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Rational Design of Novel 1,3-Oxazine Based β-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust Aβ Reduction in the Brain.
Fuchino K, Mitsuoka Y, Masui M, Kurose N, Yoshida S, Komano K, Yamamoto T, Ogawa M, Unemura C, Hosono M, Ito H, Sakaguchi G, Ando S, Ohnishi S, Kido Y, Fukushima T, Miyajima H, Hiroyama S, Koyabu K, Dhuyvetter D, Borghys H, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI. Fuchino K, et al. Among authors: kurose n. J Med Chem. 2018 Jun 28;61(12):5122-5137. doi: 10.1021/acs.jmedchem.8b00002. Epub 2018 May 23. J Med Chem. 2018. PMID: 29733614
Structure-activity relationship studies and discovery of a potent transient receptor potential vanilloid (TRPV1) antagonist 4-[3-chloro-5-[(1S)-1,2-dihydroxyethyl]-2-pyridyl]-N-[5-(trifluoromethyl)-2-pyridyl]-3,6-dihydro-2H-pyridine-1-carboxamide (V116517) as a clinical candidate for pain management.
Tafesse L, Kanemasa T, Kurose N, Yu J, Asaki T, Wu G, Iwamoto Y, Yamaguchi Y, Ni C, Engel J, Tsuno N, Patel A, Zhou X, Shintani T, Brown K, Hasegawa T, Shet M, Iso Y, Kato A, Kyle DJ. Tafesse L, et al. Among authors: kurose n. J Med Chem. 2014 Aug 14;57(15):6781-94. doi: 10.1021/jm500818a. Epub 2014 Aug 1. J Med Chem. 2014. PMID: 25057800
Discovery of novel 5-hydroxy-4-pyridone-3-carboxy acids as potent inhibitors of influenza Cap-dependent endonuclease.
Miyagawa M, Akiyama T, Mikamiyama-Iwata M, Hattori K, Kurihara N, Taoda Y, Takahashi-Kageyama C, Kurose N, Mikamiyama H, Suzuki N, Takaya K, Tomita K, Matsuo K, Morimoto K, Yoshida R, Shishido T, Yoshinaga T, Sato A, Kawai M. Miyagawa M, et al. Among authors: kurose n. Bioorg Med Chem Lett. 2016 Oct 1;26(19):4739-4742. doi: 10.1016/j.bmcl.2016.08.038. Epub 2016 Aug 18. Bioorg Med Chem Lett. 2016. PMID: 27568084
Discovery of clinical candidate Sivopixant (S-600918): Lead optimization of dioxotriazine derivatives as selective P2X3 receptor antagonists.
Kai H, Horiguchi T, Kameyma T, Onodera N, Itoh N, Fujii Y, Ichihashi Y, Hirai K, Shintani T, Nakamura K, Minami K, Kasai E, Yoneda S, Murakami Y, Ogawa H, Sekimoto R, Shinohara S, Yoshida O, Kurose N. Kai H, et al. Among authors: kurose n. Bioorg Med Chem Lett. 2021 Nov 15;52:128384. doi: 10.1016/j.bmcl.2021.128384. Epub 2021 Sep 26. Bioorg Med Chem Lett. 2021. PMID: 34587541 Free article.
Synthesis and antiviral activity of 7-benzyl-4-hydroxy-1,5-naphthyridin-2(1H)-one HIV integrase inhibitors.
Boros EE, Edwards CE, Foster SA, Fuji M, Fujiwara T, Garvey EP, Golden PL, Hazen RJ, Jeffrey JL, Johns BA, Kawasuji T, Kiyama R, Koble CS, Kurose N, Miller WH, Mote AL, Murai H, Sato A, Thompson JB, Woodward MC, Yoshinaga T. Boros EE, et al. Among authors: kurose n. J Med Chem. 2009 May 14;52(9):2754-61. doi: 10.1021/jm801404b. J Med Chem. 2009. PMID: 19374386
106 results