1.
Bioorg Med Chem Lett
; 21(8): 2450-5, 2011 Apr 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21398122
RESUMO
A novel series of CCR5 antagonists were identified based on the redesign of Schering C. An SAR was established based on inhibition of CCR5 (RANTES) binding and these compounds exhibited potent inhibition of R5 HIV-1 replication in peripheral blood mononuclear cells.
Assuntos
Amidas/química , Antagonistas dos Receptores CCR5 , Óxidos N-Cíclicos/química , HIV-1/efeitos dos fármacos , Piperidinas/química , Piridinas/química , Amidas/síntese química , Amidas/farmacocinética , Animais , Cães , Desenho de Fármacos , Humanos , Oximas , Ratos , Receptores CCR5/metabolismo , Relação Estrutura-Atividade , Replicação Viral/efeitos dos fármacos
2.
Bioorg Med Chem Lett
; 21(1): 262-6, 2011 Jan 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-21109432
RESUMO
An early lead from the AMD070 program was optimized and a structure-activity relationship was developed for a novel series of heterocyclic containing compounds. Potent CXCR4 antagonists were identified based on anti-HIV-1 activity and Ca(2+) flux inhibition that displayed good pharmacokinetics in rat and dog.