Potential of aryl–urea–benzofuranylthiazoles hybrids as multitasking agents in Alzheimer's disease

Kurt, Belma Zengin; Gazioğlu, Işıl; Basile, Livia; Sönmez, Fatih; Ginex, Tiziana; Küçükislamoğlu, Mustafa; Guccione, Salvatore

doi:10.1016/j.ejmech.2015.07.005

Cited by 38 publications

(29 citation statements)

References 47 publications

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“…In 2015, Basile, Sonmez, and co‐workers synthesized a series of 38 aryl–urea–benzofuranylthiazole derivatives (Figure ) as multifunctional agents for AD . In this work, the authors evaluate the synthesized compounds for AChE and BuChE inhibition; in addition, their cupric reducing antioxidant capacities (CUPRACs) and 2,2′‐azido‐bis(3‐ethylbenzothiazoline‐6‐sulfonic acid) (ABTS) cation radical scavenging activity are tested.…”

Section: Discussionmentioning

confidence: 99%

Benzofuran and Indole: Promising Scaffolds for Drug Development in Alzheimer's Disease

2018

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Alzheimer's disease (AD) is a progressive neurodegenerative disease with no clinically accepted treatment to cure or halt its progression. The Food and Drug Administration has approved drugs (e.g., rivastigmine, donepezil, galantamine, and memantine) that at best provide marginal benefits, thus emphasizing the urgent need to explore other molecular entities as future drug candidates for AD. Looking at the wide pharmaceutical applications of heterocyclic compounds and particularly those containing benzofuran and indole ring systems, these molecular frameworks have drawn special attention from medicinal chemists for further evaluation in numerous diseases. This article focuses on the history and recent advances of benzofuran- and indole-based compounds as inhibitors of butyrylcholinesterase, acetylcholinesterase, γ-secretase, β-secretase, tau misfolding, and β-amyloid aggregation.

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Section: Discussionmentioning

confidence: 99%

Benzofuran and Indole: Promising Scaffolds for Drug Development in Alzheimer's Disease

2018

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“…Among the aforementioned scaffolds, coumarin and thiazole have gained much attention in recent decades in the field of medicinal chemistry as leading pharmacophores with a wide range of pharmacological activities. Some of the biological properties include antioxidant, anticholinesterase activity (AChE and BuChE), carbonic anhydrase I, II, and IX inhibiting activities and aflatoxigenic activity …”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis, In Vitro Evaluation and Docking Studies of Pyrazole‐Thiazole Hybrids as Antimicrobial and Antibiofilm Agents

et al. 2018

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In the present study, a series of novel pyrazole‐thiazole hybrids (4a‐l) were designed, synthesized and assessed for their in vitro antimicrobial activity against both Gram‐positive and Gram‐negative pathogenic bacterial and fungal strains. Compounds derived from p‐CH3 phenyl (4b), p‐Br phenyl (4g), 8‐bromocoumarinyl (4k), and 6,8‐dibromocoumarinyl (4l) exhibited promising inhibitory activity against the tested bacterial strains with minimum inhibitory concentration (MIC)/minimum bactericidal concentration (MBC) spectrum of 1.9/7.8 μg/mL to 3.9/7.8 μg/mL. The compounds with p‐CH3 phenyl (4b), p‐OCH3 phenyl (4c), benzo[f]coumarinyl (4j), 8‐bromocoumarinyl (4k) substitutions showed their inhibitory potency against various Candida strains with MIC/minimum fungicidal concentration (MFC) values of 3.9/7.8 μg/mL. Also, anti‐biofilm and toxicity profile of the compounds was also tested. The biofilm inhibition results revealed that the compound 4 j exhibited promising activity with an IC50 value of 11.8 μM against S. aureus MTCC 96, while 4 k showed significant activity against S. aureus MLS16 MTCC 2940, K. planticola MTCC 530 and C. albicans MTCC 3017 with IC50 values of 12, 14 and 16 μM, respectively. The present study has emphasized that thiazole‐pyrazole hybrids with benzothiazole and coumarin scaffolds can be a novel and potent class of molecules with potential biological activities.

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“…Particular attention has been paid to their action as antioxidants,, and to their efficacy in the treatment of Alzheimer's disease . As oxidative stress is considered a causative factor in neurodegeneration, and in particular the disruptions leading to Alzheimer's disease, considerable attention has been paid to the use of benzofuran derivatives as antioxidant therapeutic agents …”

Section: Introductionmentioning

confidence: 99%

A Green and Versatile Route to Highly Functionalized Benzofuran Derivatives Using Biomimetic Oxygenation

et al. 2018

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One‐pot green reactions useful for the synthesis of novel and potentially biologically active compounds have been developed using metaloporphyrin catalyzed oxidations of benzofurans. Minor variations of the reaction parameters allow direction of the reactivity (furan versus benzene ring) and the production of multifunctional 2,3‐dihydrobenzofurans, salicyl derivatives or an unusual dimerization product. These studies suggest pathways for the metabolic oxidation and activation of pharmaceuticals and other molecules containing the benzofuran core.

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Potential of aryl–urea–benzofuranylthiazoles hybrids as multitasking agents in Alzheimer's disease

Cited by 38 publications

References 47 publications

Benzofuran and Indole: Promising Scaffolds for Drug Development in Alzheimer's Disease

Benzofuran and Indole: Promising Scaffolds for Drug Development in Alzheimer's Disease

Design, Synthesis, In Vitro Evaluation and Docking Studies of Pyrazole‐Thiazole Hybrids as Antimicrobial and Antibiofilm Agents

A Green and Versatile Route to Highly Functionalized Benzofuran Derivatives Using Biomimetic Oxygenation

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