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Lead optimization of 5-amino-6-(2,2-dimethyl-5-oxo-4-phenylpiperazin-1-yl)-4-hydroxyhexanamides to reduce a cardiac safety issue: discovery of DS-8108b, an orally active renin inhibitor.
Nakamura Y, Fujimoto T, Ogawa Y, Namiki H, Suzuki S, Asano M, Sugita C, Mochizuki A, Miyazaki S, Tamaki K, Nagai Y, Inoue S, Nagayama T, Kato M, Chiba K, Takasuna K, Nishi T. Nakamura Y, et al. Among authors: suzuki s. Bioorg Med Chem. 2013 Jun 1;21(11):3175-96. doi: 10.1016/j.bmc.2013.03.022. Epub 2013 Mar 26. Bioorg Med Chem. 2013. PMID: 23598247
N-Aryl Indoles as a Novel Class of Potent NaV1.7 Inhibitors.
Karanjule N, Hayashi N, Suzuki S, Tsuda T, Tokumaru E, Tanaka K, Kimoto H, Domon Y, Takahashi S, Kubota K, Kitano Y, Yokoyama T, Koishi R, Fujiwara C, Inaba S, Asano D, Sakakura T, Takasuna K, Shinozuka T. Karanjule N, et al. Among authors: suzuki s. ACS Med Chem Lett. 2023 May 24;14(6):788-793. doi: 10.1021/acsmedchemlett.3c00079. eCollection 2023 Jun 8. ACS Med Chem Lett. 2023. PMID: 37312847 Free PMC article.
Discovery of DS-1971a, a Potent, Selective NaV1.7 Inhibitor.
Shinozuka T, Kobayashi H, Suzuki S, Tanaka K, Karanjule N, Hayashi N, Tsuda T, Tokumaru E, Inoue M, Ueda K, Kimoto H, Domon Y, Takahashi S, Kubota K, Yokoyama T, Shimizugawa A, Koishi R, Fujiwara C, Asano D, Sakakura T, Takasuna K, Abe Y, Watanabe T, Kitano Y. Shinozuka T, et al. Among authors: suzuki s. J Med Chem. 2020 Sep 24;63(18):10204-10220. doi: 10.1021/acs.jmedchem.0c00259. Epub 2020 May 26. J Med Chem. 2020. PMID: 32392056
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