Novel tacrine-coumarin hybrids linked to 1,2,3-triazole as anti-Alzheimer’s compounds: In vitro and in vivo biological evaluation and docking study

Najafi, Zahra; Mahdavi, Mohammad; Saeedi, Mina; Karimpour-Razkenari, Elahe; Edraki, Najmeh; Sharifzadeh, Mohammad; Khanavi, Mahnaz; Akbarzadeh, Tahmineh

doi:10.1016/j.bioorg.2018.10.056

Cited by 109 publications

(59 citation statements)

References 41 publications

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“…Among all these, compound 79a was the most potent anti-AChE derivative (IC 50 ¼ 27 nM) and compound 79b displayed the best anti-BChE activity (IC 50 ¼ 6 nM), which is much more active than tacrine and donepezil as the reference drugs. 123…”

Section: Anti-diabetic Activitymentioning

confidence: 99%

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

et al. 2020

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Section: Anti-diabetic Activitymentioning

confidence: 99%

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

et al. 2020

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“…Coumarins are found in several plant families and essential oils and are used as fragrant additives in food and cosmetics [12]. Many reports have suggested that the coumarins possess a huge array of biological roles, such as antithrombotic, neuroprotective, antidiabetic, anticoagulant, anti-inflammatory, antioxidant, and antiplasmodial activities [13][14][15][16][17][18][19]. Due to technical advancement, the coumarins and its derivatives are becoming a potential source for new drug discovery [20].…”

Section: Introductionmentioning

confidence: 99%

(E)-N′-(1-(7-Hydroxy-2-Oxo-2H-Chromen-3-Yl) Ethylidene) Benzohydrazide, a Novel Synthesized Coumarin, Ameliorates Isoproterenol-Induced Myocardial Infarction in Rats through Attenuating Oxidative Stress, Inflammation, and Apoptosis

Feriani

Khdhiri

Tir

et al. 2020

Oxidative Medicine and Cellular Longevity

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The present study was directed to investigate the effect of precotreatment with (E)-N′-(1-(7-hydroxy-2-oxo-2H-chromen-3-yl) ethylidene) benzohydrazide (7-hyd.HC), a novel potent synthesized coumarin, on isoproterenol- (ISO-) induced myocardial infarction (MI) in rats. The hydrazone compound was characterized by IR, 1D, and 2D NMR analyses. Experimental induction of MI in rats was established by ISO (85 mg/kg/day, s.c) for two consecutive days (6th and 7th days). 7-hyd.HC or sintrom was given for 7 days prior and simultaneous to ISO injection. 7-hyd.HC offered a cardiopreventive effect by preventing heart injury marker leakage (LDH, ALT, AST, CK-MB, and cTn-I) from cardiomyocytes and normalizing cardiac function and ECG pattern, as well as improving lipid profile (TC, TG, LDL-C, and HDL-C), which were altered by ISO administration. Moreover, 7-hyd.HC precotreatment significantly mitigated the oxidative stress biomarkers, as evidenced by the decrease of lipid peroxidation and the increased level of the myocardial GSH level together with the SOD, GSH-Px, and catalase activities. 7-hyd.HC inhibited the cardiac apoptosis by upregulating the expression of Bcl-2 and downregulating the expression of Bax and caspase-3 genes. In addition, 7-hyd.HC reduced the elevated fibrinogen rate and better prevented the myocardial necrosis and improved the interstitial edema and neutrophil infiltration than sintrom. Overall, 7-hyd.HC ameliorated the severity of ISO-induced myocardial infarction through improving the oxidative status, attenuating apoptosis, and reducing fibrinogen production. The 7-hyd.HC actions could be mediated by its antioxidant, antiapoptotic, and anti-inflammatory capacities.

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“…Coumarin (Figure 1) is a plant‐derived natural product, and the benzopyrone structure enables its derivatives to readily interact with diverse enzymes and receptors in organisms through weak bond interactions. [ 8–10 ] Therefore, coumarin derivatives possess a variety of pharmacological properties such as anti‐inflammatory, [ 11,12 ] anticancer, [ 13–16 ] anti‐Alzheimer, [ 17,18 ] antimycobacterial, [ 19,20 ] antifungal, [ 21,22 ] antimalarial, [ 23,24 ] antiviral, [ 25,26 ] anticoagulant, [ 27,28 ] and antibacterial activities. [ 29,30 ] The mechanistic study indicated that the antibacterial activity of coumarin derivatives was mainly due to their ability to bind to the B subunit of DNA gyrase in bacteria and inhibit DNA supercoiling by blocking the ATPase activity.…”

Section: Introductionmentioning

confidence: 99%

Coumarin‐containing hybrids and their antibacterial activities

Feng

Zhang

Yang

et al. 2020

Archiv der Pharmazie

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Infections caused by Gram-positive and -negative bacteria are one of the foremost causes of morbidity and mortality globally. Antibiotics are the mainstay of therapy for bacterial infections, but the emergence and wide spread of drug-resistant pathogens have already become a huge issue for public healthcare systems. The coumarin moiety, which is ubiquitous in nature, could bind to the B subunit of DNA gyrase in bacteria and inhibit DNA supercoiling by blocking the ATPase activity; hence, coumarin derivatives possess potential antibacterial activity. Several coumarin-containing hybrids such as coumermycin A1, clorobiocin, and novobiocin have already been used in clinical practice for the treatment of various bacterial infections; thus, it is conceivable that hybridization of the coumarin moiety with other antibacterial pharmacophores may provide opportunities for the development of novel antibiotics. This review outlines the advances in coumarin-containing hybrids with antibacterial potential in the recent 5 years and the structure-activity relationships are also discussed. K E Y W O R D S antibacterial, coumarin, hybrid compounds, structure-activity relationships

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Novel tacrine-coumarin hybrids linked to 1,2,3-triazole as anti-Alzheimer’s compounds: In vitro and in vivo biological evaluation and docking study

Cited by 109 publications

References 41 publications

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

(E)-N′-(1-(7-Hydroxy-2-Oxo-2H-Chromen-3-Yl) Ethylidene) Benzohydrazide, a Novel Synthesized Coumarin, Ameliorates Isoproterenol-Induced Myocardial Infarction in Rats through Attenuating Oxidative Stress, Inflammation, and Apoptosis

Coumarin‐containing hybrids and their antibacterial activities

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