Design, Synthesis, in Vitro, and in Silico Anti-Α-Glucosidase Assays of N-Phenylacetamide-1,2,3-Triazole-Indole-2-Carboxamide Derivatives As New Anti-Diabetic Agents

Design, Synthesis, in Vitro, and in Silico Anti-Α-Glucosidase Assays of N-Phenylacetamide-1,2,3-Triazole-Indole-2-Carboxamide Derivatives As New Anti-Diabetic Agents Publisher Pubmed

Sayahi MH¹ ; Zareei S² ; Halimi M³ ; Alikhani M⁴ ; Moazzam A² ; Mohammadikhanaposhtani M⁵ ; Mojtabavi S⁶ ; Faramarzi MA⁶ ; Rastegar H⁷ ; Taslimi P⁸ ; Ibrahim EH^{9, 10, 11} ; Ghramh HA^{9, 10, 12} ; Larijani B² ; Mahdavi M²

Show Affiliations

1. Department of Chemistry, Payame Noor University, Tehran, Iran
2. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
3. Department of Biology, Babol Branch, Islamic Azad University, Babol, Iran
4. Department of Internal Medicine, School of Medicine, Rheumatology Research Center Shariati Hospital, Tehran University of Medical Sciences, Tehran, Iran
5. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
6. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
7. Cosmetic Products Research Center, Iranian Food and Drug Administration, MOHE, Tehran, Iran
8. Department of Biotechnology, Faculty of Science, Bartin University, Bartin, Turkey
9. Biology Department, Faculty of Science, King Khalid University, P.O. Box 9004, Abha, 61413, Saudi Arabia
10. Research Center for Advanced Materials Science (RCAMS), King Khalid University, Abha, Saudi Arabia
11. Blood Products Quality Control and Research Department, National Organization for Research and Control of Biologicals, Cairo, Egypt
12. Unit of Bee Research and Honey Production, Faculty of Science, King Khalid University, Abha, 61413, Saudi Arabia

Source: Scientific Reports Published:2024

Abstract

In this work, a novel series of N-phenylacetamide-1,2,3-triazole-indole-2-carboxamide derivatives 5a–n were designed by consideration of the potent α-glucosidase inhibitors containing indole and carboxamide-1,2,3-triazole-N-phenylacetamide moieties. These compounds were synthesized by click reaction and evaluated against yeast α-glucosidase. All the newly title compounds demonstrated superior potency when compared with acarbose as a standard inhibitor. Particularly, compound 5k possessed the best inhibitory activity against α-glucosidase with around a 28-fold improvement in the inhibition effect in comparison standard inhibitor. This compound showed a competitive type of inhibition in the kinetics. The molecular docking and dynamics demonstrated that compound 5k with a favorable binding energy well occupied the active site of α-glucosidase. © The Author(s) 2024.

Style	Citing Format
MLA	Sayahi MH, et al.. "Design, Synthesis, in Vitro, and in Silico Anti-Α-Glucosidase Assays of N-Phenylacetamide-1,2,3-Triazole-Indole-2-Carboxamide Derivatives As New Anti-Diabetic Agents." Scientific Reports, vol. 14, no. 1, 2024, pp. -.
APA	Sayahi MH, Zareei S, Halimi M, Alikhani M, Moazzam A, Mohammadikhanaposhtani M, Mojtabavi S, Faramarzi MA, Rastegar H, Taslimi P, Ibrahim EH, Ghramh HA, Larijani B, Mahdavi M (2024). Design, Synthesis, in Vitro, and in Silico Anti-Α-Glucosidase Assays of N-Phenylacetamide-1,2,3-Triazole-Indole-2-Carboxamide Derivatives As New Anti-Diabetic Agents. Scientific Reports, 14(1), -.
Chicago	Sayahi MH, Zareei S, Halimi M, Alikhani M, Moazzam A, Mohammadikhanaposhtani M, Mojtabavi S, et al.. "Design, Synthesis, in Vitro, and in Silico Anti-Α-Glucosidase Assays of N-Phenylacetamide-1,2,3-Triazole-Indole-2-Carboxamide Derivatives As New Anti-Diabetic Agents." Scientific Reports 14, no. 1 (2024): -.
Harvard	Sayahi MH et al. (2024) 'Design, Synthesis, in Vitro, and in Silico Anti-Α-Glucosidase Assays of N-Phenylacetamide-1,2,3-Triazole-Indole-2-Carboxamide Derivatives As New Anti-Diabetic Agents', Scientific Reports, 14(1), pp. -.
Vancouver	Sayahi MH, Zareei S, Halimi M, Alikhani M, Moazzam A, Mohammadikhanaposhtani M, et al.. Design, Synthesis, in Vitro, and in Silico Anti-Α-Glucosidase Assays of N-Phenylacetamide-1,2,3-Triazole-Indole-2-Carboxamide Derivatives As New Anti-Diabetic Agents. Scientific Reports. 2024;14(1):-.
BibTex	@article{ author = {Sayahi MH and Zareei S and Halimi M and Alikhani M and Moazzam A and Mohammadikhanaposhtani M and Mojtabavi S and Faramarzi MA and Rastegar H and Taslimi P and Ibrahim EH and Ghramh HA and Larijani B and Mahdavi M}, title = {Design, Synthesis, in Vitro, and in Silico Anti-Α-Glucosidase Assays of N-Phenylacetamide-1,2,3-Triazole-Indole-2-Carboxamide Derivatives As New Anti-Diabetic Agents}, journal = {Scientific Reports}, volume = {14}, number = {1}, pages = {-}, year = {2024} }
RIS	TY - JOUR AU - Sayahi MH AU - Zareei S AU - Halimi M AU - Alikhani M AU - Moazzam A AU - Mohammadikhanaposhtani M AU - Mojtabavi S AU - Faramarzi MA AU - Rastegar H AU - Taslimi P AU - Ibrahim EH AU - Ghramh HA AU - Larijani B AU - Mahdavi M TI - Design, Synthesis, in Vitro, and in Silico Anti-Α-Glucosidase Assays of N-Phenylacetamide-1,2,3-Triazole-Indole-2-Carboxamide Derivatives As New Anti-Diabetic Agents JO - Scientific Reports VL - 14 IS - 1 SP - EP - PY - 2024 ER -

Science Communicator Platform

Authors

Authors Affiliations

Abstract