Design, Synthesis, Antibacterial Activity, and Molecular Docking Studies of Novel Hybrid 1,3‐Thiazine‐1,3,5‐Triazine Derivatives as Potential Bacterial Translation Inhibitor

BackgroundCognitive decline (e.g., memory loss), which mainly occurs in the elderly, is termed dementia. In the present study, we intended to explore the cholinesterase inhibitory activity of some novel synthesized chalcones, together with their effect on β-amyloid anti-aggregation.Material/MethodsA novel class of chalcone derivatives have been synthesized and characterized by FT-IR, 1H-NMR, 13C-NMR, and mass and elemental analysis. These derivatives were later used for the determination of acetylcholinesterase (AChE) inhibitory and β-amyloid anti-aggregation activity.ResultsThe results of the study showed that among the developed compounds, 8g inhibits AChE more prominently than BuChE, as suggested by a selectivity index (SI) of 2.88. Furthermore, the most potent compound, 8g, showed considerable action in inhibition of β-secretase and Aβ aggregation, but not as prominent as that of curcumin as a standard.ConclusionsIn conclusion, our study revealed a novel class of chalcone derivatives as a selective inhibitor of AChE with considerably action against β-secretase and Aβ aggregation. Our results may be useful in developing AD drug therapy and warrant further investigation to generate more advanced analogues.

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“…The resultant solid was then filtered off, washed with water, dried, and re-crystallized from ethanol [27]. …”

Section: Methodsmentioning

confidence: 99%

Design and Development of a Novel Chalcone Derivative as an Anticholinesterase Inhibitor for Possible Treatment of Dementia

Zhao

Song

2017

Med Sci Monit

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“…In this regard, derivatives of 1,3,5‐triazine have received considerable attention . 1,3,5‐Triazines have various pharmacological activities, such as antibacterial, antifungal, antimalarial, antidiabetic and anticystic fibrosis effects. Moreover, 1,3,5‐triazine exerts anticancer effects by inhibiting PI3K/mTOR, Rad6 ubiquitin conjugating enzyme and human epidermal growth factor receptor tyrosine kinases (EGFR‐TKs) …”

Section: Introductionmentioning

confidence: 99%

Novel 1,3,5‐triazine derivatives exert potent anti‐cervical cancer effects by modulating Bax, Bcl2 and Caspases expression

Wang

et al. 2017

Chem Biol Drug Des

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This study aimed to develop novel 1,3,5-triazine derivatives as potent anti-cervical cancer agents. The compounds were synthesized in short steps with an excellent yield and characterized via various spectroscopic and analytical methods. A structure-activity relationship study suggested that electron-withdrawing substituents showed greater anticancer activity than electron-donating groups. Compound 7p (p-fluoro) showed the highest activity against cervical cancer cells. In a nude mouse xenograft model inoculated with HeLa cells, 7p showed dose-dependent inhibition of cervical tumour growth. Histopathological examination of excised tumour-bearing tissues showed that 7p improved the microstructure in a dose-dependent manner. Compound 7p also increased the proportions of HeLa cells in G0/G1 and S-phase and significantly decreased that of G2/M-phase. The effects of 7p on C-caspase-3, C-caspase-9, Bcl-2 and Bax expression in HeLa cells were also determined.

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“…Concerning the immense pharmacological activity of 1,3,5‐triazine and in follow up of our previous studies toward the development of novel antibacterial compounds derived from 1,3,5‐triazine, here we wish to report a novel class of hybrid 4‐aminoquinoline 1,3,5‐triazine .…”

Section: Introductionmentioning

confidence: 99%

Hybrid 4‐Aminoquinoline‐1,3,5‐triazine Derivatives: Design, Synthesis, Characterization, and Antibacterial Evaluation

Pathak

Thakur

Bhat

et al. 2014

Journal of Heterocyclic Chem

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A series of novel 4‐aminoquinoline 1,3,5‐triazine derivatives were synthesized and characterized by FTIR, 1H‐NMR, 13C‐NMR, MS, and elemental analysis. The antibacterial activities of synthesized compounds were tested against three Gram‐positive bacteria, namely Bacillus subtilis (NCIM‐2063), Bacillus cereus (NCIM‐2156), and Staphylococcus aureus (NCIM‐2079), and four Gram‐negative bacteria, namely Proteus vulgaris (NCIM‐2027), Proteus mirabilis (NCIM‐2241), Escherichia coli (NCIM‐2065), and Pseudomonas aeruginosa (NCIM‐2036), using ciprofloxacin as reference standard drug. Results showed compound 9a and 9e as potent antibacterial agents against all bacterial strains except Bacillus cereus (NCIM‐2156). Copyright © 2014 HeteroCorporation

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Design, Synthesis, Antibacterial Activity, and Molecular Docking Studies of Novel Hybrid 1,3‐Thiazine‐1,3,5‐Triazine Derivatives as Potential Bacterial Translation Inhibitor

Cited by 47 publications

References 18 publications

Design and Development of a Novel Chalcone Derivative as an Anticholinesterase Inhibitor for Possible Treatment of Dementia

Design and Development of a Novel Chalcone Derivative as an Anticholinesterase Inhibitor for Possible Treatment of Dementia

Novel 1,3,5‐triazine derivatives exert potent anti‐cervical cancer effects by modulating Bax, Bcl2 and Caspases expression

Hybrid 4‐Aminoquinoline‐1,3,5‐triazine Derivatives: Design, Synthesis, Characterization, and Antibacterial Evaluation

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