Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain |
| |
Authors: | Chiyanzu Idan Hansell Elizabeth Gut Jiri Rosenthal Philip J McKerrow James H Chibale Kelly |
| |
Institution: | Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa. |
| |
Abstract: | While commercial isatins were practically inactive against the target proteases, thiosemicarbazone derivatives were found to be active. The most active compound from the series displayed an inhibitory IC(50) value of 1 microM against rhodesain. One thiosemicarbazone was found to be active against all three proteases with inhibitory IC(50) values of 10 microM or less. A combination of N-benzylation and appropriate substitution on the aromatic portion of the isatin scaffold was generally found to be beneficial especially against cruzain for ketone inhibitors. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |