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Current Medicinal Chemistry
ISSN (Print): 0929-8673
ISSN (Online): 1875-533X
VOLUME: 20
ISSUE: 21
DOI: 10.2174/0929867311320210005      Price:  $58









Trypanosomatidae Diseases: From the Current Therapy to the Efficacious Role of Trypanothione Reductase in Drug Discovery

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Author(s): L.S.C. Bernardes, C.L. Zani and I. Carvalho
Pages 2673-2696 (24)
Abstract:
According to World Health Organization (WHO), trypanosomiasis and leishmaniasis are the most challenging among the neglected tropical diseases. Comparative studies between Leishmania spp and Trypanosoma cruzi have been conducted aiming to find a broad spectrum antiprotozoal agent acting against both parasites. Among the potential molecular target, Trypanothione reductase (TR) is considered an ideal enzyme since it is involved in the unique thiol-based metabolism observed in the Trypanosomatidae family and is a validated target for the search of antitrypanosomatidae drugs. In this review we intend to describe the currently available therapy to treat trypanosomatidae diseases and to highlight important aspects of trypanothione reductase as a target for the search of new and selective inhibitors, such as tricyclic, diphenylsulfide, bicyclic and heterocyclic, polyamine, natural product, N-oxide and nitroheterocyclic, aryl β- aminocarbonyl and α,β-unsaturated carbonyl derivatives.
Keywords:
Antitrypanosomatidae drugs, trypanosomatidae diseases, trypanothione reductase, trypanothione reductase inhibitors.
Affiliation:
Faculdade de Ciencias Farmaceuticas de Ribeirao Preto, Universidade de Sao Paulo, Av. do Cafe, s/n, Monte Alegre, Ribeirao Preto-SP, Brazil, CEP 14040-903.