The synthesis and evaluation of phenoxyacylhydroxamic acids as potential agents for Helicobacter pylori infections.
Bioorg Med Chem
; 26(14): 4145-4152, 2018 08 07.
Article
em En
| MEDLINE
| ID: mdl-29983280
ABSTRACT
Two series of ω-phenoxy contained acylhydroxamic acids as novel urease inhibitors were designed and synthesized. Biological activity evaluations revealed that ω-phenoxypropinoylhydroxamic acids were more active than phenoxyacetohydroxamic acids. Out of these compounds, 3-(3,4-dichlorophenoxy)propionylhydroxamic acid c24 showed significant potency against urease in both cell free extract (IC50â¯=â¯0.061⯱â¯0.003⯵M) and intact cell (IC50â¯=â¯0.89⯱â¯0.05⯵M), being over 450- and 120-fold more potent than the clinically prescribed urease inhibitor AHA, repectively. Non-linear fitting of experimental data (V-[S]) suggested a mixed-type inhibition mechanism and a dual site binding mode of these compounds.
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MEDLINE
Assunto principal:
Urease
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Helicobacter pylori
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Infecções por Helicobacter
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Inibidores Enzimáticos
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Ácidos Hidroxâmicos
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Antibacterianos
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article