Functionalized spirooxindole-indolizine hybrids: Stereoselective green synthesis and evaluation of anti-inflammatory effect involving TNF-α and nitrite inhibition.
Eur J Med Chem
; 152: 417-423, 2018 May 25.
Article
em En
| MEDLINE
| ID: mdl-29751235
ABSTRACT
Stereoselective synthesis of a small library of novel spiroheterocyclic hybrids including indolizine, oxindole, and substituted piperidine units has been accomplished in [bmim]Br using a [3 + 2] cycloaddition strategy in good yield and were tested for their anti-inflammatory activities. The effects of compounds (4a-o) against inflammation were studied using carrageenan-induced hind paw oedema, croton oil-induced ear oedema, and cotton pellet-induced granuloma models. Among the heterocyclic hybrids, compounds 4d, 4g, and 4o showed significant anti-inflammatory activities against acute and chronic inflammatory models. These compounds also showed significant inhibition of PGE2, TNF-α, and nitrite levels in carrageenan-induced hind paw oedema. Thus it is evident from our study that these novel spiroheterocyclic hybrids 4d, 4g, and 4o displayed significant anti-inflammatory effects that involve the reduction of PGE2, TNF-α, and nitrite levels.
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Base de dados:
MEDLINE
Assunto principal:
Compostos de Espiro
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Anti-Inflamatórios não Esteroides
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Fator de Necrose Tumoral alfa
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Edema
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Indóis
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Indolizinas
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Nitritos
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article