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The inhibitory activity against CTPS can be improved by increasing molecular complexity, by inserting groups able to establish additional interactions with the binding pocket of the enzyme. This strategy has been pursued with the synthesis of \u03b1\u2010amino\u2010substituted analogues of Acivicin and N1\u2010substituted pyrazoline derivatives. In general, there is direct correlation between the enzymatic activity and the in\u2005vitro anti\u2010trypanosomal efficacy of the derivatives studied here. 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