Design and Synthesis of Novel Pyridazine N-Aryl Acetamides: In-Vitro Evaluation of Α-Glucosidase Inhibition, Docking, and Kinetic Studies

Design and Synthesis of Novel Pyridazine N-Aryl Acetamides: In-Vitro Evaluation of Α-Glucosidase Inhibition, Docking, and Kinetic Studies Publisher Pubmed

Moghimi S¹ ; Toolabi M² ; Salarinejad S³ ; Firoozpour L¹ ; Sadat Ebrahimi SE³ ; Safari F⁴ ; Mojtabavi S⁵ ; Faramarzi MA⁵ ; Foroumadi A^{1, 3}

Show Affiliations

1. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran
2. Department of Medicinal Chemistry, School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran
3. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
4. Department of Biology, Faculty of Science, University of Guilan, Rasht, Iran
5. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran

Source: Bioorganic Chemistry Published:2020

Abstract

We herein applied the four step-synthetic route to prepare the pyridazine core attached to the various N-aryl acetamides. By this approach, a new series of pyridazine-based compounds were synthesized, characterized and evaluated for their activities against α-glucosidase enzyme. In-vitro α-glucosidase assay established that twelve compounds are more potent than acarbose. Compound 7a inhibited α-glucosidase with the IC50 value of 70.1 µM. The most potent compounds showed no cytotoxicity against HDF cell line. Molecular docking and kinetic studies were performed to determine the modes of interaction and inhibition, respectively. © 2020 Elsevier Inc.

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Style	Citing Format
MLA	Moghimi S, et al.. "Design and Synthesis of Novel Pyridazine N-Aryl Acetamides: In-Vitro Evaluation of Α-Glucosidase Inhibition, Docking, and Kinetic Studies." Bioorganic Chemistry, vol. 102, no. , 2020, pp. -.
APA	Moghimi S, Toolabi M, Salarinejad S, Firoozpour L, Sadat Ebrahimi SE, Safari F, Mojtabavi S, Faramarzi MA, Foroumadi A (2020). Design and Synthesis of Novel Pyridazine N-Aryl Acetamides: In-Vitro Evaluation of Α-Glucosidase Inhibition, Docking, and Kinetic Studies. Bioorganic Chemistry, 102(), -.
Chicago	Moghimi S, Toolabi M, Salarinejad S, Firoozpour L, Sadat Ebrahimi SE, Safari F, Mojtabavi S, Faramarzi MA, Foroumadi A. "Design and Synthesis of Novel Pyridazine N-Aryl Acetamides: In-Vitro Evaluation of Α-Glucosidase Inhibition, Docking, and Kinetic Studies." Bioorganic Chemistry 102, no. (2020): -.
Harvard	Moghimi S et al. (2020) 'Design and Synthesis of Novel Pyridazine N-Aryl Acetamides: In-Vitro Evaluation of Α-Glucosidase Inhibition, Docking, and Kinetic Studies', Bioorganic Chemistry, 102(), pp. -.
Vancouver	Moghimi S, Toolabi M, Salarinejad S, Firoozpour L, Sadat Ebrahimi SE, Safari F, et al.. Design and Synthesis of Novel Pyridazine N-Aryl Acetamides: In-Vitro Evaluation of Α-Glucosidase Inhibition, Docking, and Kinetic Studies. Bioorganic Chemistry. 2020;102():-.
BibTex	@article{ author = {Moghimi S and Toolabi M and Salarinejad S and Firoozpour L and Sadat Ebrahimi SE and Safari F and Mojtabavi S and Faramarzi MA and Foroumadi A}, title = {Design and Synthesis of Novel Pyridazine N-Aryl Acetamides: In-Vitro Evaluation of Α-Glucosidase Inhibition, Docking, and Kinetic Studies}, journal = {Bioorganic Chemistry}, volume = {102}, number = {}, pages = {-}, year = {2020} }
RIS	TY - JOUR AU - Moghimi S AU - Toolabi M AU - Salarinejad S AU - Firoozpour L AU - Sadat Ebrahimi SE AU - Safari F AU - Mojtabavi S AU - Faramarzi MA AU - Foroumadi A TI - Design and Synthesis of Novel Pyridazine N-Aryl Acetamides: In-Vitro Evaluation of Α-Glucosidase Inhibition, Docking, and Kinetic Studies JO - Bioorganic Chemistry VL - 102 IS - SP - EP - PY - 2020 ER -

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