Synthesis of benzothiadiazine derivatives exhibiting dual activity as aldose reductase inhibitors and antioxidant agents. Issue 12 (15th June 2016)

• Record Type: Journal Article
• Authors: Zhu, Shaojuan; Hao, Xin; Zhang, Shuzhen; Qin, Xiangyu; Chen, Xin; Zhu, Changjin
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 26:Issue 12(2016)
• Page Start: 2880
• Page End: 2885
• Publication Date: 2016-06-15
• Subjects: Aldose reductase -- Benzothiadiazine derivatives -- Antioxidant activity; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2016.04.047
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Several multifunctional benzothiadiazine derivatives were synthesized and examined for their inhibition to the enzyme aldose reductase and in vitro antioxidant activity to identify novel drugs for diabetes and its complications. Most of them exhibited good inhibitory activity. Importantly, a number of compounds demonstrated strong antioxidant activity and one compound in particular was extremely active in the DPPH radical scavenging and MDA inhibition analysis. The DPPH radical scavenging rate with this compound was 98.0%, 92.3% and 42.1% at concentrations of 100 μM, 10 μM, and 1 μM, respectively, and the initial reaction rate was faster than Trolox at a concentration of 10 μM.