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

Chin, Chung Man [UNESP]dos Santos, Jean Leandro [UNESP]Oliveira, Ednir Vizioli [UNESP]Blau, Lorena [UNESP]Menegon, Renato Farina [UNESP]Peccinini, Rosangela Goncalves [UNESP]2014-05-202014-05-202009-09-01Molecules. Basel: Molecular Diversity Preservation International-mdpi, v. 14, n. 9, p. 3187-3197, 2009.1420-3049http://hdl.handle.net/11449/7781The 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.3187-3197engindolinonepro-druganti-inflammatoryhydrolysisdiclofenacSynthesis, ex Vivo and in Vitro Hydrolysis Study of an Indoline Derivative Designed as an Anti-Inflammatory with Reduced Gastric Ulceration PropertiesArtigo10.3390/molecules14093187WOS:000270201900007Acesso abertoWOS000270201900007.pdf973433360797541310667434239290930000-0003-4141-0455