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

被引：2

作者：

Ali, Irfan ^{[1
]}

Rafique, Rafaila ^{[1
]}

Khan, Khalid Mohammed ^{[1
,2
]}

Chigurupati, Sridevi ^{[3
]}

Ji, Xingyue ^{[4
]}

Wadood, Abdul ^{[5
]}

Salar, Uzma ^{[6
]}

Almahmoud, Suliman A. ^{[3
]}

Rehman, Ashfaq Ur ^{[5
]}

Felemban, Shatha Ghazi ^{[7
]}

Hameed, Shehryar ^{[1
]}

Perveen, Shahnaz ^{[8
]}

机构：

[1] Univ Karachi, HEJ Res Inst Chem, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan

[2] Imam Abdulrahman Bin Faisal Univ, Inst Res & Med Consultat IRMC, Dept Clin Pharm, Dammam 31441, Saudi Arabia

[3] Qassim Univ, Coll Pharm, Dept Med Chem & Pharmacognosy, Buraydah 51431, Saudi Arabia

[4] Soochow Univ, Coll Pharmaceut Sci, Dept Med Chem, Suzhou 215006, Peoples R China

[5] Abdul Wali Khan Univ, Dept Biochem, Shankar Campus, Mardan 102345, Khyber Pakhtunk, Pakistan

[6] Univ Karachi, Dr Panjwani Ctr Mol Med & Drug Res, Int Ctr Chem & Biol Sci, Karachi 75270, Pakistan

[7] Fakeeh Coll Med Sci, Dept Med Lab Sci, Jeddah 21461, Saudi Arabia

[8] PCSIR Labs Complex, Karachi 75280, Pakistan

来源：

FUTURE MEDICINAL CHEMISTRY | 2023年 / 15卷 / 01期

关键词：

benzofuran; chalcone; in silico; in vitro; radical scavenger; synthesis; alpha-amylase; DERIVATIVES; SCAFFOLD;

D O I：

10.4155/fmc-2022-0247

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 alpha-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 alpha-amylase inhibitory activity ranging from IC50 = 12.81 +/- 0.03 to 87.17 +/- 0.15 mu M, compared with the standard acarbose (IC50 = 13.98 +/- 0.03 mu M). Compounds also demonstrated radical scavenging potential against DPPH and ABTS radicals. Conclusion: The identified compounds may serve as potential leads for further advanced research. [GRAPHICS]

引用

页码：167 / 187

页数：21

共 42 条

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