"Triazole-linked thiazolidinedione-Benzothiazole hybrids: Design and biological evaluation as AChE inhibitors".

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Tác giả: Amira Abood, Aya M Almatary, Mohammad M Al-Sanea, Abdullah A Elgazar, Abdullah Haikal, Abdelrahman Hamdi, Mahmoud A A Ibrahim, Eman E Nasr, Gary S Thompson

Ngôn ngữ: eng

Ký hiệu phân loại:

Thông tin xuất bản: United States : Bioorganic chemistry , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 717642

Novel 2,4-thiazolidinedione-benzothiazole-triazole hybrids (7a-7l) were designed and synthesized as therapeutic agents with pleotropic activity for Alzheimer's disease (AD). These compounds were evaluated for their acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) inhibitory activities. Compound 7k, exhibited exceptional AChE inhibition (IC₅₀ = 0.083 μM), while compound 7d, showed potent activity (IC₅₀ = 0.119 μM). Kinetic studies revealed that 7k was able to exert its action through mixed types of inhibition. Also, the anti-inflammatory potential of these lead compounds was assessed in LPS-stimulated RAW 264.7 macrophages. Both compounds demonstrated significant dose-dependent inhibition of key inflammatory mediators, including NO, TNF-α, IL-6, and IL-1β at non-cytotoxic concentrations (≤10 μM). Notably, compound 7k exhibited superior anti-inflammatory activity, achieving 92 % NO inhibition, 65 % TNF-α reduction, and 61.1 % IL-1β suppression at 10 μM. Moreover, compound 7k exerted neuroprotective activity against H
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