Bioorganic and Medicinal Chemistry Letters p. 3527 - 3530 (2003)
Update date:2022-08-05
Topics: Synthesis Evaluation Isatins Cruzain Falcipain-2 Rhodesain
Chiyanzu, Idan
Hansell, Elizabeth
Gut, Jiri
Rosenthal, Philip J.
McKerrow, James H.
Chibale, Kelly
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 IC50 value of 1 μM against rhodesain. One thiosemicarbazone was found to be active against all three proteases with inhibitory IC50 values of 10 μM 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.
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