Biological evaluation and molecular docking of novel 1,3,4-thiadiazole-resorcinol conjugates as multifunctional cholinesterases inhibitors

Skrzypek, Alicja; Matysiak, Joanna; Karpińska, Monika; Czarnecka, Kamila; Kręcisz, Paweł; Stary, Dorota; Kukułowicz, Jędrzej; Paw, Beata; Bajda, Marek; Szymański, Paweł; Niewiadomy, Andrzej

doi:10.1016/j.bioorg.2020.104617

Cited by 30 publications

(20 citation statements)

References 42 publications

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“…For instance, a series of resorcynyl-substituted 1,3,4-thiadiazoles have been reported as effective antifungal agents [ 11 ] and some of these compounds demonstrated the ability to enhance the anti- Candida activity of the polyene-based drug amphotericin B [ 12 ]. Moreover, some of these 1,3,4-thiadiazole derivatives exhibited notable antitumor activity [ 13 ], while other analogs from this group demonstrated significant antineurodegenerative potency [ 14 , 15 ].…”

Section: Introductionmentioning

confidence: 99%

Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors

Karcz

Starzak

Ciszkowicz

et al. 2021

IJMS

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A series of coumarin-thiadiazole hybrids and their corresponding Cu(II) and Zn(II) complexes were synthesized and characterized with the use of spectroscopic techniques. The results obtained indicate that all the coumarin-thiadiazole hybrids act as bidentate chelators of Cu(II) and Zn(II) ions. The complexes isolated differ in their ligand:metal ratio depending on the central metal. In most cases, the Zn(II) complexes are characteristic of a 1:1 ligand:metal ratio, while in the Cu(II) complexes the ligand:metal ratio is 2:1. All compounds were tested as potential antibacterial agents against Gram-positive (Staphylococcus aureus, Staphylococcus epidermidis) and Gram-negative (Escherichia coli, Pseudomonas aeruginosa) bacterial strains demonstrating activities notably lower than commercially available antibiotics. The more promising results were obtained from the assessment of antineurodegenerative potency as all compounds showed moderate acetylcholinesterase (AChE) inhibition activity

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Section: Introductionmentioning

confidence: 99%

Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors

Karcz

Starzak

Ciszkowicz

et al. 2021

IJMS

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“…Its active compound, curcumin, has long been identified as a strong antioxidant, anti-inflammatory, and antitumor agent. [37] Recently, curcumin has become a rising star in the field of AD treatment for its antiamyloid properties. [38] In several studies, curcumin has shown the effect of inhibiting A β production and aggregation while increasing Aβ clearance.…”

Section: Turmericmentioning

confidence: 99%

Treatment for alzheimer's disease: The present and future

Wei

2021

E3S Web Conf.

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Alzheimer's disease (AD) is a growing global health crisis, however, there are currently very few effective treatments for it. All existent treatments serve only to ameliorate the symptoms of AD instead of curing it. With the deepening of the disease pathology in recent years, there have been many studies and clinical trials that aim to discover new disease-modifying therapies. Nanoparticle drug delivery platform is a promising path for its high penetration rate across the blood brain barrier, while heat shock proteins provide a new strategy to target the mutant proteins that cause AD. These novel therapies may help us better treat and potentially cure AD, but many of them are still in their early stage of development and their side effects are still unknown. A truly effective treatment for AD is still years ahead.

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“…The molecular structure of a compound is responsible for various pharmacological activities, and mostly heterocyclic moieties have diverse activities. This scaffold (Figure 1A) derivatives possess a wide range of biological activities such as anticancer/antitumor (Janowska et al, 2020;Cevik et al, 2020;Gomha et al, 2017;Flefel et al, 2017;Ningegowda et al, 2017), anticonvulsant (Khatoon et al, 2018;Bhandari et al, 2008;Jatav et al, 2008;Foromadi et al, 2007;Almasirad et al, 2007;Dawood et al, 2006;Dogan et al, 2002;Varvaresou et al, 1998;Khazi et al, 1996;Stillings et al, 1986;Chapleo et al, 1986), antidiabetic (Vaishnav et al, 2017;Datar and Deokule, 2014;Thrilochana et al, 2014), anti-inflammatory (Cristina et al, 2018;Schenone et al, 2006), antidepressant (Can et al, 2012), antihypertensive (Samel and Pai, 2010), antiviral (Serban et al, 2020;Brai et al, 2019), antimicrobial (Gowda et al, 2020;Merugu et al, 2020;Mutchu et al, 2019;Sekhar et al, 2018;Joseph et al, 2015), antioxidant (Yakan, 2021;Gowda et al, 2020), anti-leishmanial (Tahghighi and Babalouei, 2017;Sadat-Ebrahimi et al, 2019), and neuroprotective (Skrzypeka et al, 2021). The biological activities of several synthesized derivatives of 1,3,4-thiadiazole are based on assumptions like "the N-C-Smoiety's presence and strong aromaticity of the ring, which is responsible for providing low toxicity and great in vivo st...…”

Section: Introductionmentioning

confidence: 99%

1,3,4-Thiadiazole Scaffold: As Anti-Epileptic Agents

Anthwal

Nain

2022

Front. Chem.

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A wide range of biological activities is exhibited by 1,3,4-thiadiazole moiety such as antidiabetic, anticancer, anti-inflammatory, anticonvulsant, antiviral, antihypertensive, and antimicrobial. To date, drugs such as butazolamide, and acetazolamide. Several modifications have been done in the 1,3,4-thiadiazole moiety which showed good potency as anticonvulsant agents which are highly effective and have less toxicity. After in-depth literature survey in this review, we have compiled various derivatives of 1,3,4-thiadiazole scaffold as anticonvulsant agents.

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Biological evaluation and molecular docking of novel 1,3,4-thiadiazole-resorcinol conjugates as multifunctional cholinesterases inhibitors

Cited by 30 publications

References 42 publications

Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors

Novel Coumarin-Thiadiazole Hybrids and Their Cu(II) and Zn(II) Complexes as Potential Antimicrobial Agents and Acetylcholinesterase Inhibitors

Treatment for alzheimer's disease: The present and future

1,3,4-Thiadiazole Scaffold: As Anti-Epileptic Agents

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