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Melanin-concentrating hormone receptor 1 antagonists. Synthesis and structure-activity relationships of novel 3-(aminomethyl)quinolines.
Kamata M, Yamashita T, Imaeda T, Tanaka T, Masada S, Kamaura M, Kasai S, Hara R, Sasaki S, Takekawa S, Asami A, Kaisho T, Suzuki N, Ashina S, Ogino H, Nakano Y, Nagisa Y, Kato K, Kato K, Ishihara Y. Kamata M, et al. Among authors: takekawa s. J Med Chem. 2012 Mar 8;55(5):2353-66. doi: 10.1021/jm201596h. Epub 2012 Feb 22. J Med Chem. 2012. PMID: 22309223
Discovery, synthesis, and structure-activity relationship of 6-aminomethyl-7,8-dihydronaphthalenes as human melanin-concentrating hormone receptor 1 antagonists.
Kamata M, Yamashita T, Imaeda T, Tanaka T, Terauchi J, Miyamoto M, Ora T, Tawada M, Endo S, Takekawa S, Asami A, Suzuki N, Nagisa Y, Nakano Y, Watanabe K, Ogino H, Kato K, Kato K, Ishihara Y. Kamata M, et al. Among authors: takekawa s. Bioorg Med Chem. 2011 Sep 15;19(18):5539-52. doi: 10.1016/j.bmc.2011.07.038. Epub 2011 Jul 26. Bioorg Med Chem. 2011. PMID: 21856163
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.
Kasai S, Kamaura M, Kamata M, Aso K, Ogino H, Nakano Y, Watanabe K, Kaisho T, Tawada M, Nagisa Y, Takekawa S, Kato K, Suzuki N, Ishihara Y. Kasai S, et al. Among authors: takekawa s. Bioorg Med Chem. 2011 Nov 1;19(21):6261-73. doi: 10.1016/j.bmc.2011.09.007. Epub 2011 Sep 10. Bioorg Med Chem. 2011. PMID: 21975069
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.
Kasai S, Kamata M, Masada S, Kunitomo J, Kamaura M, Okawa T, Takami K, Ogino H, Nakano Y, Ashina S, Watanabe K, Kaisho T, Imai YN, Ryu S, Nakayama M, Nagisa Y, Takekawa S, Kato K, Murata T, Suzuki N, Ishihara Y. Kasai S, et al. Among authors: takekawa s. J Med Chem. 2012 May 10;55(9):4336-51. doi: 10.1021/jm300167z. Epub 2012 Apr 23. J Med Chem. 2012. PMID: 22490048
Discovery of a Novel Series of N-Phenylindoline-5-sulfonamide Derivatives as Potent, Selective, and Orally Bioavailable Acyl CoA:Monoacylglycerol Acyltransferase-2 Inhibitors.
Sato K, Takahagi H, Yoshikawa T, Morimoto S, Takai T, Hidaka K, Kamaura M, Kubo O, Adachi R, Ishii T, Maki T, Mochida T, Takekawa S, Nakakariya M, Amano N, Kitazaki T. Sato K, et al. Among authors: takekawa s. J Med Chem. 2015 May 14;58(9):3892-909. doi: 10.1021/acs.jmedchem.5b00178. Epub 2015 Apr 30. J Med Chem. 2015. PMID: 25897973
Optimization of a novel series of N-phenylindoline-5-sulfonamide-based acyl CoA:monoacylglycerol acyltransferase-2 inhibitors: Mitigation of CYP3A4 time-dependent inhibition and phototoxic liabilities.
Sato K, Takahagi H, Kubo O, Hidaka K, Yoshikawa T, Kamaura M, Nakakariya M, Amano N, Adachi R, Maki T, Take K, Takekawa S, Kitazaki T, Maekawa T. Sato K, et al. Among authors: takekawa s. Bioorg Med Chem. 2015 Aug 1;23(15):4544-4560. doi: 10.1016/j.bmc.2015.06.003. Epub 2015 Jun 9. Bioorg Med Chem. 2015. PMID: 26100443
A novel and selective melanin-concentrating hormone receptor 1 antagonist ameliorates obesity and hepatic steatosis in diet-induced obese rodent models.
Kawata Y, Okuda S, Hotta N, Igawa H, Takahashi M, Ikoma M, Kasai S, Ando A, Satomi Y, Nishida M, Nakayama M, Yamamoto S, Nagisa Y, Takekawa S. Kawata Y, et al. Among authors: takekawa s. Eur J Pharmacol. 2017 Feb 5;796:45-53. doi: 10.1016/j.ejphar.2016.12.018. Epub 2016 Dec 13. Eur J Pharmacol. 2017. PMID: 27986627
Potent Body Weight-Lowering Effect of a Neuromedin U Receptor 2-selective PEGylated Peptide.
Kanematsu-Yamaki Y, Nishizawa N, Kaisho T, Nagai H, Mochida T, Asakawa T, Inooka H, Dote K, Fujita H, Matsumiya K, Hirabayashi H, Sakamoto J, Ohtaki T, Takekawa S, Asami T. Kanematsu-Yamaki Y, et al. Among authors: takekawa s. J Med Chem. 2017 Jul 27;60(14):6089-6097. doi: 10.1021/acs.jmedchem.7b00330. Epub 2017 Jul 18. J Med Chem. 2017. PMID: 28657315
119 results