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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. 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
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 1: Initial structure-activity relationship studies of a hit from a high throughput screening.
Tobinaga H, Kameyama T, Oohara M, Kobayashi N, Ohdan M, Ishizuka N, Kume M, Tomari M, Tanaka Y, Takahashi F, Kinoshita H, Shimada S, Shinohara S, Kai H. Tobinaga H, et al. Bioorg Med Chem Lett. 2018 Jul 15;28(13):2338-2342. doi: 10.1016/j.bmcl.2017.04.060. Epub 2017 Apr 19. Bioorg Med Chem Lett. 2018. PMID: 29805055
Pyrrolinone derivatives as a new class of P2X3 receptor antagonists. Part 3: Structure-activity relationships of pyrropyrazolone derivatives.
Tobinaga H, Kameyama T, Asahi K, Horiguchi T, Oohara M, Taoda Y, Hata K, Hasegawa T, Tada Y, Kurihara N, Kanda Y, Yagi S, Tomari M, Tanaka Y, Takahashi F, Taniguchi E, Takahara Y, Shimada S, Takeyama C, Yamamoto S, Shinohara S, Kai H. Tobinaga H, et al. Bioorg Med Chem Lett. 2020 Dec 15;30(24):127636. doi: 10.1016/j.bmcl.2020.127636. Epub 2020 Oct 22. Bioorg Med Chem Lett. 2020. PMID: 33132115