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Review

Recent developments in the discovery of MCH-1R antagonists for the treatment of obesity – an update

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Pages 1303-1313 | Published online: 30 Sep 2005

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (2)

Anders Johansson. (2011) Recent progress in the discovery of melanin-concentrating hormone 1-receptor antagonists. Expert Opinion on Therapeutic Patents 21:6, pages 905-925.
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Laura L Rokosz. (2007) Discovery and development of melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity. Expert Opinion on Drug Discovery 2:10, pages 1301-1327.
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Articles from other publishers (36)

Larry Yet. 2018. Privileged Structures in Drug Discovery. Privileged Structures in Drug Discovery 155 193 .
Larry Yet. 2018. Privileged Structures in Drug Discovery. Privileged Structures in Drug Discovery 83 154 .
Larry Yet. 2018. Privileged Structures in Drug Discovery. Privileged Structures in Drug Discovery 481 535 .
Thomas Högberg, Thomas M. Frimurer & Pradip K. Sasmal. (2012) Melanin concentrating hormone receptor 1 (MCHR1) antagonists—Still a viable approach for obesity treatment?. Bioorganic & Medicinal Chemistry Letters 22:19, pages 6039-6047.
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Shizuo Kasai, Makoto Kamata, Shinichi Masada, Jun Kunitomo, Masahiro Kamaura, Tomohiro Okawa, Kazuaki Takami, Hitomi Ogino, Yoshihide Nakano, Shuntarou Ashina, Kaoru Watanabe, Tomoko Kaisho, Yumi N. Imai, Sunghi Ryu, Masaharu Nakayama, Yasutaka Nagisa, Shiro Takekawa, Koki Kato, Toshiki Murata, Nobuhiro Suzuki & Yuji Ishihara. (2012) Synthesis, Structure–Activity Relationship, and Pharmacological Studies of Novel Melanin-Concentrating Hormone Receptor 1 Antagonists 3-Aminomethylquinolines: Reducing Human Ether-a-go-go-Related Gene (hERG) Associated Liabilities. Journal of Medicinal Chemistry 55:9, pages 4336-4351.
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Sanjita Sasmal, Gade Balaji, Hariprasada R. Kanna Reddy, D. Balasubrahmanyam, Gujjary Srinivas, ShivaKumar Kyasa, Pradip K. Sasmal, Ish Khanna, Rashmi Talwar, J. Suresh, Vikram P. Jadhav, Syed Muzeeb, Dhanya Shashikumar, K. Harinder Reddy, V.J. Sebastian, Thomas M. Frimurer, Øystein Rist, Lisbeth Elster & Thomas Högberg. (2012) Design and optimization of quinazoline derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists. Bioorganic & Medicinal Chemistry Letters 22:9, pages 3157-3162.
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Shizuo Kasai, Masahiro Kamaura, Makoto Kamata, Kazuyoshi Aso, Hitomi Ogino, Yoshihide Nakano, Kaoru Watanabe, Tomoko Kaisho, Michiko Tawada, Yasutaka Nagisa, Shiro Takekawa, Koki Kato, Nobuhiro Suzuki & Yuji Ishihara. (2011) Melanin-concentrating hormone receptor 1 antagonists: Synthesis, structure–activity relationship, docking studies, and biological evaluation of 2,3,4,5-tetrahydro-1H-3-benzazepine derivatives. Bioorganic & Medicinal Chemistry 19:21, pages 6261-6273.
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Pradip K. Sasmal, Sanjita Sasmal, Chandrasekhar Abbineni, B. Venkatesham, P. Tirumala Rao, M. Roshaiah, Ish Khanna, V. J. Sebastian, J. Suresh, Manvendra P. Singh, Rashmi Talwar, Dhanya Shashikumar, K. Harinder Reddy, Thomas M. Frimurer, Øystein Rist, Lisbeth Elster & Thomas Högberg. (2011) Synthesis and SAR studies of benzimidazole derivatives as melanin concentrating hormone receptor 1 (MCHR1) antagonists: Focus to detune hERG inhibition. MedChemComm 2:5, pages 385.
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Yuji Haga, Sayaka Mizutani, Akira Naya, Hiroyuki Kishino, Hisashi Iwaasa, Masahiko Ito, Junko Ito, Minoru Moriya, Nagaaki Sato, Norihiro Takenaga, Akane Ishihara, Shigeru Tokita, Akio Kanatani & Norikazu Ohtake. (2011) Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists. Bioorganic & Medicinal Chemistry 19:2, pages 883-893.
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Pradip K. Sasmal, Sanjita Sasmal, P. Tirumala Rao, B. Venkatesham, M. Roshaiah, Chandrasekhar Abbineni, Ish Khanna, Vikram P. Jadhav, J. Suresh, Rashmi Talwar, Syed Muzeeb, Jean-Marie Receveur, Thomas M. Frimurer, Øystein Rist, Lisbeth Elster & Thomas Högberg. (2010) Discovery of novel, orally available benzimidazoles as melanin concentrating hormone receptor 1 (MCHR1) antagonists. Bioorganic & Medicinal Chemistry Letters 20:18, pages 5443-5448.
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Hiroyuki Kishino, Minoru Moriya, Shunji Sakuraba, Toshihiro Sakamoto, Hidekazu Takahashi, Takao Suzuki, Ryuichi Moriya, Masahiko Ito, Hisashi Iwaasa, Norihiro Takenaga, Akane Ishihara, Akio Kanatani, Nagaaki Sato & Takehiro Fukami. (2009) Discovery of imidazo[1,2-a]pyridines as potent MCH1R antagonists. Bioorganic & Medicinal Chemistry Letters 19:16, pages 4589-4593.
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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 Ishihara, Akio Kanatani & Takehiro Fukami. (2009) Identification of 2-aminobenzimidazoles as potent melanin-concentrating hormone 1-receptor (MCH1R) antagonists. Bioorganic & Medicinal Chemistry Letters 19:13, pages 3568-3572.
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José L. Méndez-Andino & John A. Wos. (2007) MCH-R1 antagonists: what is keeping most research programs away from the clinic?. Drug Discovery Today 12:21-22, pages 972-979.
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Fabrice Balavoine, Patrice Malabre, Thierry Alleaume, Astrid Rey, Valérie Cherfils, Olivier Jeanneton, Sophie Seigneurin-Venin & Frédéric Revah. (2007) Design and synthesis of novel hydantoin-containing melanin-concentrating hormone receptor antagonists. Bioorganic & Medicinal Chemistry Letters 17:13, pages 3754-3759.
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J. P. H. Wilding. (2007) Treatment strategies for obesity. Obesity Reviews 8:s1, pages 137-144.
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Tao Guo, Huizhong Gu, Doug W. Hobbs, Dennis E. Busler & Laura L. Rokosz. (2007) Discovery of tetralin ureas as potent melanin concentrating hormone 1 receptor antagonists. Bioorganic & Medicinal Chemistry Letters 17:6, pages 1718-1721.
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Rosa Arienzo, Sue Cramp, Hazel J. Dyke, Peter M. Lockey, Dennis Norman, Alan G. Roach, Phil Smith, Melanie Wong & Stephen P. Wren. (2007) Quinazoline and benzimidazole MCH-1R antagonists. Bioorganic & Medicinal Chemistry Letters 17:5, pages 1403-1407.
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José L. Méndez-Andino, Anny-Odile Colson, Kenneth M. Meyers, Maria C. Mitchell, Karen Hodge, Jeremy M. Howard, Nicholas Kim, David C. Ackley, Jerry K. Holbert, Scott W. Mittelstadt, Martin E. Dowty, Cindy M. Obringer, Paula Suchanek, Ofer Reizes, X. Eric Hu & John A. Wos. (2007) The efficacy and cardiac evaluation of aminomethyl tetrahydronaphthalene ketopiperazines: A novel class of potent MCH-R1 antagonists. Bioorganic & Medicinal Chemistry 15:5, pages 2092-2105.
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Kenneth M. Meyers, José Méndez-Andino, Anny-Odile Colson, X. Eric Hu, John A. Wos, Maria C. Mitchell, Karen Hodge, Jeremy Howard, Jennifer L. Paris, Martin E. Dowty, Cindy M. Obringer & Ofer Reizes. (2007) Novel pyrazolopiperazinone- and pyrrolopiperazinone-based MCH-R1 antagonists. Bioorganic & Medicinal Chemistry Letters 17:3, pages 657-661.
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José Méndez-Andino, Anny-Odile Colson, Daniel Denton, Maria C. Mitchell, Doreen Cross-Doersen & X. Eric Hu. (2007) MCH-R1 antagonists based on an arginine scaffold: SAR studies on the amino-terminus. Bioorganic & Medicinal Chemistry Letters 17:3, pages 832-835.
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Kenneth M. Meyers, Nicholas Kim, José L. Méndez-Andino, X. Eric Hu, Rashid N. Mumin, Sean R. Klopfenstein, John A. Wos, Maria C. Mitchell, Jennifer L. Paris, David C. Ackley, Jerry K. Holbert, Scott W. Mittelstadt & Ofer Reizes. (2007) Aminomethyl tetrahydronaphthalene biphenyl carboxamide MCH-R1 antagonists—Increasing selectivity over hERG. Bioorganic & Medicinal Chemistry Letters 17:3, pages 814-818.
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Kenneth M. Meyers, José L. Méndez-Andino, Anny-Odile Colson, Namal C. Warshakoon, John A. Wos, Maria C. Mitchell, Karen M. Hodge, Jeremy M. Howard, David C. Ackley, Jerry K. Holbert, Scott W. Mittelstadt, Martin E. Dowty, Cindy M. Obringer, Ofer Reizes & X. Eric Hu. (2007) Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists—Increasing selectivity over hERG. Bioorganic & Medicinal Chemistry Letters 17:3, pages 819-822.
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Tao Guo, Rachael C. Hunter, Rui Zhang & William J. Greenlee. (2007) Microwave assisted synthesis of isothiazolo-, thiazolo-, imidazo-, and pyrimido-pyrimidinones as novel MCH1R antagonists. Tetrahedron Letters 48:4, pages 613-615.
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Robert GoodnowJr.Jr. & Paul Gillespie. 2007. Progress in Medicinal Chemistry Volume 45. Progress in Medicinal Chemistry Volume 45 1 61 .
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Jinlong Jiang, Myle Hoang, Jonathan R. Young, Danny Chaung, Ronsar Eid, Cherilyn Turner, Peter Lin, Xinchun Tong, Junying Wang, Carina Tan, Scott Feighner, Oksana Palyha, Donna L. Hreniuk, Jie Pan, Andreas W. Sailer, Douglas J. MacNeil, Andrew Howard, Lauren Shearman, Sloan Stribling, Ramon Camacho, Alison Strack, Lex H.T. Van der Ploeg, Mark T. Goulet & Robert J. DeVita. (2006) 2-Aminoquinoline melanin-concentrating hormone (MCH)1R antagonists. Bioorganic & Medicinal Chemistry Letters 16:20, pages 5270-5274.
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Andrew J. Carpenter, Kamal A. Al-Barazanji, Kevin K. Barvian, Michael J. Bishop, Christy S. Britt, Joel P. Cooper, Aaron S. Goetz, Mary K. Grizzle, Donald L. Hertzog, Diane M. Ignar, Ronda O. Morgan, Gregory E. Peckham, Jason D. Speake & Will R. Swain. (2006) Novel benzimidazole-based MCH R1 antagonists. Bioorganic & Medicinal Chemistry Letters 16:19, pages 4994-5000.
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