A novel dipeptidyl peptidase IV inhibitors developed through scaffold hopping and drug splicing strategy / 药学学报
Acta Pharmaceutica Sinica
;
(12): 61-67, 2014.
Artigo
em Chinês
| WPRIM
| ID: wpr-297970
ABSTRACT
Though all the marketed drugs of dipeptidyl peptidase IV inhibitors are structurally different, their inherent correlation is worthy of further investigation. Herein we rapidly discovered a novel DPP-IV inhibitor 8g (IC50 = 4.9 nmol.L-1) which exhibits as good activity and selectivity as the market drugs through scaffold hopping and drug splicing strategies based on alogliptin and linagliptin. This study demonstrated that the employment of classic medicinal chemistry strategy to the marketed drugs with specific target is an efficient approach to discover novel bioactive molecules.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Piperidinas
/
Relação Estrutura-Atividade
/
Uracila
/
Desenho de Fármacos
/
Estrutura Molecular
/
Química
/
Inibidores da Dipeptidil Peptidase IV
/
Descoberta de Drogas
/
Linagliptina
/
Hipoglicemiantes
Limite:
Humanos
Idioma:
Chinês
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2014
Tipo de documento:
Artigo
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