115046-41-8Relevant academic research and scientific papers
Synthesis and evaluation of isatins and thiosemicarbazone derivatives against cruzain, falcipain-2 and rhodesain
Chiyanzu, Idan,Hansell, Elizabeth,Gut, Jiri,Rosenthal, Philip J.,McKerrow, James H.,Chibale, Kelly
, p. 3527 - 3530 (2007/10/03)
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.
Metal Template Reactions. XXV. N-Acyl Isatin Precursors for the Synthesis of Malonamido Macrocyclic Metal Complexes
Black, David St.C.,Chaichit, Narongsak,Gatehouse, Bryan M.,Moss, G. Ian
, p. 1745 - 1754 (2007/10/02)
Reaction of sodium isatide with dimethylmalonyl dichloride yielded the oxazinoindole (6) rather than the expected product (4).The glyoxylamide (8), which served as a precursor to the macrocyclic complex (15), was therefore prepared by a sequence involving
