Potency and selectivity of P2/P3-modified inhibitors of cysteine proteases from trypanosomes.
Bioorg Med Chem Lett
; 18(2): 624-8, 2008 Jan 15.
Article
em En
| MEDLINE
| ID: mdl-18055204
ABSTRACT
A systematic study of P2 and P3 substitution in a series of vinyl sulfone cysteine protease inhibitors is described. The introduction of a methyl substituent in the P2 phenylalanine aryl ring had a favorable effect on protease inhibition and conferred modest selectivity for rhodesain over cruzain. Rhodesain selectivity could be enhanced further by combining these P2 modifications with certain P3 amide substituents.
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Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Ácidos Sulfônicos
/
Tripanossomicidas
/
Trypanosoma
/
Inibidores de Cisteína Proteinase
/
Etilenos
Limite:
Animals
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article