Discovery of novel phenethylpyridone derivatives as potent melanin-concentrating hormone 1 receptor antagonists
详细信息 查看全文
- 作者：Makoto Ando ; Etsuko Sekino ; Yuji Haga ; Minoru Moriya ; Masahiko Ito ; Junko Ito ; Hisashi Iwaasa ; Akane Ishihara ; Akio Kanatani ; Norikazu Ohtake
- 关键词：Melanin-concentrating hormone 1 receptor antagonist ; Phenethylpyridone ; Anti-obesity
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2009
- 出版时间：1 September 2009
- 年：2009
- 卷：19
- 期：17
- 页码：5186-5190
- 全文大小：1547 K
文摘
Novel phenethylpyridone derivatives were identified as potent human melanin-concentrating hormone 1 receptor (MCH-1R) antagonists. A search for surrogates for the 4-(2-aminoethoxy)phenyl moiety of 1 resulted in discovery of 2-[4-(aminomethyl)phenyl]ethyl substructure as in 6a. Successive optimization of the right-hand moiety led to the identification of a number of potent derivatives.