| Literature DB >> 26162519 |
Fazal Rahim1, Hayat Ullah2, Muhammad Tariq Javid2, Abdul Wadood3, Muhammad Taha4, Muhammad Ashraf5, Ayesha Shaukat5, Muhammad Junaid3, Shafqat Hussain6, Wajid Rehman2, Rashad Mehmood7, Muhammad Sajid8, Muhammad Naseem Khan2, Khalid Mohammed Khan6.
Abstract
A series of thiazole derivatives 1-21 were prepared, characterized by EI-MS and (1)H NMR and evaluated for α-glucosidase inhibitory potential. All twenty one derivatives showed good α-glucosidase inhibitory activity with IC50 value ranging between 18.23±0.03 and 424.41±0.94μM when compared with the standard acarbose (IC50, 38.25±0.12μM). Compound (8) (IC50, 18.23±0.03μM) and compound (7) (IC50=36.75±0.05μM) exhibited outstanding inhibitory potential much better than the standard acarbose (IC50, 38.25±0.12μM). All other analogs also showed good to moderate enzyme inhibition. Molecular docking studies were carried out in order to find the binding affinity of thiazole derivatives with enzyme. Studies showed these thiazole analogs as a new class of α-glucosidase inhibitors.Entities:
Keywords: Molecular docking; Synthesis; Thiazole; α-Glucosidase inhibition
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Year: 2015 PMID: 26162519 DOI: 10.1016/j.bioorg.2015.06.006
Source DB: PubMed Journal: Bioorg Chem ISSN: 0045-2068 Impact factor: 5.275