Microwave-assisted synthesis of novel 5-substituted benzylidene amino-2-butyl benzofuran-3-yl-4-methoxyphenyl methanones as antileishmanial and antioxidant agents

作者：Patil Sanjeev R; Bollikonda Satyanarayana; Patil Rajendra H; Sangshetti Jaiprakash N; Bobade Anil S; Asrondkar Ashish; Reddy Padi Pratap; Shinde Devanand B^*

来源：Bioorganic & Medicinal Chemistry Letters, 2018, 28(3): 482-487.

DOI：10.1016/j.bmcl.2017.12.013

• Benzofuran derivatives
• Antileishmanial activity
• Antioxidant activity
• Docking study
• ADME properties

A series of 5-substituted benzylideneamino-2-butylbenzofuran-3-yl-4-methoxyphenyl methanones is synthesized and evaluated for antileishmanial and antioxidant activities. Compounds 4f (IC50 = 52.0 +/- 0.09 mu g/ml), 4h (IC50 = 56.0 +/- 0.71 mu g/ml) and 4l (IC50 = 59.3 +/- 0.55 mu g/ml) were shown significant antileishmanial when compared with standard sodium stibogluconate (IC50 = 490.0 +/- 1.5 mu g/ml). Antioxidant study revealed that compounds 4i (IC50 = 2.44 +/- 0.47 mu g/ml) and 4l (IC50 = 3.69 +/- 0.44 mu g/ml) have shown potent comparable activity when compared with standard ascorbic acid (IC50 = 3.31 +/- 0.34 mu g/ml). Molecular docking study was carried out which replicating results of biological activity in case of initial hits 4f and 4h suggesting that these compounds have a potential to become lead molecules in drug discovery process. In silico ADME study was performed for predicting pharmacokinetic profile of the synthesised antileishmanial agents and expressed good oral drug like behaviour.

• 出版日期2018-2-1