| Full text | |
| Author(s): |
Chung, Man Chin
[1]
;
dos Santos, Jean Leandro
[1]
;
Oliveira, Ednir Vizioli
[1]
;
Blau, Lorena
[1]
;
Menegon, Renato Farina
[1]
;
Peccinini, Rosangela Goncalves
[2]
Total Authors: 6
|
| Affiliation: | [1] UNESP, Fac Ciencias Farmaceut, Dept Farmacos & Medicamentos, Lapdesf Lab Pesquisa & Desenvolvimento Farmacos, BR-14801902 Araraquara, SP - Brazil
[2] UNESP, Fac Ciencias Farmaceut, Dept Principios Ativos Nat & Toxicol, BR-14801902 Araraquara, SP - Brazil
Total Affiliations: 2
|
| Document type: | Journal article |
| Source: | Molecules; v. 14, n. 9, p. 3187-3197, SEP 2009. |
| Web of Science Citations: | 10 |
| 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. (AU) | |
| FAPESP's process: | 07/56115-0 - Optimization, synthesis and pharmacological evaluation of dual hybrid compounds useful to treat the symptoms of sickle cell disease |
| Grantee: | Jean Leandro dos Santos |
| Support Opportunities: | Scholarships in Brazil - Doctorate |