Synthesis of new clioquinol derivatives as potent α-glucosidase inhibitors; molecular docking, kinetic and structure–activity relationship studies

Wali, S. K.; Atia-tul-Wahab, *; Ullah, Saeed; Khan, Maria Aqeel; Hussain, Shahid; Shaikh, Muniza; Atta-ur-Rahman, _; Choudhary, Muhammad Iqbal

doi:10.1016/j.bioorg.2021.105506

Cited by 19 publications

(8 citation statements)

References 45 publications

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“…The microbiology lab at NMSRC (Natural and Medical Sciences Research Center) at the University of Nizwa in Oman provided all the organisms for this investigation. Each extract was evaluated in Dimethyl Sulfoxide (DMSO) at four distinct concentrations: 125, 250, 500 and 1000 µg mLG 1 . By immersing filter paper discs (5 mm) in vials holding the prepared solutions, extracts were impregnated.…”

Section: Antibacterial Activity Using Disc Diffusion Methodmentioning

confidence: 99%

“…Type 2 diabetes is one of the main metabolic illnesses, which is brought on by insufficient insulin production, diminished insulin activity or both 1 . Leading long-term consequences of diabetes, obesity, metastatic cancer and cardiovascular disorders are all correlated with persistent hyperglycaemia 2 .…”

Section: Introductionmentioning

confidence: 99%

“…The AGIs have received a lot of attention recently due to their potential clinical applications in the treatment of hyperglycaemia and as antiviral medications. Because αglucosidase control the conversion of polysaccharides to monosaccharides in the small intestine, that is why its inhibition slowdown glucose absorption 1,5,6 .…”

Section: Introductionmentioning

confidence: 99%

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Pharmacology and Enzyme Inhibitory Potentials of Myrtus communis L. Fruits Grown in Oman

Alsenaidi,

Amush,

Ullah

et al. 2023

Trends Med. Res

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Background and Objective: Myrtus communis L. is a plant used in traditional medicine worldwide. Since many ages ago, this herb's berries have all been widely utilized as a traditional medicine to treat conditions like peptic ulcers, diarrhea, haemorrhoids, inflammation and skin diseases. The purpose of the study is to evaluate the antiulcer, antidiabetic enzymatic inhibition, antibacterial and antioxidant actions of different polarity extracts of fruits of Myrtus communis L. Materials and Methods: Methanol (crude extract) and its fractions (n-hexane (MCFH), dichloromethane (MCFD), ethyl acetate (MCFE), butanol (MCFB) and aqueous (MCFA)) from fruits of Myrtus communis L. were produced and assessed for their antimicrobial, antioxidant, α-glucosidase and antiulcer in vitro bioassays. All of the fractions were tested using a brine shrimp lethality assay to determine their cytotoxic effects. Results: The examined samples demonstrated a sizable capacity to fend off the gram-negative and gram-positive bacteria. The MCFB determined the best antibacterial activity of the five extracts, with an average inhibitions zone of 9.3 mm against Staphylococcus aureus and 6.75 mm against Escherichia coli. The MCFA extract displayed the second-highest antibacterial activity against Pseudomonas aeruginosa, with an average inhibition zone of 9.5 mm, while MCFH had the least amount of activity against the bacteria that were tested. In the anti-alpha glucosidase activity, MCFE was the best with IC 50 of 20.04±0.38 µg mLG 1 and the unease inhibition was best seen with the MCFA and MCFB extracts with IC 50 values of 146.87±1.39 and 194.97±1.68 µg mLG 1 , respectively. All extracts showed no significant cytotoxic activity. Conclusion: Therefore, all tested samples, especially MCFE and MCFB extracts, were assumed to have significant capacities for the studied activities.

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Section: Antibacterial Activity Using Disc Diffusion Methodmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Pharmacology and Enzyme Inhibitory Potentials of Myrtus communis L. Fruits Grown in Oman

Alsenaidi,

Amush,

Ullah

et al. 2023

Trends Med. Res

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“…Therefore, the inhibition of α-glucosidase might reduce carbohydrate digestion, delay glucose uptake, and consequently, decrease blood sugar levels 14 , 15 . The α-glucosidase enzyme can be inhibited by acarbose, voglibose, and miglitol with sub-optimal efficacy 16 . Also, long-term administration of mentioned inhibitor may cause several side effects, such as abdominal pain, diarrhea, and flatulence.…”

Section: Introductionmentioning

confidence: 99%

Design, synthesis, and in silico studies of quinoline-based-benzo[d]imidazole bearing different acetamide derivatives as potent α-glucosidase inhibitors

Noori

Davoodi

Iraji

et al. 2022

Sci Rep

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In this study, 18 novel quinoline-based-benzo[d]imidazole derivatives were synthesized and screened for their α-glucosidase inhibitory potential. All compounds in the series except 9q showed a significant α-glucosidase inhibition with IC50 values in the range of 3.2 ± 0.3–185.0 ± 0.3 µM, as compared to the standard drug acarbose (IC50 = 750.0 ± 5.0 µM). A kinetic study indicated that compound 9d as the most potent derivative against α-glucosidase was a competitive type inhibitor. Furthermore, the molecular docking study revealed the effective binding interactions of 9d with the active site of the α-glucosidase enzyme. The results indicate that the designed compounds have the potential to be further studied as new anti-diabetic agents.

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“…Inhibition of the α-glucosidase can limit the digestion of carbohydrates resulting in declined postprandial blood sugar levels [12]. As a result, α-glucosidase inhibitors (AGIs) can be used as first-line therapy for T2DM [13][14][15].…”

Section: Introductionmentioning

confidence: 99%

Enzymes Inhibition and Antioxidant Potential of Medicinal Plants Growing in Oman

Rehman

Shah

Ullah

et al. 2022

BioMed Research International

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The recent study was designed to explore Dodonaea viscosa, Juniperus excelsa, Helianthemum lippii, and Euryops pinifolius using methanolic (MeOH) extract. Their subfractions were examined against urease, carbonic anhydrase II (CA-II), α-glucosidase enzymes, and free radicals scavenging significance based on local practices via standard methods. Significance potential against the urease enzyme was presented by ethyl acetate fraction (EtOAc) of D. viscosa with ( I C 50 = 125 ± 1.75 μg/mL), whereas the H. lippii ( I C 50 = 1 46 ± 1.39 μg/mL) in the EtOAc was found efficient to scavenge the free radicals. Besides, that appreciable capacity was observed by the J. excelsa, D. viscosa, J. excelsa, and E. pinifolius as compared to the standard acarbose ( I C 50 = 377.24 ± 1.14 μg/mL). Maximum significance was noticed in methanolic (MeOH) extract of J. excelsa and presented carbonic anhydrase CA-II ( I C 50 = 5.1 ± 0.20 μg/mL) inhibition as compared to the standard (acetazolamide). We are reporting, for the first time, the CA-II inhibition of all the selected medicinal plants and α-glucosidase, urease, and antioxidant activities of the E. pinifolius. Thus, further screening is needed to isolate the promising bioactive ingredients which act as an alternative remedy to scavenge the free radicals, antiulcer, and act as a potential source to develop new antidiabetic drugs for controlling postprandial blood sugar as well as carbonic anhydrase inhibitors.

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Synthesis of new clioquinol derivatives as potent α-glucosidase inhibitors; molecular docking, kinetic and structure–activity relationship studies

Cited by 19 publications

References 45 publications

Pharmacology and Enzyme Inhibitory Potentials of Myrtus communis L. Fruits Grown in Oman

Pharmacology and Enzyme Inhibitory Potentials of Myrtus communis L. Fruits Grown in Oman

Design, synthesis, and in silico studies of quinoline-based-benzo[d]imidazole bearing different acetamide derivatives as potent α-glucosidase inhibitors

Enzymes Inhibition and Antioxidant Potential of Medicinal Plants Growing in Oman

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