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Curr Med Chem. 2019;26(23):4323-4354. doi: 10.2174/0929867324666171023163752.

Privileged Structures in the Design of Potential Drug Candidates for Neglected Diseases.

Author information

1
Departamento de Ciencias Farmaceuticas, Centro de Ciencias da Saude, Universidade Federal de Pernambuco, 50740-520, Recife, PE, Brazil.
2
Colegiado de Nutricao, Campus Petrolina, Universidade de Pernambuco, 56328-903, Petrolina, PE, Brazil.
3
Faculdade de Integração do Sertão - FIS, Rua João Luiz de Melo, 2110 - COHAB, Serra Talhada - PE, Brazil.

Abstract

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.

KEYWORDS:

Privileged structures; antiparasitic drugs; indole; isatine; leishmania; phthalimide; plasmodium; thiazole; thiazolidinone antiprotozoal chemotherapy; thiosemicarbazone; trypanosoma.

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