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Design, synthesis and anti-P. falciparum activity of pyrazolopyridine-sulfonamide derivatives.

Abstract：

:Ten 1-phenyl-1H-pyrazolo[3,4-b]pyridine derivatives connected by a linker group to benzenesulfonamide moieties with different substituents in the 4-position were synthesized and assayed against Plasmodium falciparum. These ten compounds exhibited activity in vitro against the chloroquine-resistant clone W2 with IC50 values ranging from 3.46 to 9.30μM. The most active derivatives with substituent R2=Cl or CH3 at the benzenesulfonamide moiety exhibited the lowest IC50. Compounds with an R1=CO2Et substituent at the 5-position of the 1H-pyrazolo[3,4-b]pyridine ring presented lower activity than those with a CN substituent. The 1H-pyrazolo[3,4-b]pyridine system appears to be promising for further studies as an antimalarial for overcoming the burden of resistance in P. falciparum.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Silva TB,Bernardino AMR,Ferreira MLG,Rogerio KR,Carvalho LJM,Boechat N,Pinheiro LCS

doi

10.1016/j.bmc.2016.07.049

subject

Has Abstract

pub_date

2016-09-15 00:00:00

pages

4492-4498

issue

18

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(16)30566-1

journal_volume

24

pub_type

杂志文章

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