One-pot synthesis of novel tert-butyl-4-substituted phenyl-1H-1,2,3-triazolo piperazine/piperidine carboxylates, potential GPR119 agonists.
Bioorg Med Chem Lett
; 29(23): 126707, 2019 12 01.
Article
em En
| MEDLINE
| ID: mdl-31630858
ABSTRACT
We have synthesized a new series of 1,2,3-triazolo piperazine and piperidine carboxylate derivatives using a simple and one-pot click chemistry with significantly reduced reaction times (~5â¯min) and enhanced reaction yields (~95-98%). The fourteen novel compounds thus synthesized were tested for ability to target GPR119, a G-protein coupled target receptor that plays critical role in regulation of type-2 diabetes mellitus. Four analogs (3e, 3g, 5e and 5g) demonstrated similar or better EC50 values over previously reported AR231453 activity towards GPR119.
Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Piperidinas
/
Receptores Acoplados a Proteínas G
/
Química Click
/
Piperazina
Limite:
Humans
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article