Novel 3-nitrotriazole-based amides and carbinols as bifunctional antichagasic agents.
J Med Chem
; 58(3): 1307-19, 2015 Feb 12.
Article
em En
| MEDLINE
| ID: mdl-25580906
ABSTRACT
3-Nitro-1H-1,2,4-triazole-based amides with a linear, rigid core and 3-nitrotriazole-based fluconazole analogues were synthesized as dual functioning antitrypanosomal agents. Such compounds are excellent substrates for type I nitroreductase (NTR) located in the mitochondrion of trypanosomatids and, at the same time, act as inhibitors of the sterol 14α-demethylase (T. cruzi CYP51) enzyme. Because combination treatments against parasites are often superior to monotherapy, we believe that this emerging class of bifunctional compounds may introduce a new generation of antitrypanosomal drugs. In the present work, the synthesis and in vitro and in vivo evaluation of such compounds is discussed.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Triazóis
/
Tripanossomicidas
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Trypanosoma cruzi
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Trypanosoma brucei rhodesiense
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Doença de Chagas
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Metanol
/
Amidas
Limite:
Animals
Idioma:
En
Ano de publicação:
2015
Tipo de documento:
Article