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Structure-based lead optimization to improve potency and selectivity of a novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid series of heparanase-1 inhibitor.
Imai Y, Suzuki R, Wakasugi D, Matsuda D, Tanaka-Yamamoto N, Ohki Y, Mima M, Endo M, Tabata R, Matsuzawa H, Hasegawa Y, Kato S, Sugisaki M, Miyagawa H, Fujimoto N, Fukunaga T, Kato S, Takahashi T, Kakinuma H. Imai Y, et al. Among authors: endo m. Bioorg Med Chem. 2023 Oct 1;93:117460. doi: 10.1016/j.bmc.2023.117460. Epub 2023 Aug 26. Bioorg Med Chem. 2023. PMID: 37660465
Discovery of N-{5-[3-(3-hydroxypiperidin-1-yl)-1,2,4-oxadiazol-5-yl]-4-methyl-1,3-thiazol-2-yl}acetamide (TASP0415914) as an orally potent phosphoinositide 3-kinase γ inhibitor for the treatment of inflammatory diseases.
Oka Y, Yabuuchi T, Oi T, Kuroda S, Fujii Y, Ohtake H, Inoue T, Wakahara S, Kimura K, Fujita K, Endo M, Taguchi K, Sekiguchi Y. Oka Y, et al. Among authors: endo m. Bioorg Med Chem. 2013 Dec 15;21(24):7578-83. doi: 10.1016/j.bmc.2013.10.042. Epub 2013 Nov 7. Bioorg Med Chem. 2013. PMID: 24262886
Lead optimization of 2-hydroxymethyl imidazoles as non-hydroxamate LpxC inhibitors: Discovery of TP0586532.
Ushiyama F, Takashima H, Matsuda Y, Ogata Y, Sasamoto N, Kurimoto-Tsuruta R, Ueki K, Tanaka-Yamamoto N, Endo M, Mima M, Fujita K, Takata I, Tsuji S, Yamashita H, Okumura H, Otake K, Sugiyama H. Ushiyama F, et al. Among authors: endo m. Bioorg Med Chem. 2021 Jan 15;30:115964. doi: 10.1016/j.bmc.2020.115964. Epub 2020 Dec 29. Bioorg Med Chem. 2021. PMID: 33385955
Design, synthesis and biological evaluation of novel 1H-pyrazole-4-carbonyl-4,5,6,7-tetrahydrobenzo [b]thiophene derivatives as gut-selective NaPi2b inhibitors.
Ushiki Y, Kawabe K, Yamamoto-Okada K, Uneuchi F, Asanuma Y, Yamaguchi C, Ohta H, Shibata T, Abe T, Okumura-Kitajima L, Kosai Y, Endo M, Otake K, Munetomo E, Takahashi T, Kakinuma H. Ushiki Y, et al. Among authors: endo m. Bioorg Med Chem Lett. 2022 Mar 1;59:128572. doi: 10.1016/j.bmcl.2022.128572. Epub 2022 Jan 21. Bioorg Med Chem Lett. 2022. PMID: 35066140
Design, synthesis and biological evaluation of novel pyridine derivatives as gut-selective NaPi2b inhibitors.
Ushiki Y, Kawabe K, Yamamoto-Okada K, Uneuchi F, Asanuma Y, Yamaguchi C, Ohta H, Shibata T, Abe T, Okumura-Kitajima L, Kosai Y, Endo M, Otake K, Munetomo E, Takahashi T, Kakinuma H. Ushiki Y, et al. Among authors: endo m. Bioorg Med Chem Lett. 2022 Jun 1;65:128700. doi: 10.1016/j.bmcl.2022.128700. Epub 2022 Mar 25. Bioorg Med Chem Lett. 2022. PMID: 35346844
3,801 results