Pyrazole derivatives as new potent and selective 20-hydroxy-5,8,11,14-eicosatetraenoic acid synthase inhibitors |
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Authors: | Nakamura Toshio Kakinuma Hiroyuki Amada Hideaki Miyata Noriyuki Taniguchi Kazuo Koda Ayumi Sato Masakazu |
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Institution: | Medicinal Research Laboratories, Taisho Pharmaceutical Co. Ltd, 403 Yoshino-Cho 1-Chome, Kita-ku, Saitama-Shi, Saitama 331-9530, Japan. toshio.nakamura@po.rd.taisho.co.jp |
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Abstract: | Improvement of the physical properties of pyrazole derivative 1, which we reported previously as a potent and selective 20-HETE synthase inhibitor (IC(50) 5.7 nM), is described. Introduction of a sufficient substituted-amino group on the side chain enhanced the water-solubility of 1 (0.014 mg/mL at pH 6.8). Among the products, 2-piperazinoethoxy derivatives 3e and 6b showed solubility suitable for injection and potent inhibitory activity toward 20-HETE synthase (IC(50) 21.2 and 14.0 nM, respectively). |
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