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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: ogawa m. 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
Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine β-Secretase (BACE1) Inhibitors via Active Conformation Stabilization.
Nakahara K, Fuchino K, Komano K, Asada N, Tadano G, Hasegawa T, Yamamoto T, Sako Y, Ogawa M, Unemura C, Hosono M, Ito H, Sakaguchi G, Ando S, Ohnishi S, Kido Y, Fukushima T, Dhuyvetter D, Borghys H, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI. Nakahara K, et al. Among authors: ogawa m. J Med Chem. 2018 Jul 12;61(13):5525-5546. doi: 10.1021/acs.jmedchem.8b00011. Epub 2018 Jun 14. J Med Chem. 2018. PMID: 29775538
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists Part 2: Discovery of orally bioavailable compounds.
Tobinaga H, Kameyama T, Asahi K, Horiguchi T, Oohara M, Tada Y, Fuchino K, Jikihara S, Endoh T, Kurihara N, Kanda Y, Ogawa M, Tamura N, Yagi S, Taniguchi E, Takahara Y, Shimada S, Takeyama C, Yamamoto S, Shinohara S, Kai H. Tobinaga H, et al. Among authors: ogawa m. Bioorg Med Chem Lett. 2019 Mar 1;29(5):688-693. doi: 10.1016/j.bmcl.2019.01.039. Epub 2019 Feb 1. Bioorg Med Chem Lett. 2019. PMID: 30728111
4,723 results