Research Letter: New Potent Indole Derivatives as Hyaluronidase Inhibitors

摘要: Because of the physiologic importance hyaluronidases, identification potent and selective inhibitors hyaluronidases has become increasingly important. A variety assay methods have been used for such a purpose, i.e. classical turbidimetric, viscometric colorimetric. In this study, modified enzymatic to obtain microtiter plate-based sensitive activity screening. All were tested in stains-all at pH 7 Morgan-Elson 3.5. Among compounds, 1, 2, 3, 6, 7, 8, 16, 17 18 showed good inhibition more than 50%, so IC(50) values these derivatives determined range 25-41 microm. The value most active hyaluronidase inhibitor Vcpal (6-palmitoyl-L-ascorbic acid) was measured as 8.36 including twofold less 3.5 assay. Examination substituent effects on that para-positions benzamide needs be chlorinated or fluorinated inhibitory effect. It found introduction p-fluoro benzyl ring indole nitrogen positive effect both indole-2- 3-carboxamide derivatives.