Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists
详细信息 查看全文
- 作者：Minoru Moriya ; Hiroyuki Kishino ; Shunji Sakuraba ; Toshihiro Sakamoto ; Takuya Suga ; Hidekazu Takahashi ; Takao Suzuki ; Masahiko Ito ; Junko Ito ; Ryuichi Moriya ; Norihiro Takenaga ; Hisashi Iwaasa ; Akane I
- 关键词：MCHIR-antagonist ; Melanin-concentrating hormone ; Obesity ; GPCR
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：1 July 2009
- 年：2009
- 卷：19
- 期：13
- 页码：3568-3572
- 全文大小：1362 K
文摘
A series of 2-aminobenzimidazole-based MCH1R antagonists was identified by core replacement of the aminoquinoline lead 1. Subsequent modification of the 2- and 5-positions led to improvement in potency and intrinsic clearance. Compound 25 exhibited good plasma and brain exposure, and attenuated MCH induced food intake at 30 mg/kg PO in rats.