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Design, synthesis and in vitro trypanocidal and leishmanicidal activities of novel semicarbazone derivatives

2015; Elsevier BV; Volume: 100; Linguagem: Inglês

10.1016/j.ejmech.2015.05.046

1768-3254

Marina Amaral Alves, Aline Cavalcanti de Queiroz, Magna Suzana Alexandre‐Moreira, Javier Varela, Hugo Cerecetto, Mercedes González, A.C. Doriguetto, I. M. R. Landre, Eliezer J. Barreiro, Lı́dia Moreira Lima,

Synthesis and Biological Evaluation

Trypanosomatids are protozoan parasites that cause various diseases in human, such as leishmaniasis, Chagas disease and sleeping sickness. The highly syntenic genomes of the trypanosomatid species lead the assumption that they can encode similar proteins, indicating the possibility to design new antitrypanosomatid drugs with dual trypanosomicidal and leishmanicidal activities. In this work a series of compounds (6a-h and 7a-h), containing a semicarbazone scaffold as a peptide mimetic framework, was designed and synthesized. From this series compound 7g (LASSBio-1483) highlighted, showing dual in vitro trypanosomicidal and leishmanicidal activities, with potency similar to the standard drugs nifurtimox and pentamidine. This data, taken together with its good in silico druglikeness profile and its great chemical and plasma stability, make LASSBio-1483 (7g) a new antitrypanosomatid lead-candidate.