1.
Bioorg Med Chem Lett
; 12(3): 311-4, 2002 Feb 11.
Artigo
em Inglês
| MEDLINE
| ID: mdl-11814785
RESUMO
The discoveries of Sch 48461 and Sch 58235 and their novel pharmacology of inhibition of cholesterol absorption have prompted efforts to determine their biological mechanism of action (MOA). To this end, a series of radioiodinated analogues with good to excellent in vivo activity have been designed and synthesized as single enantiomers. They are structurally consistent with the allowable SAR of the 2-azetidinone class of cholesterol absorption inhibitors.
Assuntos
Anticolesterolemiantes/síntese química , Anticolesterolemiantes/farmacologia , Azetidinas/síntese química , Azetidinas/farmacologia , Colesterol/farmacocinética , Absorção Intestinal/efeitos dos fármacos , Animais , Azetidinas/química , Cricetinae , Desenho de Fármacos , Ezetimiba , Marcação por Isótopo , Estereoisomerismo , Relação Estrutura-Atividade
2.
Bioorg Med Chem Lett
; 12(3): 315-8, 2002 Feb 11.
Artigo
em Inglês
| MEDLINE
| ID: mdl-11814786
RESUMO
Fluorescent analogues of the cholesterol absorption inhibitor (CAI), Sch 58235, have been designed and synthesized as single enantiomers. Biological testing reveals that they are potent CAIs and are suitable tools for the investigation of the azetidinone CAI mechanism of action (MOA).
