Synthesis and study of the α-amylase inhibitory potential of thiadiazole quinoline derivatives

Taha, Muhammad; Javid, Muhammad Tariq; Imran, Syahrul; Selvaraj, Manikandan; Chigurupati, Sridevi; Ullah, Hayat; Rahim, Fazal; Khan, Fahad; Mohammad, Jahidul Islam; Khan, Khalid Mohammed

doi:10.1016/j.bioorg.2017.08.003

Cited by 89 publications

(17 citation statements)

References 32 publications

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“…Screening results showed good α‐amylase inhibitory potential with inhibitory concentration 0.002±0.60 to 708.3±0.03 μM. Derivative with thiophene substitution showed better inhibition potential than acarbose with IC 50 value 53.02±0.612 μM [78] …”

Section: Synthetic Developments On N‐heterocyclic Compoundsmentioning

confidence: 98%

“…Derivative with thiophene substitution showed better inhibition potential than acarbose with IC 50 value 53.02 � 0.612 μM. [78] Kumar et al (2019) synthesized arylamides of phenylquinolin 92 to acarbose (IC 50 = 30.32 � 2.76 μM). 2-Iodo derivative (91 L)was found to be the most potent compound among all the drivatives.…”

Section: Five or Six Membered Unsaturated Ring Containing Three Nitro...mentioning

confidence: 99%

“…Screening results showed good α-amylase inhibitory potential with inhibitory concentration 0.002 � 0.60 to 708.3 � 0.03 μM. Derivative with thiophene substitution showed better inhibition potential than acarbose with IC 50 value 53.02 � 0.612 μM [78]. Kumar et al (2019) synthesized arylamides of phenylquinolin92 and screened them for amylase inhibition potential.…”

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confidence: 99%

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Recent Developments in the Synthesis of N‐Heterocyclic Compounds as α‐Amylase Inhibitors via In‐Vitro and In‐Silico Analysis: Future Drugs for Treating Diabetes

et al. 2022

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In nature, N‐heterocyclic compounds and their derivatives are abundant. They serve as the building blocks of many biological entities, such as enzymes, alkaloids, hormones, antibiotics, and vitamins. The treatment of diabetes is one of the major applications of heterocyclic compounds. Natural as well as synthetic, both types of heterocyclic compounds show anti‐diabetic activity. There is a plethora of literature on the hyper/hypoglycaemic activity of natural compounds. This review discusses the synthesis methods, yields of the reactions and Inhibitory concentration (IC50) values of all the synthesized derivatives via different assays such as 3,5‐dinitrosalicylic acid (DNS) or starch assays. IC50 values of all the derivatives have been compared with those of standard acarbose. Structure activity relationship of most potential compounds with α‐amylase enzyme is established to show the type of interactions between them. Molecular docking studies show the type of interaction between compounds and enzyme.

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Section: Synthetic Developments On N‐heterocyclic Compoundsmentioning

confidence: 98%

Section: Five or Six Membered Unsaturated Ring Containing Three Nitro...mentioning

confidence: 99%

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confidence: 99%

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Recent Developments in the Synthesis of N‐Heterocyclic Compounds as α‐Amylase Inhibitors via In‐Vitro and In‐Silico Analysis: Future Drugs for Treating Diabetes

et al. 2022

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“…Alpha amylase activity was determined by a method adapted from the work of Taha et al [15] accordingly, α-amylase solution, phosphate buffer and starch from the reaction components were incubated in an eppendorf tube at 35 °C for 10 minutes. 100 µL of dinitrosalicylic acid (DNS) was added to the reaction and the reaction mixture was boiled for 5 minutes to stop the reaction.…”

Section: Enzymes Methodsmentioning

confidence: 99%

Describing a novel chemotherapeutic drug formulated by Diosmin for the treatment of acute lymphoblastic leukemia and diabetes mellitus

Liu

Cui

et al. 2021

Arch Med Sci

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IntroductionDiosmin is a natural citrus flavone with remarkable antioxidant and anti-inflammatory features. Acute leukemia is a common type of cancer that is caused in the blood.Material and methodsAlpha amylase activity was determined by a method adapted from the work of Taha et al.ResultsIn this study, we examined its effect on some important enzymes, the IC50 values were 196.07 for Aldose reductase, and 76.40 for alpha amylase. The molecular docking study was performed to assess the binding affinity and biological activities of diosmin in the presence of alpha amylase and aldose reductase. The results of the docking study indicated that diosmin has a remarkable binding affinity to these enzymes with a docking score of -9.768 and -140469 for alpha-amylase and aldose reductase, respectively. Therefore, this compound could be used as a potential inhibitor for these enzymes. In the cellular and molecular part of the recent study, the treated cells with Diosmin were assessed by MTT assay for 48h about the cytotoxicity and anti-human acute lymphoblastic leukemia properties on HL-60, Clone 15 HL-60, HL-60/MX1, and HL-60/MX2 cell lines. The IC50 of Diosmin were 466, 323, 502, and 537 µg/mL against HL-60, Clone 15 HL-60, HL-60/MX1, and HL-60/MX2 cell lines, respectively.ConclusionsThe viability of acute lymphoblastic leukemia cell lines reduced dose-dependently in the presence of Diosmin. It appears that the anti-human acute lymphoblastic leukemia effect of Diosmin is due to their antioxidant effects.

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“…The 1,3,4-thiadiazole, a unique structure, is a key motif in heterocyclic chemistry and also has a prominent spot in medicinal chemistry, due to its wide of pharmacological effects (Taha et al 2017). Importantly, 1,3,4-thiadiazole derivatives were identified for their antibacterial, antifungal, antiviral, anti-inflammatory, anti-anxiety, anti-convulsant, anti-cancer, anti-depressant and anti-tuberculosis activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, docking study, and in vitro anticancer evaluation of new flufenamic acid derivatives

Al-Bayati¹,

Mahmood²,

Al-Mazaydeh³

et al. 2021

PHAR

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Novel compounds (6–10) were synthesized and confirmed by spectroscopic analysis, including AT-IR, 1HNMR and CHNS. Their cytotoxic effect was evaluated by MTT assay against two cancer cell lines and two normal cell types. Compound 7 exhibited anticancer activity against MCF-7 breast cancer cell line (GI50 = 63.9 µg/ml, 148 µM), without any effect against A549 lung cancer cells, or the normal cells. Compound 7 caused cytotoxicity in MCF-7 breast cancer cells by apoptotic cell death, as suggested by fragmented nuclei after DAPI staining and agarose gel electrophoresis. In addition, treating MCF-7 cells with compound 7 resulted in an increase in the level of caspase 9 mRNA level, and its activation. Moreover, compound 7-treated MCF-7 cells showed enhanced cytochrome c release from the mitochondria to the cytosol, signifying an induction of the intrinsic apoptotic pathway. Finally, compound 7 exhibited epidermal growth factor receptor (EGFR) kinase inhibitory activity at (EC50 = 0.13 µM), which was matched by molecular docking studies that showed compound 7 might be an important EGFR kinase inhibitor.

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Synthesis and study of the α-amylase inhibitory potential of thiadiazole quinoline derivatives

Cited by 89 publications

References 32 publications

Recent Developments in the Synthesis of N‐Heterocyclic Compounds as α‐Amylase Inhibitors via In‐Vitro and In‐Silico Analysis: Future Drugs for Treating Diabetes

Recent Developments in the Synthesis of N‐Heterocyclic Compounds as α‐Amylase Inhibitors via In‐Vitro and In‐Silico Analysis: Future Drugs for Treating Diabetes

Describing a novel chemotherapeutic drug formulated by Diosmin for the treatment of acute lymphoblastic leukemia and diabetes mellitus

Synthesis, docking study, and in vitro anticancer evaluation of new flufenamic acid derivatives

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