Synthesis Of Ethyl 5-Hydroxy-6-Bromo-1H-Indole-3-Carboxylate Derivatives

In this paper, the influenza virus and its biological characteristics were described briefly. We focused largely on the actuality and the development of anti-influenza agents.The antiviral activity of Arbidol, a new antiviral agent, is most pronounced against influenza viruses of the A and B antigenic type. Its effect may be due to the activation of 2,5-oligoadenylate synthetase. Arbidol has been developed and launched for the treatment and prophylaxis of respiratory viral infections.On the basis of our former research work, taking Arbidol as lead compound, ethyl 5-hydroxy-6-bromo-lH-indole-3-carboxylate was chosen as elementary structure. Some modifications were made at 1-position, 2-position, and 4-position on the indole ring by using the principle of drug design of association and modification principles. 30 target compounds were designed and synthesized which had not been reported in literatures. The structures of the 30 target compounds were confirmed by MS and ~1H-NMR.In the course of modification at 2-position of indole ring, the structure of (phenylethylthio)-methyl or (phenylpropylthio)methyl was introduced by using principle of lead optimization to examine the effect on the activity of anti-virus. We expected to make a breakthrough on modification of this position.The antivirus activity evaluation of these target compounds is in process.