Bis(12)-Hupyridone, a Promising Multi-Functional Anti-Alzheimer’s Dimer Derived from Chinese Medicine

Han, Yifan; Cui, Wei; Choi, Tony Chunglit; Mak, Shinghung; Yu, Hua; Hu, Songhua; Li, Wenming; Zuo, Zhong

doi:10.5772/35663

Cited by 1 publication

(1 citation statement)

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“…Several studies have recently been conducted on the development of bivalent AChE inhibitors as potential therapeutic agents for Alzheimer's disease (AD). [40][41][42][43][44][45][46][47][48] Recently, our research team demonstrated the highly effective inhibition of carbonic anhydrase by a group of aromatic bis-ureido-substituted benzenesulfonamide derivatives. [49] These compounds exhibited remarkable potency in inhibiting human carbonic anhydrase IX and XII (hCA IX and XII), which are membrane-bound isozymes of the carbonic anhydrase enzyme overexpressed in tumors.…”

Section: Introductionmentioning

confidence: 99%

Bis‐Ureido‐Substituted Benzenesulfonamides: Evaluation of Their Antibacterial, Anticholinesterase, and Cytotoxicity Properties

Tekeli,

Lolak,

Tekeli

et al. 2024

ChemistrySelect

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In this study, we present the re‐synthesis of a series of twelve bis‐ureido‐substituted benzenesulfonamides, focusing on their potential as antibacterial, anticholinesterase, and cytotoxic agents. First, the antibacterial assessment of these compounds indicated varying activity levels across different bacterial strains, with S. aureus displaying resistance to all compounds, while compounds 9 and 11 exhibited promise against E. faecalis with a MIC value of 31.25 μg/mL. Additionally, P. aeruginosa showed resistance to compounds containing 4‐aminobenzene sulfonamides, whereas derivatives such as (8–11) and compound 19 displayed notable activity against E. coli, comparable to Ampicillin. Second, their anticholinesterase activities were examined, with a focus on their potential role in addressing neurological disorders, particularly Alzheimer′s disease. The findings indicated that all synthesized compounds showed a significant inhibitory effect on both AChE and BChE enzymes. Compound 11 demonstrated the most effective inhibition on the AChE enzyme with an IC50 value of 0.2160±0.09 nM, while compound 18 exhibited the most potent inhibition on the BChE enzyme with an IC50 value of 0.2257±0.06 nM. Finally, cytotoxicity studies were conducted across various cell lines, including breast, lung, and prostate cancer cells and normal cells. The results revealed that compound 12 emerged as the most potent tested compound against breast cancer cells with no cytotoxic effect on CRL‐4010 normal breast epithelial cells. The research presented here not only highlights the multifaceted pharmacological potential of bis‐ureido‐substituted benzenesulfonamides, but also indicates their potential as versatile compounds for antibacterial, anticholinesterase, and cytotoxicity applications, opening up new avenues for drug discovery and development.

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