Antidiabetic and allied biochemical roles of new chromeno-pyrano pyrimidine compounds: synthesis, in vitro and in silico analysis

作者：Hese Shrikant V; Meshram Rohan J; Kamble Rahul D; Mogle Pratima P; Patil Kapil K; Kamble Sonali S; Gacche Rajesh N; Dawane Bhaskar S^*

来源：Medicinal Chemistry Research, 2017, 26(4): 805-818.

DOI：10.1007/s00044-017-1794-0

• Chromeno-pyrano pyrimidine trione derivatives
• Aldose reductase
• Molecular docking
• Antioxidant activity
• Hemolytic activity

Diabetes is embracing the human population in logarithmic fashion both in developed as well as developing countries. Aldose reductase is one of the important enzymes of polyol pathway of sugar metabolism in humans. Aldose reductase inhibition has been identified as one of the important target for developing novel antidiabetic agents. In this report, we present an effective synthesis of 7-(substituted phenyl) chromeno-pyrano [2,3-d]pyrimidine-6,8,10-(7H,9H,11H)-trione derivatives and demonstrate their aldose reductase inhibition potential in order to identify novel schemes for finding putative aldose reductase inhibitors. The antioxidant activity of all the synthesized compounds with negligible toxicity demonstrates the biological efficacy of the synthesized compounds. The in silico molecular docking and structural analysis of docked poses conducted in the current investigation sheds light on the structural rationale of the observed aldose reductase inhibition by all the newly synthesized compounds.

• 出版日期2017-4