324545-66-6Relevant academic research and scientific papers
Synthesis and characterisation of thiobarbituric acid enamine derivatives, and evaluation of their α-glucosidase inhibitory and anti-glycation activity
Al-Majid, Abdullah Mohammed,Al-Rasheed, Hessa H.,Albericio, Fernando,Ali, M.,Barakat, Assem,Choudhary, M. Iqbal,Dahlous, Kholoud,El-Faham, Ayman,Sanam, Mehar,Sharma, Anamika,Ul-Haq, Zaheer,Yousuf, Sammer,de la Torre, Beatriz G.
, p. 692 - 701 (2020)
A new series of thiobarbituric (thiopyrimidine trione) enamine derivatives and its analogues barbituric acid derivatives was synthesised, characterised, and screen for in vitro evaluation of α-glucosidase enzyme inhibition and anti-glycation activity. This series of compounds were found to inhibit α-glucosidase activity in a reversible mixed-type manner with IC50 between 264.07 ± 1.87 and 448.63 ± 2.46 μM. Molecular docking studies indicated that compounds of 3g, 3i, 3j, and 5 are located close to the active site of α-glucosidase, which may cover the active pocket, thereby inhibiting the binding of the substrate to the enzyme. Thiopyrimidine trione derivatives also inhibited the generation of advanced glycation end-products (AGEs), which cause long-term complications in diabetes. While, compounds 3a–k, 5, and 6 showed significant to moderate anti-glycation activity (IC50 = 31.5 ± 0.81 to 554.76 ± 9.1 μM).
