In this disease, which causes a decrease in thought, memory and behavioral functions, the symptoms appear gradually with age. In this study, inhibition of acetylcholinesterase enzyme which is an important target in accordance with the cholinergic hypothesis, was studied. New 32Hpyridazinone-triazole derivatives were synthesized, confirmed by 1H-NMR, 13CNMR, HRMS analysis and their IC50 and Ki values were studied. The inhibition constants Ki of the compounds against the AChE enzyme ranged from 2.35  0.18 to 5.15  0.46 μM. The compound with the best inhibitory properties was compound 6d with a Ki value of 2.35  0.18 μM. In addition, to support the experimental data, molecular docking studies were carried out with 6b, 6d, 6e and 6f compounds with AChE crystal structure PDB ID:4M0E.

 Alzheimers disease is a neurological disease characterized by the destruction of brain cells. In this disease, which causes a decrease in thought, memory and behavioral functions, the symptoms appear gradually with age. In this study, inhibition of acetylcholinesterase enzyme which is an important target in accordance with the cholinergic hypothesis, was studied. New 32Hpyridazinone-triazole derivatives were synthesized, confirmed by 1H-NMR, 13CNMR, HRMS analysis and their IC50 and Ki values were studied. The inhibition constants Ki of the compounds against the AChE enzyme ranged from 2.35  0.18 to 5.15  0.46 μM. The compound with the best inhibitory properties was compound 6d with a Ki value of 2.35  0.18 μM. In addition, to support the experimental data, molecular docking studies were carried out with 6b, 6d, 6e and 6f compounds with AChE crystal structure PDB ID:4M0E.

 Alzheimers disease is a neurological disease characterized by the destruction of brain cells. In this disease, which causes a decrease in thought, memory and behavioral functions, the symptoms appear gradually with age. In this study, inhibition of acetylcholinesterase enzyme which is an important target in accordance with the cholinergic hypothesis, was studied. New 32Hpyridazinone-triazole derivatives were synthesized, confirmed by 1H-NMR, 13CNMR, HRMS analysis and their IC50 and Ki values were studied. The inhibition constants Ki of the compounds against the AChE enzyme ranged from 2.35  0.18 to 5.15  0.46 μM. The compound with the best inhibitory properties was compound 6d with a Ki value of 2.35  0.18 μM. In addition, to support the experimental data, molecular docking studies were carried out with 6b, 6d, 6e and 6f compounds with AChE crystal structure PDB ID:4M0E.

 Alzheimers disease is a neurological disease characterized by the destruction of brain cells. In this disease, which causes a decrease in thought, memory and behavioral functions, the symptoms appear gradually with age. In this study, inhibition of acetylcholinesterase enzyme which is an important target in accordance with the cholinergic hypothesis, was studied. New 32Hpyridazinone-triazole derivatives were synthesized, confirmed by 1H-NMR, 13CNMR, HRMS analysis and their IC50 and Ki values were studied. The inhibition constants Ki of the compounds against the AChE enzyme ranged from 2.35  0.18 to 5.15  0.46 μM. The compound with the best inhibitory properties was compound 6d with a Ki value of 2.35  0.18 μM. In addition, to support the experimental data, molecular docking studies were carried out with 6b, 6d, 6e and 6f compounds with AChE crystal structure PDB ID:4M0E.

Makale detayları

Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme

Yazarlar:

Gülce Taşkor Önel | Burçin Türkmenoğlu | Şule Gürsoy | Esra Dilek | Azime Berna Özçelik | Mehtap Uysal

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmaceutical Biochemistry | Pharmaceutical Chemistry

Dergi:

Journal of Research in Pharmacy Vol.26 Issue 5, pp.1461-1471

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001347564

pISSN:

2630-6344

Acetylcholinesterase

alzheimer’s disease

molecular docking

pyridazinone

triazole

Sayı

Makale detayları

Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme

Yazarlar: Gülce Taşkor Önel | Burçin Türkmenoğlu | Şule Gürsoy | Esra Dilek | Azime Berna Özçelik | Mehtap Uysal

Yayıncı: Marmara University

Ana Başlıklar: Pharmaceutical Biochemistry | Pharmaceutical Chemistry

Dergi: Journal of Research in Pharmacy Vol.26 Issue 5, pp.1461-1471

Belge Tipi: Makale

Yayın Tarihi: 6/2025

Belge Dili: İngilizce

Document ID (Org No.): 2001347564

pISSN: 2630-6344

Acetylcholinesterase

alzheimer’s disease

molecular docking

pyridazinone

triazole

Sayı

Yazarlar:

Gülce Taşkor Önel | Burçin Türkmenoğlu | Şule Gürsoy | Esra Dilek | Azime Berna Özçelik | Mehtap Uysal

Yayıncı:

Marmara University

Ana Başlıklar:

Pharmaceutical Biochemistry | Pharmaceutical Chemistry

Dergi:

Journal of Research in Pharmacy Vol.26 Issue 5, pp.1461-1471

Belge Tipi:

Makale

Yayın Tarihi:

6/2025

Belge Dili:

İngilizce

Document ID (Org No.):

2001347564

pISSN:

2630-6344