Design, synthesis and biological activity of a novel ethylenediamine derivatives as H1 receptor antagonists.
Bioorg Med Chem
; 27(24): 115127, 2019 12 15.
Article
em En
| MEDLINE
| ID: mdl-31703894
ABSTRACT
In this study, a series of novel ethylenediamine compounds were obtained by structural modification of the lead compounds with thonzylamine, and using the principle of modifying by bioisostere formation and modification with alkyl groups. In vitro assay, the biological activities showed that the target compounds have good properties in inhibiting mast cell degranulation and releasing histamine and ß-aminohexidase, such as the compounds 5c, 5g, 5k, 5l and 5o, especially of compound 5k to mast cell degranulation is IC50â¯=â¯0.0106⯱â¯0.001⯵molâ
L-1, histamine release was IC50â¯=â¯0.0192⯱â¯0.005⯵molâ
L-1 and ß-hexosaminidase release was IC50â¯=â¯0.0455⯱â¯0.002⯵molâ
L-1in vitro. At the same time, in vivo biological activities assay results showed that have a good Histamie induce bronchospasm effect with relatively long duration and good protective effect in vivo, among which the protective effect of compound 5k was 79.74⯱â¯0.30%, compounds 5c, 5g, 5k, 5l and 5o could inhibit the capillary permeability of increasing which were caused by histamine.
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Texto completo:
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Base de dados:
MEDLINE
Assunto principal:
Desenho de Fármacos
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Etilenodiaminas
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Antagonistas dos Receptores Histamínicos H1
Tipo de estudo:
Clinical_trials
Limite:
Animals
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Female
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Humans
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Male
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article