1.
Bioorg Med Chem Lett
; 20(2): 608-11, 2010 Jan 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-20005710
RESUMO
The triaryl bis-sulfone 1 was modified by converting the aryl A-ring to a piperidine ring. The piperidine ring was further elaborated to a spirocyclopropyl piperidine moiety. The effect on CB2 binding potency, rat calcium channel affinity, and CYP 2C9 inhibition is described.
Assuntos
Receptor CB2 de Canabinoide/antagonistas & inibidores , Sulfonamidas/síntese química , Sulfonas/química , Sulfonas/síntese química , Animais , Canais de Cálcio/metabolismo , Sistema Enzimático do Citocromo P-450 , Agonismo Inverso de Drogas , Humanos , Piperidinas/química , Ratos , Receptor CB2 de Canabinoide/metabolismo , Relação Estrutura-Atividade , Sulfonamidas/química , Sulfonamidas/farmacocinética , Sulfonas/farmacocinética
2.
Bioorg Med Chem Lett
; 15(5): 1375-8, 2005 Mar 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15713390
RESUMO
Bipiperidine amide 1 has been identified as a CC chemokine receptor 3 (CCR3) antagonist. Optimization of its structure-activity relationship has resulted in the identification of cis (R,R)-4-[(3,4-dichlorophenyl)methyl]-3-hydroxymethyl-1'(6-quinolinylcarbonyl)-1,4'-bipiperidine 14n, which exhibits potent receptor affinity and inhibition of both calcium flux and eosinophil chemotaxis.
