1.
Bioorg Med Chem Lett
; 11(19): 2593-6, 2001 Oct 08.
Artigo
em Inglês
| MEDLINE
| ID: mdl-11551757
RESUMO
A series of isoxazolyl, oxazolyl, and thiazolylpropionic acid derivatives derived from LDV was found to be a potent antagonist of the alpha(4)beta(1) integrin. The synthesis and SAR leading up to 3-[3-(1-[-[3-methoxy-4-(3-o-tolyl-ureido)-phenyl]-acetylamino]-3-methyl-butyl)-isoxazol-5-yl]-propionic acid (22) are reported. In an allergic mouse model, compound 22 was efficacious delivered systemically (58% inhib @ 10 mg/kg, sc) as well as by intra-tracheal instillation (ED(50)=2 microg/kg).
Assuntos
Integrinas/antagonistas & inibidores , Isoxazóis/farmacologia , Propionatos/farmacologia , Receptores de Retorno de Linfócitos/antagonistas & inibidores , Animais , Modelos Animais de Doenças , Humanos , Hipersensibilidade/tratamento farmacológico , Integrina alfa4beta1 , Células Jurkat , Camundongos , Relação Estrutura-Atividade
2.
J Med Chem
; 41(3): 266-70, 1998 Jan 29.
Artigo
em Inglês
| MEDLINE
| ID: mdl-9464356