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Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain

✍ Scribed by Idan Chiyanzu; Elizabeth Hansell; Jiri Gut; Philip J. Rosenthal; James H. McKerrow; Kelly Chibale

Publisher: Elsevier Science
Year: 2003
Tongue: English
Weight: 156 KB
Volume: 13
Category: Article
ISSN: 0960-894X
DOI: 10.1016/s0960-894x(03)00756-x

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✦ Synopsis

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 mM against rhodesain. One thiosemicarbazone was found to be active against all three proteases with inhibitory IC 50 values of 10 mM 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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