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Discovery of novel 5-oxa-2,6-diazaspiro[3.4]oct-6-ene derivatives as potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonists for treatment of type 2 diabetes mellitus.
Hirose H, Yamasaki T, Ogino M, Mizojiri R, Tamura-Okano Y, Yashiro H, Muraki Y, Nakano Y, Sugama J, Hata A, Iwasaki S, Watanabe M, Maekawa T, Kasai S. Hirose H, et al. Among authors: kasai s. Bioorg Med Chem. 2017 Aug 1;25(15):4175-4193. doi: 10.1016/j.bmc.2017.06.007. Epub 2017 Jun 9. Bioorg Med Chem. 2017. PMID: 28642028
Discovery of novel somatostatin receptor subtype 5 (SSTR5) antagonists: Pharmacological studies and design to improve pharmacokinetic profiles and human Ether-a-go-go-related gene (hERG) inhibition.
Yamasaki T, Hirose H, Yamashita T, Takakura N, Morimoto S, Nakahata T, Kina A, Nakano Y, Okano Tamura Y, Sugama J, Odani T, Shimizu Y, Iwasaki S, Watanabe M, Maekawa T, Kasai S. Yamasaki T, et al. Among authors: kasai s. Bioorg Med Chem. 2017 Aug 1;25(15):4153-4162. doi: 10.1016/j.bmc.2017.06.003. Epub 2017 Jun 13. Bioorg Med Chem. 2017. PMID: 28622905
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. 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
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: kasai 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
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. J Med Chem. 2012 May 10;55(9):4336-51. doi: 10.1021/jm300167z. Epub 2012 Apr 23. J Med Chem. 2012. PMID: 22490048
Melanin-Concentrating Hormone Receptor 1 Antagonists Lacking an Aliphatic Amine: Synthesis and Structure-Activity Relationships of Novel 1-(Imidazo[1,2-a]pyridin-6-yl)pyridin-2(1H)-one Derivatives.
Igawa H, Takahashi M, Kakegawa K, Kina A, Ikoma M, Aida J, Yasuma T, Kawata Y, Ashina S, Yamamoto S, Kundu M, Khamrai U, Hirabayashi H, Nakayama M, Nagisa Y, Kasai S, Maekawa T. Igawa H, et al. Among authors: kasai s. J Med Chem. 2016 Feb 11;59(3):1116-39. doi: 10.1021/acs.jmedchem.5b01704. Epub 2016 Jan 22. J Med Chem. 2016. PMID: 26736071
Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel 1-(1H-benzimidazol-6-yl)pyridin-2(1H)-one derivatives and design to avoid CYP3A4 time-dependent inhibition.
Igawa H, Takahashi M, Shirasaki M, Kakegawa K, Kina A, Ikoma M, Aida J, Yasuma T, Okuda S, Kawata Y, Noguchi T, Yamamoto S, Fujioka Y, Kundu M, Khamrai U, Nakayama M, Nagisa Y, Kasai S, Maekawa T. Igawa H, et al. Among authors: kasai s. Bioorg Med Chem. 2016 Jun 1;24(11):2486-2503. doi: 10.1016/j.bmc.2016.04.011. Epub 2016 Apr 6. Bioorg Med Chem. 2016. PMID: 27112449
Amine-free melanin-concentrating hormone receptor 1 antagonists: Novel non-basic 1-(2H-indazole-5-yl)pyridin-2(1H)-one derivatives and mitigation of mutagenicity in Ames test.
Igawa H, Takahashi M, Ikoma M, Kaku H, Kakegawa K, Kina A, Aida J, Okuda S, Kawata Y, Noguchi T, Hotta N, Yamamoto S, Nakayama M, Nagisa Y, Kasai S, Maekawa T. Igawa H, et al. Among authors: kasai s. Bioorg Med Chem. 2016 Jun 1;24(11):2504-2518. doi: 10.1016/j.bmc.2016.04.013. Epub 2016 Apr 7. Bioorg Med Chem. 2016. PMID: 27117261
730 results