My watch list
my.chemeurope.com  
Login  

Synthesis, α-amylase inhibitory potential and molecular docking study of indole derivatives

Publication date:

October 2018


Source:Bioorganic Chemistry, Volume 80

Author(s): Muhammad Taha, Mohd Syukri Baharudin, Nor Hadiani Ismail, Syahrul Imran, Muhammad Naseem Khan, Fazal Rahim, Manikandan Selvaraj, Sridevi Chigurupati, Muhammad Nawaz, Faiza Qureshi, Shantini Vijayabalan

In search of potent α-amylase inhibitor we have synthesized eighteen indole analogs (1–18), characterized by NMR and HR-EIMS and screened for α-amylase inhibitory activity. All analogs exhibited a variable degree of α-amylase inhibition with IC50 values ranging between 2.031 ± 0.11 and 2.633 ± 0.05 μM when compared with standard acarbose having IC50 values 1.927 ± 0.17 μM. All compounds showed good α-amylase inhibition. Compound 14 was found to be the most potent analog among the series. Structure-activity relationship has been established for all compounds mainly based on bringing about the difference of substituents on phenyl ring. To understand the binding interaction of the most active analogs molecular docking study was performed.
Graphical abstract




Authors:   Author(s): Muhammad Taha, Mohd Syukri Baharudin, Nor Hadiani Ismail, Syahrul Imran, Muhammad Naseem Khan, Fazal Rahim, Manikandan Selvaraj, Sridevi Chigurupati, Muhammad Nawaz, Faiza Qureshi, Shantini Vijayabalan
Journal:   Bioorganic Chemistry
Volume:   80
Year:   2018
Pages:   36
DOI:   10.1016/j.bioorg.2018.05.021
Publication date:   11-Jun-2018
Facts, background information, dossiers
More about Elsevier
Your browser is not current. Microsoft Internet Explorer 6.0 does not support some functions on Chemie.DE