Discovery of the selective sphingomyelin synthase 2 inhibitors with the novel structure of oxazolopyridine.
Bioorg Med Chem Lett
; 27(15): 3511-3515, 2017 08 01.
Article
em En
| MEDLINE
| ID: mdl-28619536
ABSTRACT
Sphingomyelin synthase (SMS) is a key enzyme in sphingomyelin biosynthetic pathway, whose activity is highly related to the atherosclerosis progression. SMS2 could serve as a promising therapeutic target for atherosclerosis. Based on the structure of lead compound D2, a series of oxazolopyridine derivatives were designed, synthesized, and their inhibitory activities against purified SMS1 and SMS2 enzymes were evaluated respectively. The representative molecules QY4 and QY16 possess micromolar inhibitory activities against SMS2 and excellent isoform preferences over SMS1, qualified to be selected as potential molecules in further discovery of specific SMS2 inhibitors.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Piridinas
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Transferases (Outros Grupos de Fosfato Substituídos)
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Inibidores Enzimáticos
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Proteínas de Membrana
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Proteínas do Tecido Nervoso
Limite:
Humans
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article