Yeni imidazol-hidrazon türevlerinin sentezi ve antikolinesteraz aktivitesi

Abstract

Alzheimer hastalığı (AH) öncelikli olarak yaşlı popülasyonda görülen, klinik olarak bellek ve bilişsel bozukluklar ile karakterize, ilerleyici ve nörodejeneratif bir hastalıktır. Hastalığın etiyolojisinin henüz tam olarak belirlenememiş olması, hasta popülasyonunun yıllar geçtikçe artması, radikal bir tedavinin olmayışı, tedavi ve bakım maliyetinin oldukça yüksek olması, hastaların yaşam kalitesini oldukça düşürmesi gibi sebepler hastalığın önemini artırmakta ve araştırmacıları bu alana yönlendirmektedir. Bu çalışmada, bazı yeni imidazol-hidrazon türevleri, imidazol-hidrazon gruplarının potansiyel antikolinesteraz aktivitesi göz önüne alınarak sentezlendi. Sentez çalışmalarında, hidrazon bileşikleri çeşitli imidazol-karbaldehit türevleri ile reaksiyona sokuldu ve sonuç bileşikleri elde edildi. Elde edilen bileşiklerin yapıları IR, 1H NMR, 13C NMR ve Kütle spektroskopik yöntemleri ile aydınlatıldı. Sentezlenen bileşiklerin kolinesteraz enzimi üzerindeki etkileri Ellman metodu kullanılarak değerlendirildi. Sentezlenen bileşiklerin aktivite çalışmaları sonucunda orta düzeyde antikolinesteraz aktivitesi gösterdiği belirlenmiştir.

Keywords

• Hidrazon
• imidazol
• antikolinesteraz
• ellman metodu

Synthesis of new imidazole-hydrazone derivatives and anticholinesterase activity

Abstract

Alzheimer's disease (AD) is a progressive and neurodegenerative disease primarily seen in the elderly population, clinically characterized by memory and cognitive impairment. The importance of disease increase because of some reasons; the etiology of the disease has not been determined yet, increase in patient population over the years, absence of radical treatment, high cost of treatment and care, significant reduction in quality of life of patients, and these lead to direct researchers to this field. In this study, some new imidazole-hydrazone derivatives were synthesized considering potential anticholinesterase activity of imidazole-hydrazone groups. In synthesis studies, hydrazone compounds was reacted with various imidazole-carbaldehyde derivatives and final product were gained. Structures of obtained compounds were confirmed by IR, 1H NMR, 13C NMR and Mass spectroscopic methods. Effects of the synthesized compounds on cholinesterase enzyme were observed by using Ellman’s method. Moderate anticholinesterase activity of the synthesized compounds was determined as a result of activity studies.

Keywords

• Hydrazone
• imidazole
• anticholinesterase
• ellman’s method

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