Design, Synthesis and Α-Glucosidase Inhibition Study of Novel Pyridazin-Based Derivatives

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Design, Synthesis and Α-Glucosidase Inhibition Study of Novel Pyridazin-Based Derivatives Publisher

Firoozpour L¹ ; Kazemzadeh Arasi F² ; Toolabi M³ ; Moghimi S¹ ; Armandeh M⁴ ; Salmani F⁵ ; Pakrad R⁵ ; Firuzpour H⁵ ; Ghasemi Dogaheh M⁶ ; Ebrahimi SES² ; Hme Ketabforoosh S⁷ ; Karima S⁵ ; Foroumadi A^{1, 2}

Show Affiliations

1. Department of Medicinal Chemistry, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
2. Department of Medicinal Chemistry, School of Pharmacy, Tehran University of Medical Sciences, International Campus, Tehran, Iran
3. Department of Medicinal Chemistry, School of Pharmacy, Ahvaz Jundishapur University of Medical Sciences, Ahvaz, Iran
4. Department of Toxicology and Pharmacology, Faculty of Pharmacy, Toxicology and Disease Group, Pharmaceutical Sciences Research Center (PSRC), The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran
5. Department of Clinical Biochemistry, School of Medicine, Shahid Beheshti University of Medical Sciences (SBMU), Tehran, Iran
6. Drug Design and Development Research Center, The Institute of Pharmaceutical Sciences (TIPS), Tehran University of Medical Sciences, Tehran, Iran
7. Department of Medicinal Chemistry, School of Pharmacy, Alborz University of Medical Sciences, Karaj, Iran

Source: Medicinal Chemistry Research Published:2023

Abstract

In this paper, pyridazin derivatives containing different thiobenzyl moieties were synthesized and screened for their inhibitory activities against rat intestinal α-glucosidase enzyme. The final products were easily obtained without the need to harsh purification steps. The in vitro results revealed that all the synthesized compounds were more potent (IC50s = 26.3–148.9 μM) than the clinically used drug, acarbose. The kinetic study revealed the competitive inhibition behavior of compound 5m (Ki = −56 μM). Docking studies showed imperative interactions such as hydrogen bonding, Pi-Pi T-shaped, and Pi-anion interactions confirming the observed activity. The RMSD value was determined less than 3 A and validated the study. Graphical Abstract: [Figure not available: see fulltext.] © 2023, The Author(s), under exclusive licence to Springer Science+Business Media, LLC, part of Springer Nature.

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Style	Citing Format
MLA	Firoozpour L, et al.. "Design, Synthesis and Α-Glucosidase Inhibition Study of Novel Pyridazin-Based Derivatives." Medicinal Chemistry Research, vol. 32, no. 4, 2023, pp. 713-722.
APA	Firoozpour L, Kazemzadeh Arasi F, Toolabi M, Moghimi S, Armandeh M, Salmani F, Pakrad R, Firuzpour H, Ghasemi Dogaheh M, Ebrahimi SES, Hme Ketabforoosh S, Karima S, Foroumadi A (2023). Design, Synthesis and Α-Glucosidase Inhibition Study of Novel Pyridazin-Based Derivatives. Medicinal Chemistry Research, 32(4), 713-722.
Chicago	Firoozpour L, Kazemzadeh Arasi F, Toolabi M, Moghimi S, Armandeh M, Salmani F, Pakrad R, et al.. "Design, Synthesis and Α-Glucosidase Inhibition Study of Novel Pyridazin-Based Derivatives." Medicinal Chemistry Research 32, no. 4 (2023): 713-722.
Harvard	Firoozpour L et al. (2023) 'Design, Synthesis and Α-Glucosidase Inhibition Study of Novel Pyridazin-Based Derivatives', Medicinal Chemistry Research, 32(4), pp. 713-722.
Vancouver	Firoozpour L, Kazemzadeh Arasi F, Toolabi M, Moghimi S, Armandeh M, Salmani F, et al.. Design, Synthesis and Α-Glucosidase Inhibition Study of Novel Pyridazin-Based Derivatives. Medicinal Chemistry Research. 2023;32(4):713-722.
BibTex	@article{ author = {Firoozpour L and Kazemzadeh Arasi F and Toolabi M and Moghimi S and Armandeh M and Salmani F and Pakrad R and Firuzpour H and Ghasemi Dogaheh M and Ebrahimi SES and Hme Ketabforoosh S and Karima S and Foroumadi A}, title = {Design, Synthesis and Α-Glucosidase Inhibition Study of Novel Pyridazin-Based Derivatives}, journal = {Medicinal Chemistry Research}, volume = {32}, number = {4}, pages = {713-722}, year = {2023} }
RIS	TY - JOUR AU - Firoozpour L AU - Kazemzadeh Arasi F AU - Toolabi M AU - Moghimi S AU - Armandeh M AU - Salmani F AU - Pakrad R AU - Firuzpour H AU - Ghasemi Dogaheh M AU - Ebrahimi SES AU - Hme Ketabforoosh S AU - Karima S AU - Foroumadi A TI - Design, Synthesis and Α-Glucosidase Inhibition Study of Novel Pyridazin-Based Derivatives JO - Medicinal Chemistry Research VL - 32 IS - 4 SP - 713 EP - 722 PY - 2023 ER -

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