Synthesis and evaluation of novel dapsone-thalidomide hybrids for the treatment of type 2 leprosy reactions
s.l; s.n; 2014. 4 p. tab, graf.
Não convencional
em Inglês
| Sec. Est. Saúde SP, HANSEN, Hanseníase, SESSP-ILSLPROD, Sec. Est. Saúde SP, SESSP-ILSLACERVO, Sec. Est. Saúde SP
| ID: biblio-1095645
Biblioteca responsável:
BR191.1
Localização: BR191.1; 9560/S
ABSTRACT
We synthesized a series of novel dapsone-thalidomide hybrids (3a-i) by molecular hybridization and evaluated their potential for the treatment of type 2 leprosy reactions. All of the compounds had analgesic properties. Compounds 3c and 3h were the most active antinociceptive compounds and reduced acetic acid-induced abdominal constrictions by 49.8% and 39.1%, respectively. The hybrid compounds also reduced tumor necrosis factor-α levels in lipopolysaccharide-stimulated L929 cells. Compound 3i was the most active compound; at concentrations of 15.62 and 125 µM, compound 3i decreased tumor necrosis factor-α levels by 86.33% and 87.80%, respectively. In nude mice infected with Mycobacterium leprae in vivo, compound 3i did not reduce the number of bacilli compared with controls. Compound 3i did not have mutagenic effects in Salmonella typhimurium strains TA100 and TA102, with or without metabolic activation (S9 mixture). Our results indicate that compound 3i is a novel lead compound for the treatment of type 2 leprosy reactions.
Texto completo:
Disponível
Coleções:
Bases de dados nacionais
/
Brasil
Contexto em Saúde:
ODS3 - Saúde e Bem-Estar
/
Doenças Neglicenciadas
Base de dados:
HANSEN
/
Hanseníase
/
Sec. Est. Saúde SP
/
SESSP-ILSLACERVO
/
SESSP-ILSLPROD
Assunto principal:
Relação Estrutura-Atividade
/
Talidomida
/
Estrutura Molecular
/
Linhagem Celular
/
Dapsona
/
Relação Dose-Resposta a Droga
/
Hanseníase
/
Antibacterianos
/
Mycobacterium leprae
Limite:
Animais
/
Humanos
Idioma:
Inglês
Ano de publicação:
2014
Tipo de documento:
Não convencional
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