Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies

Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies Publisher Pubmed

Adib M¹ ; Peytam F¹ ; Shourgeshty R¹ ; Mohammadikhanaposhtani M² ; Jahani M¹ ; Imanparast S³ ; Faramarzi MA³ ; Larijani B⁴ ; Moghadamnia AA^{2, 5} ; Esfahani EN⁶ ; Bandarian F⁶ ; Mahdavi M⁴

Show Affiliations

1. School of Chemistry, College of Science, University of Tehran, PO Box 14155-6455, Tehran, Iran
2. Cellular and Molecular Biology Research Center, Health Research Institute, Babol University of Medical Sciences, Babol, Iran
3. Department of Pharmaceutical Biotechnology, Faculty of Pharmacy and Biotechnology Research Center, Tehran University of Medical Sciences, Tehran, Iran
4. Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran
5. Department of Pharmacology, Faculty of Medical Sciences, Babol University of Medical Sciences, Babol, Iran
6. Diabetes Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran

Source: Bioorganic and Medicinal Chemistry Letters Published:2019

Abstract

Twenty three fused carbazole–imidazoles 6a–w were designed, synthesized, and screened as new α-glucosidase inhibitors. All the synthesized fused carbazole-imidazoles 6a-w were found to be more active than acarbose (IC 50 = 750.0 ± 1.5 µM) against yeast α-glucosidase with IC 50 values in the range of 74.0 ± 0.7–298.3 ± 0.9 µM. Kinetic study of the most potent compound 6v demonstrated that this compound is a competitive inhibitor for α-glucosidase (K i value = 75 µM). Furthermore, the in silico studies of the most potent compounds 6v and 6o confirmed that these compounds interacted with the key residues in the active site of α-glucosidase. © 2019

Style	Citing Format
MLA	Adib M, et al.. "Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies." Bioorganic and Medicinal Chemistry Letters, vol. 29, no. 5, 2019, pp. 713-718.
APA	Adib M, Peytam F, Shourgeshty R, Mohammadikhanaposhtani M, Jahani M, Imanparast S, Faramarzi MA, Larijani B, Moghadamnia AA, Esfahani EN, Bandarian F, Mahdavi M (2019). Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies. Bioorganic and Medicinal Chemistry Letters, 29(5), 713-718.
Chicago	Adib M, Peytam F, Shourgeshty R, Mohammadikhanaposhtani M, Jahani M, Imanparast S, Faramarzi MA, et al.. "Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies." Bioorganic and Medicinal Chemistry Letters 29, no. 5 (2019): 713-718.
Harvard	Adib M et al. (2019) 'Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies', Bioorganic and Medicinal Chemistry Letters, 29(5), pp. 713-718.
Vancouver	Adib M, Peytam F, Shourgeshty R, Mohammadikhanaposhtani M, Jahani M, Imanparast S, et al.. Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies. Bioorganic and Medicinal Chemistry Letters. 2019;29(5):713-718.
BibTex	@article{ author = {Adib M and Peytam F and Shourgeshty R and Mohammadikhanaposhtani M and Jahani M and Imanparast S and Faramarzi MA and Larijani B and Moghadamnia AA and Esfahani EN and Bandarian F and Mahdavi M}, title = {Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies}, journal = {Bioorganic and Medicinal Chemistry Letters}, volume = {29}, number = {5}, pages = {713-718}, year = {2019} }
RIS	TY - JOUR AU - Adib M AU - Peytam F AU - Shourgeshty R AU - Mohammadikhanaposhtani M AU - Jahani M AU - Imanparast S AU - Faramarzi MA AU - Larijani B AU - Moghadamnia AA AU - Esfahani EN AU - Bandarian F AU - Mahdavi M TI - Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies JO - Bioorganic and Medicinal Chemistry Letters VL - 29 IS - 5 SP - 713 EP - 718 PY - 2019 ER -

Style

Citing Format

MLA

Adib M, et al.. "Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies." Bioorganic and Medicinal Chemistry Letters, vol. 29, no. 5, 2019, pp. 713-718.

APA

Adib M, Peytam F, Shourgeshty R, Mohammadikhanaposhtani M, Jahani M, Imanparast S, Faramarzi MA, Larijani B, Moghadamnia AA, Esfahani EN, Bandarian F, Mahdavi M (2019). Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies. Bioorganic and Medicinal Chemistry Letters, 29(5), 713-718.

Chicago

Adib M, Peytam F, Shourgeshty R, Mohammadikhanaposhtani M, Jahani M, Imanparast S, Faramarzi MA, et al.. "Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies." Bioorganic and Medicinal Chemistry Letters 29, no. 5 (2019): 713-718.

Harvard

Adib M et al. (2019) 'Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies', Bioorganic and Medicinal Chemistry Letters, 29(5), pp. 713-718.

Vancouver

Adib M, Peytam F, Shourgeshty R, Mohammadikhanaposhtani M, Jahani M, Imanparast S, et al.. Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies. Bioorganic and Medicinal Chemistry Letters. 2019;29(5):713-718.

BibTex

@article{ author = {Adib M and Peytam F and Shourgeshty R and Mohammadikhanaposhtani M and Jahani M and Imanparast S and Faramarzi MA and Larijani B and Moghadamnia AA and Esfahani EN and Bandarian F and Mahdavi M}, title = {Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies}, journal = {Bioorganic and Medicinal Chemistry Letters}, volume = {29}, number = {5}, pages = {713-718}, year = {2019} }

RIS

TY - JOUR
AU - Adib M
AU - Peytam F
AU - Shourgeshty R
AU - Mohammadikhanaposhtani M
AU - Jahani M
AU - Imanparast S
AU - Faramarzi MA
AU - Larijani B
AU - Moghadamnia AA
AU - Esfahani EN
AU - Bandarian F
AU - Mahdavi M
TI - Design and Synthesis of New Fused Carbazole-Imidazole Derivatives As Anti-Diabetic Agents: In Vitro Α-Glucosidase Inhibition, Kinetic, and in Silico Studies
JO - Bioorganic and Medicinal Chemistry Letters
VL - 29
IS - 5
SP - 713
EP - 718
PY - 2019
ER -

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