| Literature DB >> 31911306 |
Muhammad Taha1, Fazal Rahim2, Khalid Zaman2, Manikandan Selvaraj3, Nizam Uddin4, Rai Khalid Farooq5, Muhammad Nawaz6, Muhammad Sajid7, Faisal Nawaz8, Mohamad Ibrahim9, Khalid Mohammed Khan10.
Abstract
A series of twenty-six analogs of benzimidazole based oxadiazole have been synthesized and evaluated against alpha-glycosidase enzyme. Most the analogs showed excellent to good inhibitory potential. Among the screened analogs, analog 1, 2, 3 and 14 with IC50 values 4.6 ± 0.1, 9.50 ± 0.3, 2.6 ± 0.1 and 9.30 ± 0.4 µM respectively showedexcellent inhibitory potential than reference drug acarbose (IC50 = 38.45 ± 0.80 µM). Some of the analogs like 19, 21, 22 and 23 with methyl and methoxy substituent on phenyl ring show hydrophobic interaction and were found with no inhibitory potential. The binding interactions between synthesized analogs and ligands protein were confirmed through molecular docking study. Various spectroscopic techniques like 1H NMR, 13C NMR, and EI-MS were used for characterization of all synthesized analogs. These derivatives were synthesized by simple mode of synthesis like heterocyclic ring formation.Entities:
Keywords: Benzimidazole; Molecular docking; Oxadiazole; Synthesis; α-glycosidase inhibition
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Year: 2019 PMID: 31911306 DOI: 10.1016/j.bioorg.2019.103555
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275