Synthesis and cholinesterase enzymes inhibition of novel eugenol substituted carbamate derivatives

Year 2017, , 335 - 342, 01.06.2017

Fatih Sönmez

https://doi.org/10.16984/saufenbilder.284240

Abstract

In this study, 14 novel eugenol derivatives with the carbamate moiety were synthesized and their inhibitory effects on
acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. 4-allyl-2-methoxyphenyl-(3,4-
dicholorophenyl)carbamate (3f) was found to be the most potent AChE inhibitor with IC50 value of 71.6 µM, and 4-
allyl-2-methoxyphenyl(3-methoxyphenyl)carbamate (3a) exhibited the strongest inhibition against BuChE with IC50
value of 0.58 µM. Additionally, structure-activity relationship were also investigated. 

Keywords

Eugenol, carbamate, Alzheimer’s disease

Eugenol sübstitüe yeni karbamat türevlerinin sentezi ve kolinesteraz enzimlerinin inhibisyonu

Abstract

Bu çalışmada, karbamat grubu içeren 14 yeni eugenol türevleri sentezlenmiş ve bunların asetilkolinesteraz (AChE) ve
bütirilkolinesteraz (BuChE) enzimleri üzerine inhibitör etkileri incelenmiştir. 4-allil-2-metoksifenil-(3,4-
diklorofenil)karbamat (3f) 71.6 µM’lık IC50 değeri ile en iyi AChE inhibitörü olarak belirlenmiştir. 4-allil-2-
metoksifenil(3-metoksifenil)karbamat (3a) 0.58 µM’lık IC50 değeri ile BuChE’ye karşı en güçlü inhibisyonu
sergilemiştir. Ayrıca sentezlenen bileşikler için yapı-aktivite ilişkileri de incelenmiştir.  

Keywords

Eugenol, Karbamat, Alzheimer hastalığı

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