1,2,3-Triazole substituted phthalocyanine metal complexes as potential inhibitors for anticholinesterase and antidiabetic enzymes with molecular docking studies
Date
09.12.2020Metadata
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Umit M. Koc € ¸yigit a , Parham Taslimib , Burak Tuz€ un€ c , Hasan Yakand , Halit Muglu e and Emre Guzel € f a Department of Basic Pharmaceutical Sciences, Sivas Cumhuriyet University, Sivas, Turkey; b Department of Biotechnology, Faculty of Science, Bartın University, Bartin, Turkey; c Department of Chemistry, Sivas Cumhuriyet University, Sivas, Turkey; d Department of Chemistry Education, Ondokuz Mayıs University, Samsun, Turkey; e Department of Chemistry, Kastamonu University, Kastamonu, Turkey; f Department of Fundamental Sciences, Faculty of Technology, Sakarya University of Applied Sciences, Sakarya, Turkey Communicated by Ramaswamy H. SarmaAbstract
In recent years, acetylcholinesterase (AChE) and a-glycosidase (a-gly) inhibition have emerged as a
promising and important approach for pharmacological intervention in many diseases such as glaucoma,
epilepsy, obesity, cancer, and Alzheimer’s. In this manner, the preparation and enzyme inhibition
activities of peripherally 1,2,3-triazole group substituted metallophthalocyanine derivatives with
strong absorption in the visible region were presented. These novel metallophthalocyanine derivatives
(2-6) effectively inhibited AChE, with Ki values in the range of 40.11 ± 5.61 to 78.27 ± 15.42 mM. For
a-glycosidase, the most effective Ki values of compounds 1 and 2 were with Ki values of 16.11 ± 3.13
and 18.31 ± 2.42 mM, respectively. Also, theoretical calculations were investigated to compare the
chemical and biological activities of the ligand (1) and its metal complexes (2–6). Biological activities
of 1 and its complexes against acetylcholinesterase for ID 4M0E (AChE) and a-glycosidase for ID 1R47
(a-gly) are calculated. Theoretical calculations were compatible with the experimental results and these
1,2,3-triazole substituted phthalocyanine metal complexes were found to be efficient inhibitors for
anticholinesterase and antidiabetic enzymes.