Synthesis, ex Vivo and in Vitro Hydrolysis Study of an Indoline Derivative Designed as an Anti-Inflammatory with Reduced Gastric Ulceration Properties

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Data

2009-09-01

Autores

Chin, Chung Man [UNESP]
dos Santos, Jean Leandro [UNESP]
Oliveira, Ednir Vizioli [UNESP]
Blau, Lorena [UNESP]
Menegon, Renato Farina [UNESP]
Peccinini, Rosangela Goncalves [UNESP]

Título da Revista

ISSN da Revista

Título de Volume

Editor

Molecular Diversity Preservation International-mdpi

Resumo

The compound 1-(2,6-dichlorophenyl)indolin-2-one (1), planned as a pro-drug of diclofenac (2), was easily synthesized in 94% yield by an intramolecular reaction in the presence of coupling agent (i.e., EDC). Compound 1 showed anti-inflammatory and analgesic activity without gastro-ulcerogenic effects. The chemical and enzymatic hydrolysis profile of the lactam derivative 1 does not indicate conversion to diclofenac (2). This compound is a new non-ulcerogenic prototype for treatment of chronic inflammatory diseases.

Descrição

Palavras-chave

indolinone, pro-drug, anti-inflammatory, hydrolysis, diclofenac

Como citar

Molecules. Basel: Molecular Diversity Preservation International-mdpi, v. 14, n. 9, p. 3187-3197, 2009.