Ontology highlight
ABSTRACT:
SUBMITTER: Fytas C
PROVIDER: S-EPMC3140774 | biostudies-literature | 2011 Jul
REPOSITORIES: biostudies-literature
Fytas Christos C Zoidis Grigoris G Tzoutzas Nikolaos N Taylor Martin C MC Fytas George G Kelly John M JM
Journal of medicinal chemistry 20110627 14
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 act ...[more]