Abstract
DPP-4Is are well recognized therapy for type 2 diabetes. In spite of sharing a common mode of action, the chemical diversity among members of DPP‐4Is raised the question whether structural differences may result in distinguished activities. DPP-4Is were recently explored as drug repurposing means for treatment of SARS-CoV-2 due to the urgent need for small molecule drugs for controlling infections. The use of DPP-4Is was not correlated with adverse COVID-19-related consequences among patients with type 2 diabetes. Inspired by these reasons and the importance of pyrimidinone ring as DPP-4I with both antioxidant and anti-inflammatory activities, we succeeded to prepare some novel pyrimidinone and thio-pyrimidinone derivatives, which were then screened for their antidiabetic activity and DPP-4 inhibition. In addition, their anti‐inflammatory effect on LPS-stimulated RAW 264.7 cells were evaluated. Furthermore, their antioxidant activities were also tested.
【저자키워드】 IL-6, molecular docking, CRP, OGT, Pyrimidinones, Co-receptor, DPPH, 【초록키워드】 Treatment, SARS-CoV-2, therapy, Anti-inflammatory, antioxidant, type 2 diabetes, activity, infections, Patient, activities, derivatives, Cell, consequence, tested, addition, evaluated, raised, screened, question, not correlated, small molecule drug, 【제목키워드】 COVID-19, novel, Effect, type 2 diabete,