The protozoan parasite Trypanosoma brucei causes human African trypanosomiasis (HAT), a fatal and neglected disease in the tropic areas. Owing to the scarcity of investments, new drug approvals, and resistance development to the current drugs, novel and selective targets are urgently needed to be explored. Trypanothione reductase, nitro-reductase, pteridine reductase 1, methionyl-tRNA synthetase, phosphodiesterases, and rhodesain represent emerging and attractive enzymes for the development of alternative anti-parasitic agents. The structure-activity relationships for each target were discussed as well as the correlation between in vitro and cell-based assays. These compounds could provide new therapeutic options for the limited arsenal of antitrypanosomal agents and are characterized by a good selectivity profile in terms of cytotoxicity against mammalian cells.

New Compounds for the Management of Trypanosoma brucei Infection

Luisi G.
Primo
;
Carradori S.
Ultimo
2022-01-01

Abstract

The protozoan parasite Trypanosoma brucei causes human African trypanosomiasis (HAT), a fatal and neglected disease in the tropic areas. Owing to the scarcity of investments, new drug approvals, and resistance development to the current drugs, novel and selective targets are urgently needed to be explored. Trypanothione reductase, nitro-reductase, pteridine reductase 1, methionyl-tRNA synthetase, phosphodiesterases, and rhodesain represent emerging and attractive enzymes for the development of alternative anti-parasitic agents. The structure-activity relationships for each target were discussed as well as the correlation between in vitro and cell-based assays. These compounds could provide new therapeutic options for the limited arsenal of antitrypanosomal agents and are characterized by a good selectivity profile in terms of cytotoxicity against mammalian cells.
2022
Antiprotozoal Drug Development and Delivery
Alane Beatriz Vermelho, Claudiu T. Supuran
Inglese
113
141
29
978-3-031-06850-8
978-3-031-06849-2
Springer
SVIZZERA
Methionyl-tRNA synthetase inhibitors; Nitro-reductase inhibitors; Phosphodiesterase inhibitors; Pteridine reductase 1 inhibitors; Rhodesain inhibitors; Trypanosoma brucei; Trypanothione reductase inhibitors
no
2 Contributo in Volume::2.1 Contributo in volume (Capitolo o Saggio)
2
268
reserved
Luisi, G.; Carradori, S.
info:eu-repo/semantics/bookPart
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11564/785793
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