A comprehensive review of recent advances in the biological activities of 1,2,4‐oxadiazoles

Hendawy, Omnia M.

doi:10.1002/ardp.202200045

Cited by 21 publications

(5 citation statements)

References 93 publications

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“…In diabetic rats treated with 1,3,4-oxadiazole derivative as compared to the diseased, an increase in plasma insulin levels was observed. This could be due to the potential of insulin sensitivity on the cell membrane [ 39 ]. Improving insulin sensitivity is the ultimate physiological effect of oxadiazole derivative in improving the homeostasis of glucose [ 40 ].…”

Section: Discussionmentioning

confidence: 99%

Evaluation of Antidiabetic Activity of Oxadiazole Derivative in Rats

Qazi

Ahmad

Sahibzada³

et al. 2023

Evidence-Based Complementary and Alternative Medicine

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The oxadiazole ring has long been used for the treatment of several diseases. This study aimed to analyze the antihyperglycemic and antioxidant roles of the 1,3,4-oxadiazole derivative with its toxicity. Diabetes was induced through intraperitoneal administration of alloxan monohydrate at 150 mg/kg in rats. Glimepiride and acarbose were used as standards. Rats were divided into groups of normal control, disease control, standard, and diabetic rats (treated with 5, 10, and 15 mg/kg of 1,3,4-oxadiazole derivative). After 14 days of oral administration of 1,3,4-oxadiazole derivatives (5, 10, and 15 mg/kg) to the diabetic group, the blood glucose level, body weight, glycated hemoglobin (HbA1c), insulin level, antioxidant effect, and histopathology of the pancreas were performed. The toxicity was measured by estimating liver enzyme, renal function, lipid profile, antioxidative effect, and liver and kidney histopathological study. The blood glucose and body weight were measured before and after treatment. Alloxan significantly increased blood glucose levels, HbA1c, alanine transaminase, aspartate aminotransferase, urea, cholesterol, triglycerides, and creatinine. In contrast, body weight, insulin level, and antioxidant factors were reduced compared to the normal control group. Treatment with oxadiazole derivatives showed a significant reduction in blood glucose levels, HbA1c, alanine transaminase, aspartate aminotransferase, urea, cholesterol, triglycerides, and creatinine as compared to the disease control group. The 1,3,4-oxadiazole derivative significantly improved body weight, insulin level, and antioxidant factors compared to the disease control group. In conclusion, the oxadiazole derivative showed potential antidiabetic activity and indicated its potential as a therapeutic.

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Section: Discussionmentioning

confidence: 99%

Evaluation of Antidiabetic Activity of Oxadiazole Derivative in Rats

Qazi

Ahmad

Sahibzada³

et al. 2023

Evidence-Based Complementary and Alternative Medicine

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“…[43,44] 1,2,4-oxadiazoles are heterocyclic aromatic compounds that have shown promising potential for many biological applications, in particular as enzyme inhibitors. [45][46][47][48] Kraemer and coworkers performed a virtual screening for aldose reductase inhibitors and discovered a 1,2,4-oxadiazole derivative (BTB02809, in this work referred to as OXA) as a potent ALR2 antagonist (Figure 1). [49] We have synthesized this molecule and evaluated its ALR2 inhibition when incorporated in a lanthanide-based hydrogel as a new material to tackle diabetes complications.…”

Section: Introductionmentioning

confidence: 97%

Luminescent Supramolecular Metallogels: Drug Loading and Eu(III) as Structural Probe

Freire,

Coelho,

Maciel

et al. 2024

Chemistry A European J

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Supramolecular metallogels combine the rheological properties of gels with the color, magnetism, and other properties of metal ions. Lanthanide ions such as Eu(III) can be valuable components of metallogels due to their fascinating luminescence. In this work, we combine Eu(III) and iminodiacetic acid (IDA) into luminescent hydrogels. We investigate the tailoring of the rheological properties of these gels by changes in their metal:ligand ratio. Further, we use the highly sensitive Eu(III) luminescence to obtain information about the chemical structure of the materials. In special, we take advantage of computational calculations to employ an indirect method for structural elucidation, in which the simulated luminescent properties of candidate structures are matched to the experimental data. With this strategy, we can propose molecular structures for different EuIDA gels. We also explore the usage of these gels for the loading of bioactive molecules such as OXA, observing that its aldose reductase activity remains present in the gel. We envision that the findings from this work could inspire the development of luminescent hydrogels with tunable rheology for applications such as 3D printing and imaging‐guided drug delivery platforms. Finally, Eu(III) emission‐based structural elucidation could be a powerful tool in the characterization of advanced materials.

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“…Moreover, progress in the synthesis and medicinal application of the 1,2,4-oxadiazole core is being regularly reported (for recent reviews see Refs. [ 7 , 8 , 9 , 10 , 11 , 12 ]). The interesting feature of the 1,2,4-oxadiazole moiety from a medicinal chemistry viewpoint is its potential coverage of a broad spectrum of therapeutic areas, including oncology [ 13 , 14 , 15 ], immunology [ 16 ], neurology [ 17 , 18 , 19 , 20 ], infectious diseases [ 21 , 22 , 23 , 24 ], metabolism and endocrinology [ 25 , 26 , 27 , 28 ], urology [ 29 , 30 ], gastroenterology [ 31 ], cardiology [ 32 ], rheumatology [ 33 ], and respirology [ 34 ].…”

Section: Introductionmentioning

confidence: 99%

Room Temperature Synthesis of Bioactive 1,2,4-Oxadiazoles

Baykov

Shetnev

Semenov

et al. 2023

IJMS

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1,2,4-Oxadiazole is an essential motif in drug discovery represented in many experimental, investigational, and marketed drugs. This review covers synthetic methods that allow the conversion of different types of organic compounds into 1,2,4-oxadiazole at ambient temperature and the practical application of the latter approaches for the preparation of pharmaceutically important molecules. The discussed methods are divided into three groups. The first combines two-stage protocols requiring the preliminary preparation of O-acylamidoximes followed by cyclization under the action of organic bases. The advantages of this route are its swiftness, high efficiency of the cyclization process, and uncomplicated work--up. However, it requires the preparation and isolation of O-acylamidoximes as a separate preliminary step. The second route is a one-pot synthesis of 1,2,4-oxadiazoles directly from amidoximes and various carboxyl derivatives or aldehydes in aprotic bipolar solvents (primarily DMSO) in the presence of inorganic bases. This recently proposed pathway proved to be highly efficient in the field of medicinal chemistry. The third group of methods consists of diverse oxidative cyclizations, and these reactions have found modest application in drug design thus far. It is noteworthy that the reviewed methods allow for obtaining 1,2,4-oxadiazoles with thermosensitive functions and expand the prospects of using the oxadiazole core as an amide- or ester-like linker in the design of bioactive compounds.

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A comprehensive review of recent advances in the biological activities of 1,2,4‐oxadiazoles

Cited by 21 publications

References 93 publications

Evaluation of Antidiabetic Activity of Oxadiazole Derivative in Rats

Evaluation of Antidiabetic Activity of Oxadiazole Derivative in Rats

Luminescent Supramolecular Metallogels: Drug Loading and Eu(III) as Structural Probe

Room Temperature Synthesis of Bioactive 1,2,4-Oxadiazoles

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