4-Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1R) antagonists

被引：15
|
作者：
Jiang, Jinlong
Lin, Peter
Hoang, Myle
Chang, Lehua
Tan, Carina
Feighner, Scott
Palyha, Oksana C.
Hreniuk, Donna L.
Pan, Jie
Sailer, Andreas W.
Morin, Nancy R.
MacNeil, Douglas J.
Howard, Andrew D.
Van der Ploeg, Lex H. T.
Goulet, Mark T.
DeVita, Robert J.
机构：
[1] Merck Res Labs, Dept Med Chem, Rahway, NJ 07065 USA
[2] Merck Res Labs, Dept Metab Disorders, Rahway, NJ 07065 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 20期
关键词：
MCH; melanin-concentrating hormone; antagonist; obesity; depression; anxiety; quinoline;
D O I：
10.1016/j.bmcl.2006.08.008
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Structure-activity relationships of a 4-aminoquinoline MCHlR antagonist lead series were explored by synthesis of analogs with modifications at the 2-, 4-, and 6-positions of the original HTS hit. Improvements to the original screening lead included lipophilic groups at the 2-position and biphenyl, cyclohexyl phenyl, and hydrocinnamyl carboxamides at the 6-position. Modifications of the 4-amino group were not well tolerated. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：5275 / 5279
页数：5
相关论文
共 50 条
  • [1] Aminoquinoline melanin-concentrating hormone 1-receptor (MCH1-R) antagonists
    DeVita, Robert J.
    CURRENT TOPICS IN MEDICINAL CHEMISTRY, 2007, 7 (15) : 1433 - 1439
  • [2] Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists
    Moriya, Minoru
    Kishino, Hiroyuki
    Sakuraba, Shunji
    Sakamoto, Toshihiro
    Suga, Takuya
    Takahashi, Hidekazu
    Suzuki, Takao
    Ito, Masahiko
    Ito, Junko
    Moriya, Ryuichi
    Takenaga, Norihiro
    Iwaasa, Hisashi
    Ishihara, Akane
    Kanatani, Akio
    Fukami, Takehiro
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (13) : 3568 - 3572
  • [3] Identification and characterization of a selective radioligand for melanin-concentrating hormone 1-receptor (MCH1R)
    Ito, Masahiko
    Sakamoto, Toshihiro
    Suzuki, Takao
    Egashira, Shinichiro
    Moriya, Minoru
    Ishihara, Akane
    Iwaasa, Hisashi
    Matsushita, Hiroko
    Nakase, Kazuho
    Wallace, Michael A.
    Dean, Dennis
    Sato, Nagaaki
    Tokita, Shigeru
    Kanatani, Akio
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (10) : 2835 - 2839
  • [4] Small molecule melanin-concentrating hormone receptor 1 (MCH1R) antagonists as anxiolytic and antidepressive agents
    Dyck, B
    DRUG DEVELOPMENT RESEARCH, 2005, 65 (04) : 291 - 300
  • [5] 2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists
    Jiang, Jinlong
    Hoang, Myle
    Young, Jonathan R.
    Chaung, Danny
    Eid, Ronsar
    Turner, Cherilyn
    Lin, Peter
    Tong, Xinchun
    Wang, Junying
    Tan, Carina
    Feighner, Scott
    Palyha, Oksana
    Hreniuk, Donna L.
    Pan, Jie
    Sailer, Andreas W.
    MacNeil, Douglas J.
    Howard, Andrew
    Shearman, Lauren
    Stribling, Sloan
    Camacho, Ramon
    Strack, Alison
    Van der Ploeg, Lex H. T.
    Goulet, Mark T.
    DeVita, Robert J.
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2006, 16 (20) : 5270 - 5274
  • [6] Recent Updates on the Melanin-Concentrating Hormone (MCH) and Its Receptor System: Lessons from MCH1R Antagonists
    Shinjae Chung
    Gregory S. Parks
    Cheol Lee
    Olivier Civelli
    Journal of Molecular Neuroscience, 2011, 43 : 115 - 121
  • [7] Recent Updates on the Melanin-Concentrating Hormone (MCH) and Its Receptor System: Lessons from MCH1R Antagonists
    Chung, Shinjae
    Parks, Gregory S.
    Lee, Cheol
    Civelli, Olivier
    JOURNAL OF MOLECULAR NEUROSCIENCE, 2011, 43 (01) : 115 - 121
  • [8] Diamine template as novel Melanin-concentrating hormone 1 receptor (MCH1r) antagonists with improved cardiovascular safety
    Jiang, Yu
    Chen, Chien-An
    Chen, Bin
    Eldemenky, Eman M.
    Mazza, Christine G.
    Ray, Nick
    Marzabadi, Mohammad R.
    Forray, Carlos
    Li, Boshan
    Zhang, Hong
    Jones, Kenneth A.
    Dong, Dahai
    Chandrasena, Gamini
    Craig, Douglas A.
    Ping, Xiaoli
    Andersen, Kim
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2010, 240
  • [9] Strategy to control hERG activity of brain penetrant Melanin-concentrating hormone 1 receptor (MCH1r) antagonists
    Jiang, Yu
    Chen, Bin
    Hong, Sang-Phyo
    Eldemenky, Eman M.
    Lu, Kai
    Marzabadi, Mohammad R.
    Li, Boshan
    Zhang, Hong
    Jones, Kenneth A.
    White, Andrew D.
    Labelle, Marc
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 2010, 240
  • [10] Disruption of the Melanin-Concentrating Hormone Receptor 1 (MCH1R) Affects Thyroid Function
    Chung, Shinjae
    Liao, Xiao-Hui
    Di Cosmo, Caterina
    Van Sande, Jacqueline
    Wang, Zhiwei
    Refetoff, Samuel
    Civelli, Olivier
    ENDOCRINOLOGY, 2012, 153 (12) : 6145 - 6154
12345