Synthesis and evaluation of benzylisoquinoline derivatives for their inhibition on pancreatic lipase and preadipocyte proliferation / 中国天然药物
Chinese Journal of Natural Medicines (English Ed.)
;
(6): 382-390, 2016.
Article
Dans Anglais
| WPRIM
| ID: wpr-812600
ABSTRACT
The present study was designed to synthesize and evaluate a series of benzylisoquinoline derivatives. These compounds were synthesized by Bischler-Napieralski cyclization to yield 1-benzyl-3,4-dihydroisoquinolines, and the products were obtained by reductions. All these compounds were identified by MS, (1)H NMR and (13)C NMR. The inhibitory activities on pancreatic lipase and preadipocyte proliferation for the synthesized compounds and alkaloids from Nulembo nucifera were assessed in vitro. Most of the compounds showed inhibitory activities on both pancreatic lipase and preadipocyte proliferation. Particularly, compounds 7p-7u and 9d-9f exhibited significant inhibitory activity on pancreatic lipase while compounds 7c, 7d, 7f, 7g, 7i, and 7j potently inhibited the proliferation of 3T3-L1 preadipocytes. Our results provided a basis for future evaluation and development of these compounds as leads for therapeutics for human diseases.
Texte intégral:
Disponible
Indice:
WPRIM (Pacifique occidental)
Sujet Principal:
Pharmacologie
/
Relation structure-activité
/
Chimie
/
Adipocytes
/
Biologie cellulaire
/
Benzylisoquinoléines
/
Prolifération cellulaire
/
Antienzymes
/
Triacylglycerol lipase
/
Métabolisme
Limites du sujet:
Humains
langue:
Anglais
Texte intégral:
Chinese Journal of Natural Medicines (English Ed.)
Année:
2016
Type:
Article
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