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

Artigo

Date

2009-09-01

Registration in:

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

1420-3049

http://hdl.handle.net/11449/7781

10.3390/molecules14093187

WOS:000270201900007

WOS000270201900007.pdf

9734333607975413

1066743423929093

0000-0003-4141-0455

http://repositorioslatinoamericanos.uchile.cl/handle/2250/3884559

Author

Universidade Estadual Paulista (Unesp)

Institutions

Universidade Paulista Júlio de Mesquita Filho (Brasil)

Abstract

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.

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