Synthetic benzofuran-linked chalcones with dual actions: a potential therapeutic approach to manage diabetes mellitus.

Abstract

Background: Identification of molecules having dual capabilities to reduce postprandial hyperglycemia and oxidative stress is one of the therapeutic approaches to treat diabetes mellitus. In this connection, a library of benzofuran-linked chalcone derivatives were evaluated for their dual action. Methods: A series of substituted benzofuran-linked chalcones (2-33) were synthesized and tested for α-amylase inhibitory as well as 2,2-diphenylpicrylhydrazyl (DPPH) and 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging activities. Results: All compounds showed α-amylase inhibitory activity ranging from IC50 = 12.81 ± 0.03 to 87.17 ± 0.15 μM, compared with the standard acarbose (IC50 = 13.98 ± 0.03 μM). Compounds also demonstrated radical scavenging potential against DPPH and ABTS radicals. Conclusion: The identified compounds may serve as potential leads for further advanced research.

• Authors: Irfan Ali, Rafaila Rafique, Khalid Mohammed Khan, Sridevi Chigurupati, Xingyue Ji, Abdul Wadood, Uzma Salar, Suliman A Almahmoud, Ashfaq Ur Rehman, Shatha Ghazi Felemban, Shehryar Hameed, Shahnaz Perveen
• Journal: Future medicinal chemistry (Future Med Chem) Vol. 15 Issue 2 Pg. 167-187 (01 2023) ISSN: 1756-8927 [Electronic] England
• PMID: 36799245 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• 2,2'-azino-di-(3-ethylbenzothiazoline)-6-sulfonic acid
• Chalcones
• alpha-Amylases
• Benzofurans

Topics

• Humans
• Chalcones (pharmacology, therapeutic use, chemistry)
• Diabetes Mellitus (drug therapy)
• alpha-Amylases
• Benzofurans (pharmacology, therapeutic use)