Molecular modeling and synthesis of novel benzimidazole-derived thiazolidinone bearing chalcone derivatives: a promising approach to develop potential anti-diabetic agents DOI

Shahzad Ahmad Abbasi,

Wajid Rehman, Fakher Rahim

et al.

Zeitschrift für Naturforschung C, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 20, 2024

Abstract Diabetes mellitus (DM) is a disorder which raised at the alarming level and it characterized by hyperglycemia results from impaired action of insulin, production insulin or both these simultaneously. Consequently, causes problems failure different body organs such as kidneys, heart, eyes, nerve system. Since this disease cannot be completely cured until now, we aimed to design series enzymes inhibitors tested them for DM treatment. In series, benzimidazole-based thiazolidinone bearing chalcone derivatives completed in four step reaction their structures were confirmed through various spectroscopic techniques. A significant efficacy on antidiabetic was observed, with IC 50 values ranging 25.05 ± 0.04 56.08 0.07 μM α-amylase 22.07 0.02 53.06 α-glucosidase. The obtained compared those standard glimepiride drug (IC = 18.05 µM 15.02 0 .03 α-glucosidase). synthesized compounds showed promising potency. Moreover, molecular docking study conducted most active analogs better understand interactions sites targeted enzymes.

Language: Английский

Novel bis-benzimidazole-triazole hybrids: anticancer study, in silico approaches, and mechanistic investigation DOI
Moataz A. Soliman, Hany E. A. Ahmed, Elsayed H. Eltamany

et al.

Future Medicinal Chemistry, Journal Year: 2024, Volume and Issue: unknown, P. 1 - 15

Published: Dec. 13, 2024

Benzimidazole-triazole conjugates are very active hotspot for design and synthesis of promising anticancer agents. The target analogs showed potent selective cytotoxicity over different cancer cell lines breast lung ones.

Language: Английский

Citations

2

Recent Progress in the Synthesis and Biological Assessment of Benzimidazole-1,2,3- Triazole Hybrids DOI
Dileep Kumar Singh, Haider Iqbal, Mohd. Ayub Ansari

et al.

Current Organic Chemistry, Journal Year: 2024, Volume and Issue: 28(10), P. 733 - 756

Published: April 17, 2024

Abstract: In recent times, many research groups have focused their attention on nitrogencontaining heterocyclic compounds with the aim of gaining a deeper understanding biological characteristics. Among them, molecules based 1,2,3-triazole and benzimidazole exhibited diverse applications are present in drug molecules. The purpose this review is to describe various benzimidazole-1,2,3-triazole hybrids provide comprehensive evaluation properties. discussed study been synthesized through Cu(I)-catalyzed 1,3-dipolar cycloaddition reaction between azides alkynes, utilizing scaffold as linkage two connecting groups. synthesis several benzimidazole-1,2,3- triazole covered review, along assessment anticancer, antiproliferative, antitubercular, antibacterial, antidepressant, other activities. Moreover, our opinion, may be useful for development medicinally significant

Language: Английский

Citations

1

2-Benzimidazolamine-Acetamide Derivatives as Antibacterial Agents: Synthesis, ADMET, Molecular Docking, and Molecular Simulation Studies DOI

Nasreen Akhtar Mazumdar,

Afreen Inam,

Ayesha Akhtar

et al.

Synthesis, Journal Year: 2024, Volume and Issue: unknown

Published: Oct. 28, 2024

Abstract A series of 2-benzimidazolamine-acetamide derivatives were synthesized by substitution reaction different anilines with chloroacetyl chloride followed the 2-aminobenzimidazole formed substituted chloroacetamides. The structures all compounds elucidated various spectral techniques and evaluated against five bacterial strains. Out ten, N-(2-fluorophenyl)-substituted acetamide displayed better minimum inhibitory concentration (MIC). Disk diffusion assay combination studies also performed on same compound. Molecular docking this compound E. coli methionine aminopeptidase (METAP) effective binding, molecular dynamics simulation further suggested a stable complex formation. Thus, these results indicate that scaffolds can serve as model for developing antibacterial agents.

Language: Английский

Citations

1

Green synthesis of benzimidazole derivatives using copper(II)-supported on alginate hydrogel beads DOI

Khaoula Oudghiri,

Azzeddine Taoufyk,

Moha Taourirte

et al.

International Journal of Biological Macromolecules, Journal Year: 2024, Volume and Issue: 282, P. 137169 - 137169

Published: Nov. 2, 2024

Language: Английский

Citations

1

Molecular modeling and synthesis of novel benzimidazole-derived thiazolidinone bearing chalcone derivatives: a promising approach to develop potential anti-diabetic agents DOI

Shahzad Ahmad Abbasi,

Wajid Rehman, Fakher Rahim

et al.

Zeitschrift für Naturforschung C, Journal Year: 2024, Volume and Issue: unknown

Published: Nov. 20, 2024

Abstract Diabetes mellitus (DM) is a disorder which raised at the alarming level and it characterized by hyperglycemia results from impaired action of insulin, production insulin or both these simultaneously. Consequently, causes problems failure different body organs such as kidneys, heart, eyes, nerve system. Since this disease cannot be completely cured until now, we aimed to design series enzymes inhibitors tested them for DM treatment. In series, benzimidazole-based thiazolidinone bearing chalcone derivatives completed in four step reaction their structures were confirmed through various spectroscopic techniques. A significant efficacy on antidiabetic was observed, with IC 50 values ranging 25.05 ± 0.04 56.08 0.07 μM α-amylase 22.07 0.02 53.06 α-glucosidase. The obtained compared those standard glimepiride drug (IC = 18.05 µM 15.02 0 .03 α-glucosidase). synthesized compounds showed promising potency. Moreover, molecular docking study conducted most active analogs better understand interactions sites targeted enzymes.

Language: Английский

Citations

1