(2E)-2-(4-ethoxybenzylidene)-3,4-dihydro-2H-naphthalen-1-one single crystal: Synthesis, growth, crystal structure, spectral characterization, biological evaluation and binding interactions with SARS-CoV-2 main protease

Afsar, N.; Jonathan, D. Reuben; Revathi, B.; Satheesh, Dhurairaj; Manivannan, S.

doi:10.1016/j.molstruc.2021.130967

Cited by 9 publications

(1 citation statement)

References 42 publications

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“…Given this context, in order to enable the emergence of new classes of more effective drugs, new alternatives with fewer side effects and lower cost have been developed [15,16]. Chalcones, which belong to the class of flavonoids, have attracted the attention of researchers not only from a synthetic and biosynthetic point of view but also from a pharmacological point of view [17]. Claisen-Schmidt condensation is typically used to synthesize chalcones in the presence of basic catalysts [18,19].…”

Section: Introductionmentioning

confidence: 99%

Antidiabetic Activities and GC-MS Analysis of 4-Methoxychalcone

Acho,

Oliveira,

Carneiro

et al. 2024

AppliedChem

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Diabetes mellitus is a chronic metabolic disease that is mainly characterized by hyperglycemia. Chalcones and their derivatives have demonstrated promising pharmacological potential for the treatment of diabetes. The aim of the study was to evaluate antidiabetic activities and analyze 4-methoxychalcone (MPP) using GC-MS. The compound was characterized using mass spectroscopy, nuclear magnetic resonance and headspace with gas chromatography coupled to mass spectrometry (HS-GC-MS). MPP was evaluated via the inhibition of the alpha-glucosidase enzyme, cell viability and antiglycation and hemolytic activities in vitro. The study of the interaction between the bovine serum albumin protein and MPP was investigated via molecular docking. Oral sucrose tolerance and oral glucose tolerance tests were performed in streptozotocin (STZ)-induced diabetic mice. The HS-GC-MS method was able to accurately detect and characterize the compound, and the interaction between MPP and BSA revealed the remarkable affinity for the two main binding sites of BSA. This was confirmed by the in vitro antiglycation test, since MPP showed activity through both oxidative and non-oxidative stress. MPP significantly attenuated the increase in glycemia after glucose loading in STZ-induced diabetic mice. These results confirm that MPP has antihyperglycemic activity and may be an alternative for the treatment of diabetes mellitus.

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