Eugenol sübstitüe yeni karbamat türevlerinin sentezi ve kolinesteraz enzimlerinin inhibisyonu

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.

Synthesis and cholinesterase enzymes inhibition of novel eugenol substituted carbamate derivatives

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.

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