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Page 1
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: nakayama m. 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: nakayama m. 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: nakayama m. 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: nakayama m. 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
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: nakayama m. 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
Correction to 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: nakayama m. J Med Chem. 2016 Apr 14;59(7):3577. doi: 10.1021/acs.jmedchem.6b00433. Epub 2016 Apr 5. J Med Chem. 2016. PMID: 27045534 No abstract available.
Synthesis and biological evaluation of novel selective androgen receptor modulators (SARMs). Part II: Optimization of 4-(pyrrolidin-1-yl)benzonitrile derivatives.
Asano M, Hitaka T, Imada T, Yamada M, Morimoto M, Shinohara H, Hara T, Yamaoka M, Santou T, Nakayama M, Imai Y, Habuka N, Yano J, Wilson K, Fujita H, Hasuoka A. Asano M, et al. Among authors: nakayama m. Bioorg Med Chem Lett. 2017 May 1;27(9):1897-1901. doi: 10.1016/j.bmcl.2017.03.038. Epub 2017 Mar 21. Bioorg Med Chem Lett. 2017. PMID: 28363748
Discovery of orally efficacious RORγt inverse agonists, part 1: Identification of novel phenylglycinamides as lead scaffolds.
Shirai J, Tomata Y, Kono M, Ochida A, Fukase Y, Sato A, Masada S, Kawamoto T, Yonemori K, Koyama R, Nakagawa H, Nakayama M, Uga K, Shibata A, Koga K, Okui T, Shirasaki M, Skene R, Sang B, Hoffman I, Lane W, Fujitani Y, Yamasaki M, Yamamoto S. Shirai J, et al. Among authors: nakayama m. Bioorg Med Chem. 2018 Jan 15;26(2):483-500. doi: 10.1016/j.bmc.2017.12.006. Epub 2017 Dec 9. Bioorg Med Chem. 2018. PMID: 29262987
3,249 results