1.
Bioorg Med Chem Lett
; 15(12): 3081-5, 2005 Jun 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15876531
RESUMO
The synthesis and SAR of 5-heterocycle-substituted aminothiazole adenosine receptor antagonists is described. Several compounds show high affinity and selectivity for the A2B and A3 receptors. One compound (5f) shows good ADME properties in the rat and as such may be an important new compound in testing the current hypotheses proposing a therapeutic role for a dual A2B/A3 antagonist in allergic diseases.
Assuntos
Antagonistas do Receptor A2 de Adenosina , Antagonistas do Receptor A3 de Adenosina , Receptor A2B de Adenosina/metabolismo , Receptor A3 de Adenosina/metabolismo , Tiazóis , Animais , Compostos Heterocíclicos/síntese química , Compostos Heterocíclicos/farmacocinética , Compostos Heterocíclicos/farmacologia , Ratos , Ratos Wistar , Relação Estrutura-Atividade , Tiazóis/síntese química , Tiazóis/farmacocinética , Tiazóis/farmacologia
2.
Bioorg Med Chem
; 12(19): 5213-24, 2004 Oct 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15351404
RESUMO
A series of novel corticosteroid derivatives featuring C-17 furoate ester functionality have been synthesised. Profiling in vitro and in vivo has resulted in the identification of a compound with a longer duration of action and a lower oral side effect profile in rodents compared to budesonide.