Ana Cristina Lima Leite
◽
José Wanderlan Pontes Espíndola
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Marcos Veríssimo de Oliveira Cardoso
◽
Gevanio Bezerra de Oliveira Filho
Background:
Privileged motifs are recurring in a wide range of biologically
active compounds that reach different pharmaceutical targets and pathways and could represent
a suitable start point to access potential candidates in the neglected diseases field.
The current therapies to treat these diseases are based in drugs that lack of the desired effectiveness,
affordable methods of synthesis and allow a way to emergence of resistant
strains. Due the lack of financial return, only few pharmaceutical companies have been
investing in research for new therapeutics for neglected diseases (ND).
Methods:
Based on the literature search from 2002 to 2016, we discuss how six privileged
motifs, focusing phthalimide, isatin, indole, thiosemicarbazone, thiazole, and thiazolidinone
are particularly recurrent in compounds active against some of neglected diseases.
Results:
It was observed that attention was paid particularly for Chagas disease, malaria,
tuberculosis, schistosomiasis, leishmaniasis, dengue, African sleeping sickness (Human
African Trypanosomiasis - HAT) and toxoplasmosis. It was possible to verify that, among
the ND, antitrypanosomal and antiplasmodial activities were between the most searched.
Besides, thiosemicarbazone moiety seems to be the most versatile and frequently explored
scaffold. As well, phthalimide, isatin, thiazole, and thiazolidone nucleus have been also
explored in the ND field.
Conclusion:
Some described compounds, appear to be promising drug candidates, while
others could represent a valuable inspiration in the research for new lead compounds.