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Trypanocidal activity of new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine derivatives: Synthesis, in vitro and in vivo studies.

Abstract：

:Despite the serious public health problems caused by Chagas disease in several countries, the available therapy remains with only two drugs that are poorly active during the chronic phase of the disease in addition to having severe side effects. In search of new trypanocidal agents, herein we describe the synthesis and biological evaluation of eleven new 1,6-diphenyl-1H-pyrazolo[3,4-b]pyridine compounds containing the carbohydrazide or the 2,3-dihydro-1,3,4-oxadiazole moieties. Two of them showed promising in vitro activity against amastigote forms of T. cruzi and were evaluated in vivo in male BALB/c mice infected with T. cruzi Y strain. Our results suggest that the substitution at the C-2 position of the phenyl group connected to the carbohydrazide or to the 2,3-dihydro-1,3,4-oxadiazole moieties plays an important role in the trypanocidal activity of this class of compounds. Moreover, the compound containing the 2,3-dihydro-1,3,4-oxadiazole moiety has demonstrated more favorable structural requirements for in vivo activity than its carbohydrazide analog.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Ribeiro JLS,Soares JCAV,Portapilla GB,Providello MV,Lima CHS,Muri EMF,de Albuquerque S,Dias LRS

doi

10.1016/j.bmc.2020.115855

subject

Has Abstract

pub_date

2021-01-01 00:00:00

pages

115855

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(20)30685-4

journal_volume

29

pub_type

杂志文章

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