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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: yamano y. 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: yamano y. 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
Discovery of an Extremely Potent Thiazine-Based β-Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.
Tadano G, Komano K, Yoshida S, Suzuki S, Nakahara K, Fuchino K, Fujimoto K, Matsuoka E, Yamamoto T, Asada N, Ito H, Sakaguchi G, Kanegawa N, Kido Y, Ando S, Fukushima T, Teisman A, Urmaliya V, Dhuyvetter D, Borghys H, Van Den Bergh A, Austin N, Gijsen HJM, Yamano Y, Iso Y, Kusakabe KI. Tadano G, et al. Among authors: yamano y. J Med Chem. 2019 Oct 24;62(20):9331-9337. doi: 10.1021/acs.jmedchem.9b01140. Epub 2019 Oct 8. J Med Chem. 2019. PMID: 31549838
Trifluoromethyl Dihydrothiazine-Based β-Secretase (BACE1) Inhibitors with Robust Central β-Amyloid Reduction and Minimal Covalent Binding Burden.
Anan K, Iso Y, Oguma T, Nakahara K, Suzuki S, Yamamoto T, Matsuoka E, Ito H, Sakaguchi G, Ando S, Morimoto K, Kanegawa N, Kido Y, Kawachi T, Fukushima T, Teisman A, Urmaliya V, Dhuyvetter D, Borghys H, Austin N, Van Den Bergh A, Verboven P, Bischoff F, Gijsen HJM, Yamano Y, Kusakabe K. Anan K, et al. Among authors: yamano y. ChemMedChem. 2019 Nov 20;14(22):1894-1910. doi: 10.1002/cmdc.201900478. Epub 2019 Nov 12. ChemMedChem. 2019. PMID: 31657130
Cefiderocol (S-649266), A new siderophore cephalosporin exhibiting potent activities against Pseudomonas aeruginosa and other gram-negative pathogens including multi-drug resistant bacteria: Structure activity relationship.
Aoki T, Yoshizawa H, Yamawaki K, Yokoo K, Sato J, Hisakawa S, Hasegawa Y, Kusano H, Sano M, Sugimoto H, Nishitani Y, Sato T, Tsuji M, Nakamura R, Nishikawa T, Yamano Y. Aoki T, et al. Among authors: yamano y. Eur J Med Chem. 2018 Jul 15;155:847-868. doi: 10.1016/j.ejmech.2018.06.014. Epub 2018 Jun 8. Eur J Med Chem. 2018. PMID: 29960205
A novel series of parenteral cephalosporins exhibiting potent activities against both Pseudomonas aeruginosa and other gram-negative pathogens. Part 2: Synthesis and structure-activity relationships.
Yamawaki K, Nomura T, Yasukata T, Tanimoto N, Uotani K, Miwa H, Yamano Y, Takeda K, Nishitani Y. Yamawaki K, et al. Among authors: yamano y. Bioorg Med Chem. 2008 Feb 15;16(4):1632-47. doi: 10.1016/j.bmc.2007.11.028. Epub 2007 Nov 17. Bioorg Med Chem. 2008. PMID: 18065229
In Vitro Antimicrobial Activity of a Siderophore Cephalosporin, S-649266, against Enterobacteriaceae Clinical Isolates, Including Carbapenem-Resistant Strains.
Kohira N, West J, Ito A, Ito-Horiyama T, Nakamura R, Sato T, Rittenhouse S, Tsuji M, Yamano Y. Kohira N, et al. Among authors: yamano y. Antimicrob Agents Chemother. 2015 Nov 16;60(2):729-34. doi: 10.1128/AAC.01695-15. Print 2016 Feb. Antimicrob Agents Chemother. 2015. PMID: 26574013 Free PMC article.
In vitro antimicrobial activity of S-649266, a catechol-substituted siderophore cephalosporin, when tested against non-fermenting Gram-negative bacteria.
Ito A, Kohira N, Bouchillon SK, West J, Rittenhouse S, Sader HS, Rhomberg PR, Jones RN, Yoshizawa H, Nakamura R, Tsuji M, Yamano Y. Ito A, et al. Among authors: yamano y. J Antimicrob Chemother. 2016 Mar;71(3):670-7. doi: 10.1093/jac/dkv402. Epub 2015 Dec 7. J Antimicrob Chemother. 2016. PMID: 26645269
709 results