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

Silva Thais B.; Bernardino Alice M. R.; Ferreira Maria de Lourdes G.Rogerio Kamilla R.Carvalho Leonardo J. M.Boechat NubiaPinheiro Luiz C. S.

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

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

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Ten 1-phenyl-1H-pyrazolo3,4-bpyridine derivatives connected by a linker group to benzenesulfon-amide 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 9.30 mu M. The most active derivatives with substituent R-2 = Cl or CH3 at the benzenesulfonamide moiety exhibited the lowest IC50. Compounds with an R-1 = CO2Et substituent at the 5-position of the 1H-pyrazolo3,4-bpyridine ring presented lower activity than those with a CN substituent. The 1H-pyrazolo3,4-bpyridine system appears to be promising for further studies as an antimalarial for overcoming the burden of resistance in P. falciparum. (C) 2016 Elsevier Ltd. All rights reserved.

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《Bioorganic and medicinal chemistry》 |2016年第18期|4492-4498|共7页
作者
Silva Thais B.; Bernardino Alice M. R.; Ferreira Maria de Lourdes G.Rogerio Kamilla R.Carvalho Leonardo J. M.Boechat NubiaPinheiro Luiz C. S.;
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作者单位

Fundacao Oswaldo Cruz, Farmanguinhos FIOCRUZ, Inst Tecnol Farmacos, Dept Sintese Farmacos, Rua;

Fundacao Oswaldo Cruz, Inst Oswaldo Cruz, Lab Pesquisa Malaria, BR-21041250 Rio De Janeiro, RJ;

Univ Fed Fluminense, Dept Quim Organ, Programa Posgrad Quim, Niteroi, RJ, Brazil;

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正文语种英语
中图分类药学;
关键词
Malaria; Pyrazolopyridine; Sulfonamide; Plasmodium falciparum;

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

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