Identification of sulfonylpyrimidines as novel selective aldosterone synthase (CYP11B2) inhibitors.
Bioorg Med Chem
; 108: 117775, 2024 Jun 15.
Article
en En
| MEDLINE
| ID: mdl-38851000
ABSTRACT
4-[(5-[2-Methyl-5-(methylsulfonyl)pentan-2-yl]sulfonylpyrimidin-4-yl)amino]benzonitrile 2 was identified as a novel potent aldosterone synthase inhibitor. Compound 2 was found to inhibit human CYP11B2 in the nanomolar range, and showed an aldosterone-lowering effect in a furosemide-treated cynomolgus monkey model. Although human CYP11B2 has the high homology sequence with human CYP11B1, compound 2 showed more than 80 times higher selectivity over human CYP11B1 in vitro.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Pirimidinas
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Citocromo P-450 CYP11B2
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Inhibidores Enzimáticos
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Macaca fascicularis
Límite:
Animals
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Humans
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2024
Tipo del documento:
Article