RESUMO
The decarboxylation of L-aspartate by E. coli L-aspartate-alpha-decarboxylase (ADC) is shown to occur with retention of configuration; analysis of the protein structure identifies Tyr58 as the proton donor in the decarboxylation mechanism.
Assuntos
Glutamato Descarboxilase/química , Glutamato Descarboxilase/metabolismo , Tirosina/metabolismo , Sítios de Ligação , Escherichia coli/enzimologia , Regulação Bacteriana da Expressão Gênica , Modelos Moleculares , Ressonância Magnética Nuclear Biomolecular , Conformação Proteica , Prótons , EstereoisomerismoRESUMO
N-Acyl and N-sulfonylhydroxymetyhylpyrroles have been synthesised and shown to inhibit alpha-chymotrypsin. A hydrophobic group in the N-substituent has been shown to be required for activity.
Assuntos
Quimotripsina/antagonistas & inibidores , Pirróis/farmacologia , Inibidores de Serina Proteinase/farmacologia , Animais , Bovinos , Cinética , Pirróis/síntese química , Inibidores de Serina Proteinase/síntese química , Relação Estrutura-AtividadeRESUMO
We report a general method for the synthesis of mycalazol 11 and some related 5-acyl-2-hydroxymethylpyrroles using a Stille coupling of 5-(tri-n-butylstannyl)pyrrole-2-carboxaldehyde with an acid chloride as the key step. The newly prepared 5-acyl-2-hydroxymethylpyrroles 5-7, together with the 5-carboxamido-2-hydroxymethylpyrrole 10, have been assayed for in vitro cytotoxicity against the P388 murine leukemia cell line.