Thiazole based carbohydrazide derivatives as α-amylase inhibitor and their molecular docking study

• Published in: Heteroatom Chemistry
• Main Author: Taha M.; Irshad M.; Imran S.; Rahim F.; Selvaraj M.; Almandil N.B.; Mosaddik A.; Chigurupati S.; Nawaz F.; Ismail N.H.; Ibrahim M.
• Format: Article
• Language: English
• Published: Hindawi Limited 2019
• Online Access: https://www.scopus.com/inward/record.uri?eid=2-s2.0-85064346121&doi=10.1155%2f2019%2f7502347&partnerID=40&md5=855bb7ee90c8d6dee00ba27ded350a1d
• ISSN: 10427163
• DOI: 10.1155/2019/7502347

In this study we are going to present thiazole based carbohydrazide in search of potent antidiabetic agent as α-amylase inhibitors. Thiazole based carbohydrazide derivatives 1-25 have been synthesized, characterized by 1 HNMR, 13 CNMR, and EI-MS, and evaluated for α-amylase inhibition. Except compound 11 all analogs showed α-amylase inhibitory activity with IC 50 values from 1.709 ± 0.12 to 3.049 ± 0.25 μM against the standard acarbose (IC 50 = 1.637 ± 0.153 μM). Compounds 1, 10, 14, and 20 exhibited outstanding inhibitory potential with IC 50 value 1.763 ± 0.03, 1.747 ± 0.20, 1.709 ± 0.12, and 1.948 ± 0.23 μM, respectively, compared with the standard acarbose. Structure activity relationships have been established for the active compounds. To get an idea about the binding interaction of the compounds, molecular docking studies were done. © 2019 Muhammad Taha et al.