Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents

Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents Publisher

Mohammadikhanaposhtani M¹ ; Noori M² ; Valizadeh Y² ; Dastyafteh N² ; Ghomi MK² ; Mojtabavi S³ ; Faramarzi MA³ ; Hosseini S⁴ ; Biglar M² ; Larijani B² ; Rastegar H⁵ ; Hamedifar H⁶ ; Mirzazadeh R⁷ ; Mahdavi M²

Show Affiliations

1. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
2. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
3. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, Iran
4. Shahid Beheshti University of Medical Sciences, Tehran, Iran
5. Cosmetic products research center, Iranian food and drug administration, MOHE, Tehran, Iran
6. CinnaGen Medical Biotechnology Research Center, Alborz University of Medical Sciences, Karaj, Iran
7. Department of Biochemistry, Pasteur Institute of Iran, Tehran, Iran

Source: ChemistrySelect Published:2022

Abstract

In this work, novel anti-α-glucosidase agents, thieno[2,3-b]quinoline-acetamide derivatives 5 a–m have been designed and synthesized. These compounds were evaluated in vitro against yeast α-glucosidase. Most of the title new compounds exhibited a significant α-glucosidase inhibitory activity in comparison to positive control, acarbose. In this regards, the most potent compound amongst the tested compounds, compound 5 k, with IC50=48.66±0.02 μM was 15.6-fold more potent than acarbose. Compound 5 k was a competitive inhibitor into α-glucosidase and interacted with important residues of the active site of this enzyme. Three most potent compounds among the newly synthesized compounds 5 j–k and 5 m were evaluated in silico in term of the oral druglikeness and pharmacokinetic properties. The obtained results predicted that these compounds had satisfactory oral druglikeness and pharmacokinetic properties. © 2022 Wiley-VCH GmbH.

Style	Citing Format
MLA	Mohammadikhanaposhtani M, et al.. "Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents." ChemistrySelect, vol. 7, no. 44, 2022, pp. -.
APA	Mohammadikhanaposhtani M, Noori M, Valizadeh Y, Dastyafteh N, Ghomi MK, Mojtabavi S, Faramarzi MA, Hosseini S, Biglar M, Larijani B, Rastegar H, Hamedifar H, Mirzazadeh R, Mahdavi M (2022). Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents. ChemistrySelect, 7(44), -.
Chicago	Mohammadikhanaposhtani M, Noori M, Valizadeh Y, Dastyafteh N, Ghomi MK, Mojtabavi S, Faramarzi MA, et al.. "Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents." ChemistrySelect 7, no. 44 (2022): -.
Harvard	Mohammadikhanaposhtani M et al. (2022) 'Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents', ChemistrySelect, 7(44), pp. -.
Vancouver	Mohammadikhanaposhtani M, Noori M, Valizadeh Y, Dastyafteh N, Ghomi MK, Mojtabavi S, et al.. Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents. ChemistrySelect. 2022;7(44):-.
BibTex	@article{ author = {Mohammadikhanaposhtani M and Noori M and Valizadeh Y and Dastyafteh N and Ghomi MK and Mojtabavi S and Faramarzi MA and Hosseini S and Biglar M and Larijani B and Rastegar H and Hamedifar H and Mirzazadeh R and Mahdavi M}, title = {Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents}, journal = {ChemistrySelect}, volume = {7}, number = {44}, pages = {-}, year = {2022} }
RIS	TY - JOUR AU - Mohammadikhanaposhtani M AU - Noori M AU - Valizadeh Y AU - Dastyafteh N AU - Ghomi MK AU - Mojtabavi S AU - Faramarzi MA AU - Hosseini S AU - Biglar M AU - Larijani B AU - Rastegar H AU - Hamedifar H AU - Mirzazadeh R AU - Mahdavi M TI - Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents JO - ChemistrySelect VL - 7 IS - 44 SP - EP - PY - 2022 ER -

Style

Citing Format

MLA

Mohammadikhanaposhtani M, et al.. "Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents." ChemistrySelect, vol. 7, no. 44, 2022, pp. -.

APA

Mohammadikhanaposhtani M, Noori M, Valizadeh Y, Dastyafteh N, Ghomi MK, Mojtabavi S, Faramarzi MA, Hosseini S, Biglar M, Larijani B, Rastegar H, Hamedifar H, Mirzazadeh R, Mahdavi M (2022). Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents. ChemistrySelect, 7(44), -.

Chicago

Mohammadikhanaposhtani M, Noori M, Valizadeh Y, Dastyafteh N, Ghomi MK, Mojtabavi S, Faramarzi MA, et al.. "Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents." ChemistrySelect 7, no. 44 (2022): -.

Harvard

Mohammadikhanaposhtani M et al. (2022) 'Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents', ChemistrySelect, 7(44), pp. -.

Vancouver

Mohammadikhanaposhtani M, Noori M, Valizadeh Y, Dastyafteh N, Ghomi MK, Mojtabavi S, et al.. Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents. ChemistrySelect. 2022;7(44):-.

BibTex

@article{ author = {Mohammadikhanaposhtani M and Noori M and Valizadeh Y and Dastyafteh N and Ghomi MK and Mojtabavi S and Faramarzi MA and Hosseini S and Biglar M and Larijani B and Rastegar H and Hamedifar H and Mirzazadeh R and Mahdavi M}, title = {Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents}, journal = {ChemistrySelect}, volume = {7}, number = {44}, pages = {-}, year = {2022} }

RIS

TY - JOUR
AU - Mohammadikhanaposhtani M
AU - Noori M
AU - Valizadeh Y
AU - Dastyafteh N
AU - Ghomi MK
AU - Mojtabavi S
AU - Faramarzi MA
AU - Hosseini S
AU - Biglar M
AU - Larijani B
AU - Rastegar H
AU - Hamedifar H
AU - Mirzazadeh R
AU - Mahdavi M
TI - Synthesis, Α-Glucosidase Inhibition, in Silico Pharmacokinetic, and Docking Studies of Thieno[2,3-B]Quinoline-Acetamide Derivatives As New Anti-Diabetic Agents
JO - ChemistrySelect
VL - 7
IS - 44
SP -
EP -
PY - 2022
ER -

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Abstract