Hydroxyoxazolidines as alpha-aminoacetaldehye equivalents: novel inhibitors of calpain.

Peet, N P; Kim, H O; Marquart, A L; Angelastro, M R; Nieduzak, T R; White, J N; Friedrich, D; Flynn, G A; Webster, M E; Vaz, R J; Linnik, M D; Koehl, J R; Mehdi, S; Bey, P; Emary, B; Hwang, K K

Peet, N P; Kim, H O; Marquart, A L; Angelastro, M R; Nieduzak, T R; White, J N; Friedrich, D; Flynn, G A; Webster, M E; Vaz, R J; Linnik, M D; Koehl, J R; Mehdi, S; Bey, P; Emary, B; Hwang, K K.

Afiliação

Peet NP; Hoechst Marion Roussel, Inc., Bridgewater, NJ 08807, USA.

Bioorg Med Chem Lett ; 9(16): 2365-70, 1999 Aug 16.

Article em En | MEDLINE | ID: mdl-10476870

ABSTRACT

ABSTRACT

The synthesis of [1-[(5-hydroxy-4-(phenylmethyl)-3-oxazolidinyl)carbonyl]-2-ethylpropy lcarbamic acid phenylmethyl ester (2; MDL 104,903), a potent inhibitor of calpain, is described. Synthesis of related compounds, which offer insights into the mechanism of action for 2, are also described, as is an O-acetyl prodrug derivative of 2.

Assuntos

Calpaína/antagonistas & inibidores; Carbamatos/farmacologia; Oxazóis/farmacologia; Inibidores de Proteases/farmacologia; Carbamatos/química; Espectroscopia de Ressonância Magnética; Oxazóis/química; Inibidores de Proteases/química

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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Oxazóis / Inibidores de Proteases / Carbamatos / Calpaína Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 1999 Tipo de documento: Article País de afiliação: Estados Unidos

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