Article 2021 · 43 citations

Synthesis of novel tris-chalcones and determination of their inhibition profiles against some metabolic enzymes

Burmaoglu, Serdar, Yilmaz, Ali Osman, Polat, M. Fatih, Kaya, Ruya, Gulcin, Ilhami, Algul, Oztekin

Abstract

In this study, we report the synthesis of novel tris-chalcones and testing of human carbonic anhydrase I, and II isoenzymes (hCA I, and hCA II), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and alpha-glycosidase (alpha-Gly) inhibitors for the development of novel chalcone structures towards for treatment of some diseases. The compounds demonstrated K-i values between 13.6 +/- 1.1 and 50.0 +/- 17.1 nM on hCA I, 9.9 +/- 0.8 and 39.5 +/- 15.1 nM on hCA II, 3.1 +/- 0.2 and 20.1 +/- 1.9 nM on AChE, 4.9 +/- 0.4 and 14.7 +/- 5.2 nM on BChE and 3.9 +/- 0.2 and 22.4 +/- 10.7 nM on alpha-Gly enzymes. The results revealed that novel tris-chalcones can have promising drug potential for glaucoma, leukaemia, epilepsy; Alzheimer's disease that was associated with the high enzymatic activity of hCA I, hCA II, AChE, and BChE enzymes.

Keywords

Tris-chalcone carbonic anhydrase acetylcholinesterase butyrylcholinesterase alpha-glycosidase CARBONIC-ANHYDRASE INHIBITORS TROUT ONCORHYNCHUS-MYKISS ERYTHROCYTE ISOZYMES I CRYSTAL-STRUCTURE ANTICHOLINERGIC ACTIVITIES BIOLOGICAL EVALUATION MEDICINAL CHEMISTRY 1ST SYNTHESIS HALOGEN BOND ACETYLCHOLINESTERASE

WoS Categories

Biochemistry & Molecular Biology Biophysics Endocrinology & Metabolism Physiology

Sustainable Development Goals

Good Health and Well-being

Citation

Journal: ARCHIVES OF PHYSIOLOGY AND BIOCHEMISTRY
Year: 2021
Volume: 127
Issue: 2
Pages: 153-161
ISSN: 1381-3455
eISSN: 1744-4160
DOI: 10.1080/13813455.2019.1623265
WoS UID: WOS:000474135700001

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