1313592-57-2Relevant academic research and scientific papers
Novel lipophilic acetohydroxamic acid derivatives based on conformationally constrained spiro carbocyclic 2,6-diketopiperazine scaffolds with potent trypanocidal activity
Fytas, Christos,Zoidis, Grigoris,Tzoutzas, Nikolaos,Taylor, Martin C.,Fytas, George,Kelly, John M.
, p. 5250 - 5254 (2011/10/02)
We describe novel acetohydroxamic acid derivatives with potent activity against cultured bloodstream-form Trypanosoma brucei and selectivity indices of >1000. These analogues were derived from conformationally constrained, lipophilic, spiro carbocyclic 2,6-diketopiperazine (2,6-DKP) scaffolds by attaching acetohydroxamic acid moieties to the imidic nitrogen. Optimal activity was achieved by placing benzyl groups adjacent to the basic nitrogen of the 2,6-DKP core. S-Enantiomer 7d was the most active derivative against T. brucei (IC50 = 6.8 nM) and T. cruzi (IC50 = 0.21 μM).
