Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors

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Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors Publisher Pubmed

Saeedi M^{1, 2} ; Mohammadikhanaposhtani M³ ; Asgari MS⁴ ; Eghbalnejad N⁵ ; Imanparast S⁶ ; Faramarzi MA⁶ ; Larijani B⁷ ; Mahdavi M⁷ ; Akbarzadeh T^{2, 8}

Show Affiliations

1. Medicinal Plants Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
2. Persian Medicine and Pharmacy Research Center, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
3. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
4. School of Chemistry, College of Science, University of Tehran, Tehran, Iran
5. Faculty of Pharmacy, International Campus (TUMS-IC), Tehran University of Medical Sciences, Tehran, Iran
6. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, P.O. Box 14155-6451, Tehran, 1417614411, Iran
7. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
8. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

Source: Bioorganic and Medicinal Chemistry Published:2019

Abstract

In this work, new derivatives of diarylimidazole-1,2,3-triazole 7a-p were designed, synthesized, and evaluated for their in vitro α-glucosidase inhibitory activity. All compounds showed potent inhibitory activity in the range of IC50 = 90.4–246.7 µM comparing with acarbose as the standard drug (IC50 = 750.0 µM). Among the synthesized compounds, compounds 7b, 7c, and 7e were approximately 8 times more potent than acarbose. The kinetic study of those compounds indicated that they acted as the competitive inhibitors of α-glucosidase. Molecular docking studies were also carried out for compounds 7b, 7c, and 7e using modeled α-glucosidase to find the interaction modes responsible for the desired inhibitory activity. © 2019 Elsevier Ltd

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Style	Citing Format
MLA	Saeedi M, et al.. "Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors." Bioorganic and Medicinal Chemistry, vol. 27, no. 23, 2019, pp. -.
APA	Saeedi M, Mohammadikhanaposhtani M, Asgari MS, Eghbalnejad N, Imanparast S, Faramarzi MA, Larijani B, Mahdavi M, Akbarzadeh T (2019). Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors. Bioorganic and Medicinal Chemistry, 27(23), -.
Chicago	Saeedi M, Mohammadikhanaposhtani M, Asgari MS, Eghbalnejad N, Imanparast S, Faramarzi MA, Larijani B, Mahdavi M, Akbarzadeh T. "Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors." Bioorganic and Medicinal Chemistry 27, no. 23 (2019): -.
Harvard	Saeedi M et al. (2019) 'Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors', Bioorganic and Medicinal Chemistry, 27(23), pp. -.
Vancouver	Saeedi M, Mohammadikhanaposhtani M, Asgari MS, Eghbalnejad N, Imanparast S, Faramarzi MA, et al.. Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors. Bioorganic and Medicinal Chemistry. 2019;27(23):-.
BibTex	@article{ author = {Saeedi M and Mohammadikhanaposhtani M and Asgari MS and Eghbalnejad N and Imanparast S and Faramarzi MA and Larijani B and Mahdavi M and Akbarzadeh T}, title = {Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors}, journal = {Bioorganic and Medicinal Chemistry}, volume = {27}, number = {23}, pages = {-}, year = {2019} }
RIS	TY - JOUR AU - Saeedi M AU - Mohammadikhanaposhtani M AU - Asgari MS AU - Eghbalnejad N AU - Imanparast S AU - Faramarzi MA AU - Larijani B AU - Mahdavi M AU - Akbarzadeh T TI - Design, Synthesis, in Vitro, and in Silico Studies of Novel Diarylimidazole-1,2,3-Triazole Hybrids As Potent Α-Glucosidase Inhibitors JO - Bioorganic and Medicinal Chemistry VL - 27 IS - 23 SP - EP - PY - 2019 ER -

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