An overview of the synthetic routes to essential oral anti-diabetes drugs

Sagandira, Cloudius R.; Sagandira, Mellisa B.; Watts, Paul

doi:10.1016/j.tet.2021.132378

Cited by 18 publications

(10 citation statements)

References 57 publications

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“…Finally, the reactions in the systems were stopped using 2 mL of Na 2 CO 3 aqueous solution (0.1 M). After that, the absorbance of the released nitrophenol from pNPG in the systems in the existence of the materials and in the absence of them (controls) was detected using a microplate reader at 420 nm and applied to calculate the inhibition percentage, as in Equation (5).…”

Section: Inhibition Assay Of α-Glucosidasementioning

confidence: 99%

“…Type-2, as a stark metabolic disorder, is the mostly detected diabetes type and might affect up to 90% of patients by 2030 [1,4]. Normally, it is associated with post-prandial hyperglycemia (abnormal glucose levels) and abnormal release of reactive free oxidizing radicals (reactive oxygen species (ROS)) [5,6]. Cardiomyopathy, polyphagia, kidney failure, coronary heart disease, polydipsia, morbidity, mortality, nephropathy, neuropathy, glycosuria, and retinopathy are the common types of clinical complications that are related to type-2 diabetes mellitus and abnormal levels of blood glucose [7][8][9].…”

Section: Introductionmentioning

confidence: 99%

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Insight into the Potential Antioxidant and Antidiabetic Activities of Scrolled Kaolinite Single Sheet (KNs) and Its Composite with ZnO Nanoparticles: Synergetic Studies

et al. 2023

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The kaolinite sheets were scrolled by sonication-induced chemical delamination processes into well-developed nanotubes (KNs) which were used as substrates for microwave-based ZnO nanoparticles (ZnO/KNs). The biological activities of synthetic ZnO/KNs structures, in terms of the antioxidant and antidiabetic properties, were assessed in comparative studies with the separated phases of the synthetic ZnO and KNs as well as the commercially used ZnO. The KNs substrate resulted in a notable enhancement in the antioxidant and antidiabetic properties of ZnO, which was assigned positive influence on the surface area, interactive interfaces, charge separation, and agglomeration properties of ZnO in addition to the detectable bioactive properties of the KNs structure. The ZnO/KNs structure achieved remarkable scavenging efficiencies for 1, 1-diphenyl-2-picrylhydrazil (DPPH) (89.8 ± 1.57%), nitric oxide (90.6 ± 1.63%), 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) (ABTS) (86.8 ± 1.28%), and superoxide (43.9 ± 1.72%) radicals. Additionally, it shows high inhibition effects on porcine α-amylase (84.3 ± 1.92%), crude α-amylase (70.6 ± 1.37%), pancreatic α-Glucosidase (94.7 ± 1.54%), crude α-Glucosidase (95.4 ± 1.64%), and amyloglucosidase (95.3 ± 1.32%) enzymes. This antidiabetic activity is significantly higher than the activity of miglitol and close to or slightly higher than acarbose, which leads us to recommend the use of ZnO/KNs when considering the cost and side effects of the commercially used drugs.

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Section: Inhibition Assay Of α-Glucosidasementioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Insight into the Potential Antioxidant and Antidiabetic Activities of Scrolled Kaolinite Single Sheet (KNs) and Its Composite with ZnO Nanoparticles: Synergetic Studies

et al. 2023

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“…Next, the viability of this method with respect to Nchloroamines was probed (Scheme 2). Varieties of cyclic Nchloroamines, including bicyclic and spirocyclic derivatives with four-to seven-membered rings, were competent substrates to give satisfactory outcomes (23)(24)(25)(26)(27)(28)(29). N-chloroamines derived from primary amines were also examined, and N-chlorobenzylamine was set as the model substrate for optimization.…”

Section: Methodsmentioning

confidence: 99%

Dearomative Aminocarbonylation of Arenes via Bifunctional Coordination to Chromium

Wang

Zeng

et al. 2022

Angew Chem Int Ed

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Amides are ubiquitous in physical and life sciences. Given the significant abundance of arenes, dearomative aminocarbonylation of arenes would lead to a large and underexplored chemical space for amide discovery. However, such reactions are challenging due to the high degree of resonance stabilization and selectivity issues. Herein, we disclose an unprecedented dearomative trifluoromethylative aminocarbonylation of arenes via bifunctional coordination to chromium, providing a modular platform for the construction of amides possessing trifluoromethyl (CF 3 ) groups and three-dimensional rings. Its versatility further enabled a switchable difluoromethylation or trifluoromethylation aminocarbonylation of arene CÀ H bonds. A possible mechanism was proposed based on control experiments. Finally, the synthetic utility was well demonstrated by diverse applications in the total synthesis of CF 3 -functionalized amide-type drugs, including praziquantel, nateglinide, maraviroc and alloyohimbane.

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“…The trifluoromethylated analog of anthelmintic drug praziquantel [23] 72 was easily prepared from (η 6 -benzene)Cr-(CO) 3 through the established dearomative trifluoromethylative aminocarbonylation followed by a hydrogenation process (Scheme 5B). Starting from the enantioenriched product (À )-38, the trifluoromethylated analog of antidiabetic drug nateglinide [24] 73-1 were produced in 90 % yield through hydrogenation and esterlysis treatment (Scheme 5C). The enantioselective synthesis of trifluoromethylated analog of anti-AIDS drug maraviroc [25] 75 was successfully conducted within 3 steps from one of the diastereoisomers of 42 (Scheme 5D).…”

Section: Methodsmentioning

confidence: 99%

Dearomative Aminocarbonylation of Arenes via Bifunctional Coordination to Chromium

Wang

Zeng

et al. 2022

Angewandte Chemie

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An overview of the synthetic routes to essential oral anti-diabetes drugs

Cited by 18 publications

References 57 publications

Insight into the Potential Antioxidant and Antidiabetic Activities of Scrolled Kaolinite Single Sheet (KNs) and Its Composite with ZnO Nanoparticles: Synergetic Studies

Insight into the Potential Antioxidant and Antidiabetic Activities of Scrolled Kaolinite Single Sheet (KNs) and Its Composite with ZnO Nanoparticles: Synergetic Studies

Dearomative Aminocarbonylation of Arenes via Bifunctional Coordination to Chromium

Dearomative Aminocarbonylation of Arenes via Bifunctional Coordination to Chromium

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