作者
Kishan B Patel, Dushyant V Patel, Nirav R Patel, Ashish M Kanhed, Divya M Teli, Bhumi Gandhi, Bhavik S Shah, Bharat N Chaudhary, Navnit K Prajapati, Kirti V Patel, Mange Ram Yadav
发表日期
2022/11/29
期刊
Journal of Biomolecular Structure and Dynamics
卷号
40
期号
20
页码范围
10278-10299
出版商
Taylor & Francis
简介
With the aim to combat a multi-faceted neurodegenerative Alzheimer’s disease (AD), a series of carbazole-based semicarbazide and hydrazide derivatives were designed, synthesized and assessed for their cholinesterase (ChE) inhibitory, antioxidant and biometal chelating activity. Among them, (E)-2-((9-ethyl-9H-carbazol-3-yl)methylene)-N-(pyridin-2-yl)hydrazinecarbothioamide (62) and (E)-2-((9-ethyl-9H-carbazol-3-yl)methylene)-N-(5-chloropyridin-2-yl)hydrazinecarbothioamide (63) emerged as the premier candidates with good ChE inhibitory activities (IC50 values of 1.37 µM and 1.18 µM for hAChE, IC50 values of 2.69 µM and 3.31 µM for EqBuChE, respectively). All the test compounds displayed excellent antioxidant activity (reduction percentage of DPPH values for compounds (62) and (63) were 85.67% and 84.49%, respectively at 100 µM concentration). Compounds (62) and (63) conferred specific …
引用总数
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