Substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl-phenylalanine analogues as potent VLA-4 antagonists.
Bioorg Med Chem Lett
; 12(4): 637-40, 2002 Feb 25.
Article
em En
| MEDLINE
| ID: mdl-11844689
ABSTRACT
A series of substituted N-(3,5-dichlorobenzenesulfonyl)-L-prolyl- and alpha-methyl-L-prolyl-phenylalanine derivatives was prepared as VLA-4/VCAM antagonists. The compounds showed excellent potency with a wide variety of neutral, polar, electron withdrawing or donating groups on the phenylalanine ring (IC50 approximately 1 nM). Heteroaryl ring substitution for phenylalanine was also well tolerated. Pharmacokinetic studies in rat were performed on a representative set of compounds in both series.
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Base de dados:
MEDLINE
Assunto principal:
Integrina alfa4beta1
/
Dipeptídeos
Limite:
Animals
Idioma:
En
Ano de publicação:
2002
Tipo de documento:
Article