| Literature DB >> 31699396 |
Fazal Rahim1, Khalid Zaman2, Muhammad Taha3, Hayat Ullah2, Mehreen Ghufran4, Abdul Wadood4, Wajid Rehman2, Nizam Uddin5, Syed Adnan Ali Shah6, Muhammad Sajid7, Faisal Nawaz8, Khalid Mohammed Khan9.
Abstract
Voglibose and acarbose are distinguished α-glucosidase inhibitors used for controlling of diabetes mellitus. Unfortunately, these distinguished and clinically used inhibitors have also numerous side effects. Subsequently, there is still needed to develop safer therapy. Despite of a broad spectrum of biological importance of benzimidazole, it is occasionally evaluated for α-glucosidase activity. Current study deals with the synthesis and biological screening of benzimidazole bearing bis-Schiff bases (1-19) for their α-glucosidase inhibitory activity. All analogues exhibited excellent to good inhibitory potential (IC50 = 2.20 ± 0.1to 88.60 ± 1.70 µM) when compared with standard drug acarbose (IC50 = 38.45 ± 0.80 µM). A structure activity relationship has been established on the basis of electronic effects and position of different substituents present on phenyl ring. In order to rationalize the binding interactions of most active analogues with the active site of α-glucosidase enzyme, molecular docking study was conducted.Entities:
Keywords: Benzimidazole; Bis-Schiff bases; Molecular docking; SAR; Synthesis; α-Glucosidase
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Year: 2019 PMID: 31699396 DOI: 10.1016/j.bioorg.2019.103394
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275