Orientador(es)
Resumo(s)
Dipeptide esters of paracetamol were prepared in high yields. These compounds are quantitatively hydrolyzed to paracetamol and corresponding 2,5-diketopiperazines at pH 7.4 and 37 ° C. The reactivity is increased in sarcosine and proline peptides and decreased by bulky side chains at both the N- and C-terminal residues of the dipeptide carrier. Moreover, dipeptide esters of paracetamol did not affect the levels of hepatic glutathione. Thus, dipeptides seem promising candidates as carriers for cyclization-activated prodrugs. © 2005 Elsevier Ltd. All rights reserved.
Descrição
Palavras-chave
Chemistry, Medicinal Chemistry, Organic
Contexto Educativo
Citação
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - Vol. 15, n. 6 (2005), p. 1595-1598
Editora
PERGAMON-ELSEVIER SCIENCE LTD