2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability.
Bioorg Med Chem Lett
; 18(20): 5402-5, 2008 Oct 15.
Article
em En
| MEDLINE
| ID: mdl-18835161
ABSTRACT
In this report, the strategy and outcome of expanding SAR exploration to improve solubility and metabolic stability are discussed. Compound 35 exhibited excellent potency, selectivity over A(1) and improved solubility of >4 mg/mL at pH 8.0. In addition, compound 35 had good metabolic stability with a scaled intrinsic clearance of 3 mL/min/kg (HLM) and demonstrated efficacy in the haloperidol induced catalepsy model.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirimidinas
/
Química Farmacêutica
/
Antagonistas do Receptor A2 de Adenosina
/
Aminopiridinas
Limite:
Humans
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article