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Wiley, ChemMedChem, 9(7), p. 1623-1634, 2012

DOI: 10.1002/cmdc.201200304

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Synthesis and Biological Evaluation of CTP Synthetase Inhibitors as Potential Agents for the Treatment of African Trypanosomiasis

Journal article published in 2012 by Lucia Tamborini ORCID, Andrea Pinto, Terry K. Smith, Louise L. Major, Maria C. Iannuzzi, Sandro Cosconati ORCID, Luciana Marinelli, Ettore Novellino, Leonardo Lo Presti, Pui E. Wong, Michael P. Barrett, Carlo De Micheli, Paola Conti ORCID
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This paper is available in a repository.

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Abstract

Acivicin analogues with an increased affinity for CTP synthetase (CTPS) were designed as potential new trypanocidal agents. The inhibitory activity against CTPS can be improved by increasing the molecular complexity, by inserting groups able to establish additional interaction with the binding pocket of the enzyme. This strategy has been pursued with the synthesis of α-amino-substituted analogues of Acivicin and N1-substituted-pyrazoline derivatives. In general, there is a direct correlation between the enzymatic activity and the in vitro anti-trypanosomal efficacy of the derivatives studied here. However, this cannot be taken as a general rule, since other important factors may play a role, notably the ability of uptake / diffusion of the molecules into the trypanosomes.