Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase
2015; Elsevier BV; Volume: 62; Linguagem: Inglês
10.1016/j.bioorg.2015.06.006
ISSN1090-2120
AutoresFazal Rahim, Hayat Ullah, Muhammad Tariq Javid, Abdul Wadood, Muhammad Taha, Muhammad Ashraf, Ayesha Shaukat, Muhammad Junaid, Shafqat Hussain, Wajid Rehman, Rashad Mehmood, Muhammad Sajid, Muhammad Naseem Khan, Khalid Mohammed Khan,
Tópico(s)Psidium guajava Extracts and Applications
ResumoA 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.
Referência(s)