1.
Bioorg Med Chem Lett
; 16(19): 4994-5000, 2006 Oct 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16904318
RESUMO
The identification of an MCH R1 antagonist screening hit led to the optimization of a class of benzimidazole-based MCH R1 antagonists. Structure-activity relationships and efforts to optimize pharmacokinetic properties are detailed along with the demonstration of the effectiveness of an MCH R1 antagonist in an animal model of obesity.
Assuntos
Benzimidazóis/farmacologia , Obesidade/tratamento farmacológico , Receptores de Somatostatina/antagonistas & inibidores , Animais , Benzimidazóis/farmacocinética , Disponibilidade Biológica , Composição Corporal , Relação Dose-Resposta a Droga , Camundongos , Modelos Animais , Relação Estrutura-Atividade , Redução de Peso/efeitos dos fármacos
2.
Bioorg Med Chem Lett
; 16(18): 4723-7, 2006 Sep 15.
Artigo
em Inglês
| MEDLINE
| ID: mdl-16870432
RESUMO
Optimization of a series of constrained melanin-concentrating hormone receptor 1 (MCH R1) antagonists has provided compounds with potent and selective MCH R1 activity. Details of the optimization process are provided and the use of one of the compounds in an animal model of diet-induced obesity is presented.
