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ID: ALA1145878
Journal: Bioorg Med Chem Lett
Title: Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain.
Authors: Chiyanzu I, Hansell E, Gut J, Rosenthal PJ, McKerrow JH, Chibale K.
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.
CiteXplore: 14505663