Molecules p. 3187 - 3197 (2009)
Update date:2022-08-11
Topics:
Chung, Man Chin
Dos Santos, Jean Leandro
Oliveira, Ednir Vizioli
Blau, Lorena
Renato Farina Menegon
Peccinini, Rosangela Goncalves
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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Doi:10.1002/mrc.1270121004
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