Synthesis, Characterization, Molecular Docking, and Biological Activities of Coumarin–1,2,3-Triazole-Acetamide Hybrid Derivatives

Synthesis, Characterization, Molecular Docking, and Biological Activities of Coumarin–1,2,3-Triazole-Acetamide Hybrid Derivatives Publisher Pubmed

Sepehri N¹ ; Mohammadikhanaposhtani M² ; Asemanipoor N³ ; Hosseini S⁴ ; Biglar M³ ; Larijani B³ ; Mahdavi M³ ; Hamedifar H⁵ ; Taslimi P⁶ ; Sadeghian N⁷ ; Gulcin I⁷

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1. Nano Alvand Company, Avicenna Tech Park, Tehran University of Medical Sciences, Tehran, Iran
2. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
3. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
4. Department of Pharmaceutical Chemistry, School of Pharmacy, Shahid Beheshti University of Medical Sciences, Tehran, Iran
5. CinnaGen Medical Biotechnology Research Center, Alborz University of Medical Sciences, Karaj, Iran
6. Department of Biotechnology, Faculty of Science, Bartin University, Bartin, Turkey
7. Department of Chemistry, Faculty of Science, Ataturk University, Erzurum, Turkey

Source: Archiv der Pharmazie Published:2020

Abstract

Coumarins and their derivatives are receiving increasing attention due to numerous biochemical and pharmacological applications. In this study, a series of novel coumarin–1,2,3-triazole-acetamide hybrids was tested against some metabolic enzymes including α-glycosidase (α-Gly), α-amylase (α-Amy), acetylcholinesterase (AChE), butyrylcholinesterase (BChE), human carbonic anhydrase I (hCA I), and hCA II. The new coumarin–1,2,3-triazole-acetamide hybrids showed Ki values in the range of 483.50–1,243.04 nM against hCA I, 508.55–1,284.36 nM against hCA II, 24.85–132.85 nM against AChE, 27.17–1,104.36 nM against BChE, 590.42–1,104.36 nM against α-Gly, and 55.38–128.63 nM against α-Amy. The novel coumarin–1,2,3-triazole-acetamide hybrids had effective inhibition profiles against all tested metabolic enzymes. Also, due to the enzyme inhibitory effects of the new hybrids, they are potential drug candidates to treat diseases such as epilepsy, glaucoma, type-2 diabetes mellitus (T2DM), Alzheimer's disease (AD), and leukemia. Additionally, these inhibition effects were compared with standard enzyme inhibitors like acetazolamide (for hCA I and II), tacrine (for AChE and BChE), and acarbose (for α-Gly and α-Amy). Also, those coumarin–1,2,3-triazole-acetamide hybrids with the best inhibition score were docked into the active site of the indicated metabolic enzymes. © 2020 Deutsche Pharmazeutische Gesellschaft

Style	Citing Format
MLA	Sepehri N, et al.. "Synthesis, Characterization, Molecular Docking, and Biological Activities of Coumarin–1,2,3-Triazole-Acetamide Hybrid Derivatives." Archiv der Pharmazie, vol. 353, no. 10, 2020, pp. -.
APA	Sepehri N, Mohammadikhanaposhtani M, Asemanipoor N, Hosseini S, Biglar M, Larijani B, Mahdavi M, Hamedifar H, Taslimi P, Sadeghian N, Gulcin I (2020). Synthesis, Characterization, Molecular Docking, and Biological Activities of Coumarin–1,2,3-Triazole-Acetamide Hybrid Derivatives. Archiv der Pharmazie, 353(10), -.
Chicago	Sepehri N, Mohammadikhanaposhtani M, Asemanipoor N, Hosseini S, Biglar M, Larijani B, Mahdavi M, et al.. "Synthesis, Characterization, Molecular Docking, and Biological Activities of Coumarin–1,2,3-Triazole-Acetamide Hybrid Derivatives." Archiv der Pharmazie 353, no. 10 (2020): -.
Harvard	Sepehri N et al. (2020) 'Synthesis, Characterization, Molecular Docking, and Biological Activities of Coumarin–1,2,3-Triazole-Acetamide Hybrid Derivatives', Archiv der Pharmazie, 353(10), pp. -.
Vancouver	Sepehri N, Mohammadikhanaposhtani M, Asemanipoor N, Hosseini S, Biglar M, Larijani B, et al.. Synthesis, Characterization, Molecular Docking, and Biological Activities of Coumarin–1,2,3-Triazole-Acetamide Hybrid Derivatives. Archiv der Pharmazie. 2020;353(10):-.
BibTex	@article{ author = {Sepehri N and Mohammadikhanaposhtani M and Asemanipoor N and Hosseini S and Biglar M and Larijani B and Mahdavi M and Hamedifar H and Taslimi P and Sadeghian N and Gulcin I}, title = {Synthesis, Characterization, Molecular Docking, and Biological Activities of Coumarin–1,2,3-Triazole-Acetamide Hybrid Derivatives}, journal = {Archiv der Pharmazie}, volume = {353}, number = {10}, pages = {-}, year = {2020} }
RIS	TY - JOUR AU - Sepehri N AU - Mohammadikhanaposhtani M AU - Asemanipoor N AU - Hosseini S AU - Biglar M AU - Larijani B AU - Mahdavi M AU - Hamedifar H AU - Taslimi P AU - Sadeghian N AU - Gulcin I TI - Synthesis, Characterization, Molecular Docking, and Biological Activities of Coumarin–1,2,3-Triazole-Acetamide Hybrid Derivatives JO - Archiv der Pharmazie VL - 353 IS - 10 SP - EP - PY - 2020 ER -

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