作者
Dushyant V Patel, Nirav R Patel, Ashish M Kanhed, Divya M Teli, Kishan B Patel, Prashant D Joshi, Sagar P Patel, Pallav M Gandhi, Bharat N Chaudhary, Navnit K Prajapati, Kirti V Patel, Mange Ram Yadav
发表日期
2020/8/1
期刊
Bioorganic Chemistry
卷号
101
页码范围
103977
出版商
Academic Press
简介
Molecules capable of engaging with multiple targets associated with pathological condition of Alzheimer's disease have proved to be potential anti-Alzheimer's agents. In our goal to develop multitarget-directed ligands for the treatment of Alzheimer’s disease, a novel series of carbazole-based stilbene derivatives were designed by the fusion of carbazole ring with stilbene scaffold. The designed compounds were synthesized and evaluated for their anti-AD activities including cholinesterase inhibition, Aβ aggregation inhibition, antioxidant and metal chelation properties. Amongst them, (E)-1-(4-(2-(9-ethyl-9H-carbazol-3-yl)vinyl)phenyl)-3-(2-(pyrrolidin-1-yl)ethyl)thiourea (50) appeared to be the best candidate with good inhibitory activities against AChE (IC50 value of 2.64 μM) and BuChE (IC50 value of 1.29 μM), and significant inhibition of self-mediated Aβ1–42 aggregation (51.29% at 25 μM concentration). The …
引用总数
20202021202220232024110991
学术搜索中的文章
DV Patel, NR Patel, AM Kanhed, DM Teli, KB Patel… - Bioorganic Chemistry, 2020