1005324-89-9Relevant academic research and scientific papers
Design, synthesis and biological activities of dihydroaurones
VENKATESWARLU, SOMEPALLI,MURTY, GANDROTU NARASIMHA,SATYANARAYANA, MEKA,SIDDAIAH, VIDAVALUR
, p. 1396 - 1402 (2021/06/09)
To widen aurones applicability in achromatic food and cosmetic applications, a series of dihydroaurones were designed to mimic natural aurones as well as synthetic aurones. Dihydroaurones have been synthesized from the corresponding aurones by hydrogenation. These dihydroaurones and their corresponding aurones were screened for antioxidant, anti-inflammatory and tyrosinase enzyme inhibitory activity. Synthesized dihydroaurones (3b-f) displayed superior antioxidant activity in superoxide free radical scavenging assay than the standard gallic acid. Dihydroaurones (3b-f) also exhibited significant tyrosinase enzyme inhibitory activity and two dihydroaurones (3h, 3j) showed promising 5-lipoxygenase inhibitory activity.
Synthesis of 6-hydroxyaurone analogues and evaluation of their α-glucosidase inhibitory and glucose consumption-promoting activity: Development of highly active 5,6-disubstituted derivatives
Sun, Hua,Ding, Weina,Song, Xiaotong,Wang, Dong,Chen, Mingzhu,Wang, Kaili,Zhang, Yazhou,Yuan, Peng,Ma, Ying,Wang, Runling,Dodd, Robert H.,Zhang, Yongmin,Lu, Kui,Yu, Peng
, p. 3226 - 3230 (2017/07/07)
A series of 6-hydroxyaurones and their analogues have been synthesized and evaluated for their in vitro α-glucosidase inhibitory and glucose consumption-promoting activity. These compounds exhibited varying degrees of α-glucosidase inhibitory activity, 11 of them showing higher potency than that of the control standard acarbose (IC50?=?50.30?μM). Surprisingly, analogues devoid of a substituent at C-2 but having an aryl group at C-5 were found to be highly active (e.g., 7f, IC50?=?9.88?μM). Docking analysis substantiated these findings. The kinetic analysis of compound 7f, the most potent α-glucosidase inhibitor of this study, revealed that it inhibited α-glucosidase in an irreversible and mixed competitive mode. In addition, compounds 7f and 10c exhibited significant glucose consumption promoting activity at 1?μM.
