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Discovery of a novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid derivative as a potent and selective heparanase-1 inhibitor utilizing an improved synthetic approach.
Imai Y, Suzuki R, Matsuda D, Tanaka-Yamamoto N, Ohki Y, Tabata R, Kato S, Sugisaki M, Fujimoto N, Fukunaga T, Kato S, Takahashi T, Kakinuma H. Imai Y, et al. Among authors: kakinuma h. Bioorg Med Chem Lett. 2024 Jan 1;97:129543. doi: 10.1016/j.bmcl.2023.129543. Epub 2023 Nov 6. Bioorg Med Chem Lett. 2024. PMID: 37939863
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: kakinuma h. 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 Novel Pyrazolylpyridine Derivatives for 20-Hydroxyeicosatetraenoic Acid Synthase Inhibitors with Selective CYP4A11/4F2 Inhibition.
Kawamura M, Kobashi Y, Tanaka H, Bohno-Mikami A, Hamada M, Ito Y, Hirata T, Ohara H, Kojima N, Koretsune H, Gunji E, Fukunaga T, Inatani S, Hasegawa Y, Suzuki A, Takahashi T, Kakinuma H. Kawamura M, et al. Among authors: kakinuma h. J Med Chem. 2022 Nov 10;65(21):14599-14613. doi: 10.1021/acs.jmedchem.2c01089. Epub 2022 Nov 1. J Med Chem. 2022. PMID: 36318660
Discovery of novel 2-[(4-hydroxy-6-oxo-2,3-dihydro-1H-pyridine-5-carbonyl)amino]acetic acid derivatives as HIF prolyl hydroxylase inhibitors for treatment of renal anemia.
Hamada M, Takayama T, Shibata T, Hiratate A, Takahashi M, Yashiro M, Takayama N, Okumura-Kitajima L, Koretsune H, Kajiyama H, Naruse T, Kato S, Takano H, Kakinuma H. Hamada M, et al. Among authors: kakinuma h. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1725-1730. doi: 10.1016/j.bmcl.2018.04.039. Epub 2018 Apr 16. Bioorg Med Chem Lett. 2018. PMID: 29681433
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: kakinuma h. 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
Design, synthesis and biological evaluation of novel indole 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: kakinuma h. Bioorg Med Chem. 2022 Jul 15;66:116783. doi: 10.1016/j.bmc.2022.116783. Epub 2022 May 2. Bioorg Med Chem. 2022. PMID: 35576656
173 results