Utilize este identificador para referenciar este registo: http://hdl.handle.net/10451/21518
Título: Cyclization-activated prodrugs
Autor: Gomes, Paula
Vale, Nuno
Moreira, Rui
Palavras-chave: Chemistry, Organic
Data: 2007
Editora: MOLECULAR DIVERSITY PRESERVATION INT
Citação: MOLECULES. - Vol. 12, n. 11 (NOV 2007), p. 2484-2506
Resumo: Many drugs suffer from an extensive first-pass metabolism leading to drug inactivation and/or production of toxic metabolites, which makes them attractive targets for prodrug design. The classical prodrug approach, which involves enzyme-sensitive covalent linkage between the parent drug and a carrier moiety, is a well established strategy to overcome bioavailability/toxicity issues. However, the development of prodrugs that can regenerate the parent drug through non-enzymatic pathways has emerged as an alternative approach in which prodrug activation is not influenced by inter- and intraindividual variability that affects enzymatic activity. Cyclization-activated prodrugs have been capturing the attention of medicinal chemists since the middle-1980s, and reached maturity in prodrug design in the late 1990s. Many different strategies have been exploited in recent years concerning the development of intramoleculary-activated prodrugs spanning from analgesics to anti-HIV therapeutic agents. Intramolecular pathways have also a key role in two-step prodrug activation, where an initial enzymatic cleavage step is followed by a cyclization-elimination reaction that releases the active drug. This work is a brief overview of research on cyclization-activated prodrugs from the last two decades.
URI: http://hdl.handle.net/10451/21518
ISSN: 1420-3049
Aparece nas colecções:FF - Produção Científica 2000-2009

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