Synthesis and Characterization of New Imidazole Derivatives as Potential Anticholinesterase Agents

Abstract

Alzheimer's disease is one of the most common neurodegenerative diseases. This disease, which is seen with a rate of 70-76% in developed countries, does not have a radical treatment, which directs the scientific world to work on this issue. The cholinergic hypothesis suggests that low acetylcholine (ACh) levels are the main cause of memory and cognitive impairment in AD patients. The absence of a radical treatment makes this area attractive for scientists. Imidazole compounds are important compounds in medicinal chemistry due to their wide variety of biological activities. In this study, new imidazole derivatives were synthesized and the structure determinations were elucidated using ¹H-NMR, ¹³C-NMR and mass spectroscopy methods. The activity profiles of the compounds were performed using the in vitro Elisa method. The data obtained as a result of the activity showed that the anticholinesterase activity profiles of the 6 and 7 coded compounds were promising.

Keywords

• Imidazole
• Anticholinesterase activity

Potansiyel Antikolinesteraz Ajanlar Olarak Yeni İmidazol Türevlerinin Sentezi ve Karakterizasyonu

Abstract

Alzheimer hastalığı en sık görülen nörodejeneratif hastalıklarıdan biridir. Gelişmiş ülkelerde %70-76 oranla görülen bu hastalığın radikal bir tedaviye sahip olmaması bilim dünyasını bu konu üzerinde çalışmaya yönlendirmektedir. Kolinerjik hipotez, AH hastalarında hafıza ve bilişsel bozukluğun ana nedeni düşük asetilkolin (ACh) düzeyinin olduğunu düşündürmektedir. Radikal bir tedavinin mevcut olmaması bilim insanları için bu alanı çekici kılmaktadır. İmidazol bileşikleri, çok çeşitli biyolojik aktiviteleri nedeniyle medisinal kimyada önemli bileşiklerdir. Bu çalışmada, yeni imidazol türevleri sentezlenmiş ve yapı tayinleri ¹H-NMR, ¹³C-NMR ve kütle spektroskopisi metodları kullanılarak aydınlatılmıştır. Bileşiklerin aktivite profilleri in vitro Ellman metodu kullanılarak gerçekleştirilmiştir. Aktivite sonucunda elde edilen veriler, 6 ve 7 kodlu bileşiklerin antikolinesteraz aktivite profillerinin umut vaat edici olduğunu ortaya koymuştur.

Keywords

• İmidazol
• Antikolinesteraz aktivite
• NMR

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