Discovery of indazole aldosterone synthase (CYP11B2) inhibitors as potential treatments for hypertension.
Bioorg Med Chem Lett
; 27(11): 2384-2388, 2017 06 01.
Article
em En
| MEDLINE
| ID: mdl-28416132
ABSTRACT
We report the discovery and hit-to-lead optimization of a structurally novel indazole series of CYP11B2 inhibitors. Benchmark compound 34 from this series displays potent inhibition of CYP11B2, high selectivity versus related steroidal and hepatic CYP targets, and lead-like physical and pharmacokinetic properties. On the basis of these and other data, the indazole series was progressed to lead optimization for further refinement.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Citocromo P-450 CYP11B2
/
Hipertensão
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Indazóis
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Anti-Hipertensivos
Limite:
Animals
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Humans
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Male
Idioma:
En
Revista:
Bioorg Med Chem Lett
Assunto da revista:
BIOQUIMICA
/
QUIMICA
Ano de publicação:
2017
Tipo de documento:
Article