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Discovery of novel somatostatin receptor subtype 5 (SSTR5) antagonists: Pharmacological studies and design to improve pharmacokinetic profiles and human Ether-a-go-go-related gene (hERG) inhibition.
Yamasaki T, Hirose H, Yamashita T, Takakura N, Morimoto S, Nakahata T, Kina A, Nakano Y, Okano Tamura Y, Sugama J, Odani T, Shimizu Y, Iwasaki S, Watanabe M, Maekawa T, Kasai S. Yamasaki T, et al. Among authors: yamashita t. Bioorg Med Chem. 2017 Aug 1;25(15):4153-4162. doi: 10.1016/j.bmc.2017.06.003. Epub 2017 Jun 13. Bioorg Med Chem. 2017. PMID: 28622905
Discovery of a 3-pyridylacetic acid derivative (TAK-100) as a potent, selective and orally active dipeptidyl peptidase IV (DPP-4) inhibitor.
Miyamoto Y, Banno Y, Yamashita T, Fujimoto T, Oi S, Moritoh Y, Asakawa T, Kataoka O, Yashiro H, Takeuchi K, Suzuki N, Ikedo K, Kosaka T, Tsubotani S, Tani A, Sasaki M, Funami M, Amano M, Yamamoto Y, Aertgeerts K, Yano J, Maezaki H. Miyamoto Y, et al. Among authors: yamashita t. J Med Chem. 2011 Feb 10;54(3):831-50. doi: 10.1021/jm101236h. Epub 2011 Jan 10. J Med Chem. 2011. PMID: 21218817
Design, synthesis, and structure-activity relationships of spirolactones bearing 2-ureidobenzothiophene as acetyl-CoA carboxylases inhibitors.
Yamashita T, Kamata M, Endo S, Yamamoto M, Kakegawa K, Watanabe H, Miwa K, Yamano T, Funata M, Sakamoto J, Tani A, Mol CD, Zou H, Dougan DR, Sang B, Snell G, Fukatsu K. Yamashita T, et al. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6314-8. doi: 10.1016/j.bmcl.2011.08.117. Epub 2011 Sep 6. Bioorg Med Chem Lett. 2011. PMID: 21944854
Symmetrical approach of spiro-pyrazolidinediones as acetyl-CoA carboxylase inhibitors.
Kamata M, Yamashita T, Kina A, Tawada M, Endo S, Mizukami A, Sasaki M, Tani A, Nakano Y, Watanabe Y, Furuyama N, Funami M, Amano N, Fukatsu K. Kamata M, et al. Among authors: yamashita t. Bioorg Med Chem Lett. 2012 Jul 15;22(14):4769-72. doi: 10.1016/j.bmcl.2012.05.062. Epub 2012 May 19. Bioorg Med Chem Lett. 2012. PMID: 22677317
Design, Synthesis, and Evaluation of [18F]T-914 as a Novel Positron-Emission Tomography Tracer for Lysine-Specific Demethylase 1.
Matsuda S, Hattori Y, Matsumiya K, McQuade P, Yamashita T, Aida J, Sandiego CM, Gouasmat A, Carroll VM, Barret O, Tamagnan G, Koike T, Kimura H. Matsuda S, et al. Among authors: yamashita t. J Med Chem. 2021 Sep 9;64(17):12680-12690. doi: 10.1021/acs.jmedchem.1c00653. Epub 2021 Aug 23. J Med Chem. 2021. PMID: 34423983 Free article.
Discovery of Pyrazolo[1,5-a]pyrazin-4-ones as Potent and Brain Penetrant GluN2A-Selective Positive Allosteric Modulators Reducing AMPA Receptor Binding Activity.
Sakurai F, Yukawa T, Kina A, Murakami M, Takami K, Morimoto S, Seto M, Kamata M, Yamashita T, Nakashima K, Narita N, Bettini E, Ugolini A, Corsi M, Hasui T. Sakurai F, et al. Among authors: yamashita t. Bioorg Med Chem. 2022 Feb 15;56:116576. doi: 10.1016/j.bmc.2021.116576. Epub 2021 Dec 16. Bioorg Med Chem. 2022. PMID: 35051811 Free article.
Design and synthesis of 6-methylpyridin-2-one derivatives as novel and potent GluN2A positive allosteric modulators for the treatment of cognitive impairment.
Yukawa T, Yamashita T, Imaeda T, Kakei H, Hashizume S, Nakamura M, Daini M, Okabe A, Nakashima K, Harada A, Narita N, Bettini E, Ugolini A, Corsi M, Hasui T. Yukawa T, et al. Among authors: yamashita t. Bioorg Med Chem. 2023 Feb 1;79:117150. doi: 10.1016/j.bmc.2022.117150. Epub 2022 Dec 24. Bioorg Med Chem. 2023. PMID: 36640594 Free article.
Design and synthesis of 3-pyridylacetamide derivatives as dipeptidyl peptidase IV (DPP-4) inhibitors targeting a bidentate interaction with Arg125.
Miyamoto Y, Banno Y, Yamashita T, Fujimoto T, Oi S, Moritoh Y, Asakawa T, Kataoka O, Takeuchi K, Suzuki N, Ikedo K, Kosaka T, Tsubotani S, Tani A, Funami M, Amano M, Yamamoto Y, Aertgeerts K, Yano J, Maezaki H. Miyamoto Y, et al. Among authors: yamashita t. Bioorg Med Chem. 2011 Jan 1;19(1):172-85. doi: 10.1016/j.bmc.2010.11.038. Epub 2010 Nov 25. Bioorg Med Chem. 2011. PMID: 21163664
6,799 results