当前位置: X-MOL 学术BMC Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis, anti-leishmanial and molecular docking study of bis-indole derivatives
BMC Chemistry ( IF 4.3 ) Pub Date : 2019-08-06 , DOI: 10.1186/s13065-019-0617-4
Muhammad Taha , Imad Uddin , Mohammed Gollapalli , Noor Barak Almandil , Fazal Rahim , Rai Khalid Farooq , Muhammad Nawaz , Mohamed Ibrahim , Mohammed A. Alqahtani , Yasser A. Bamarouf , Manikandan Selvaraj

We have synthesized new series of bisindole analogs (1–27), characterized by 1HNMR and HR-EI-MS and evaluated for their anti-leishmanial potential. All compounds showed outstanding inhibitory potential with IC50 values ranging from 0.7 ± 0.01 to 13.30 ± 0.50 µM respectively when compared with standard pentamidine with IC50 value of 7.20 ± 0.20 µM. All analogs showed greater potential than standard except 10, 19 and 23 when compared with standard. Structure activity relationship has been also established for all compounds. Molecular docking studies were carried out to understand the binding interaction of active molecules.

中文翻译:

双吲哚衍生物的合成,抗利什曼肽和分子对接研究

我们合成了一系列新的双吲哚类似物(1–27),其特征在于1HNMR和HR-EI-MS并评估了其抗利什曼肽的潜力。与标准戊tam胺(IC50值为7.20±0.20 µM)相比,所有化合物均显示出出色的抑制潜能,IC50值分别为0.7±0.01至13.30±0.50 µM。与标准品相比,所有类似物均显示出比标准品更大的潜力,除了10、19和23。还已经为所有化合物建立了结构活性关系。进行了分子对接研究以了解活性分子的结合相互作用。
更新日期:2019-08-06
down
wechat
bug