Novel and highly potent histamine H3 receptor ligands. Part 3: an alcohol function to improve the pharmacokinetic profile.
Bioorg Med Chem Lett
; 23(9): 2548-54, 2013 May 01.
Article
em En
| MEDLINE
| ID: mdl-23535326
ABSTRACT
Synthesis and biological evaluation of potent histamine H3 receptor antagonists incorporating a hydroxyl function are described. Compounds in this series exhibited nanomolar binding affinities for human receptor, illustrating a new possible component for the H3 pharmacophore. As demonstrated with compound BP1.4160 (cyclohexanol 19), the introduction of an alcohol function counter-intuitively allowed to reach high in vivo efficiency and favorable pharmacokinetic profile with reduced half-life.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Receptores Histamínicos H3
/
Cicloexanóis
/
Etanol
/
Antagonistas dos Receptores Histamínicos H3
/
Ligantes
Limite:
Animals
/
Humans
/
Male
Idioma:
En
Ano de publicação:
2013
Tipo de documento:
Article