| Registro completo |
| Provedor de dados: |
BJPS
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| País: |
Brazil
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| Título: |
Ortho-nitrobenzyl derivatives as potential anti-schistosomal agents
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| Autores: |
Lopes,Marcela Silva
Suzuki,Brian Michio
Pereira,Glaécia Aparecida do Nascimento
Probst,Alexandra Christina
Ferreira,Rafaela Salgado
Oliveira,Júlia Teixeira de
Tecchio,Kimberly Brito
Santos,Fabio Vieira dos
Caffrey,Conor Robert
Oliveira,Renata Barbosa de
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| Data: |
2018-01-01
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| Ano: |
2018
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| Palavras-chave: |
Nitro-aromatic
Schistosoma mansoni/ anti-schistosomal activity
Cathepsin B1
Mutagenicity
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| Resumo: |
ABSTRACT In the search for new anti-schistosomal agents, a series of fifteen ortho-nitrobenzyl derivatives was assayed in vitro against both the schistosomulum (somule) and adult forms of Schistosoma mansoni. Compounds 8 and 12 showed significant activity against somules at low micromolar concentrations, but none was active against adults. The SAR demonstrated that the compounds most active against the parasite were mutagenic to the human cell line RKO-AS45-1 only at concentrations 10- to 40-fold higher than the worm-killing dose. Given their electrophilicity, compounds were also screened as inhibitors of the S. mansoni cysteine protease (cathepsin B1) in vitro. Amides 5 and 15 exhibited a modest inhibition activity with values of 55.7 and 50.6 % at 100 µM, respectively. The nitrobenzyl compounds evaluated in this work can be regarded as hits in the search for more active and safe anti-schistosomal agents.
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| Tipo: |
Info:eu-repo/semantics/article
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| Idioma: |
Inglês
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| Identificador: |
http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502018000200613
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| Editor: |
Universidade de São Paulo, Faculdade de Ciências Farmacêuticas
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| Relação: |
10.1590/s2175-97902018000217376
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| Formato: |
text/html
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| Fonte: |
Brazilian Journal of Pharmaceutical Sciences v.54 n.2 2018
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| Direitos: |
info:eu-repo/semantics/openAccess
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