502654-48-0Relevant articles and documents
Pyrazole derivatives as new potent and selective 20-hydroxy-5,8,11,14- eicosatetraenoic acid synthase inhibitors
Nakamura, Toshio,Kakinuma, Hiroyuki,Amada, Hideaki,Miyata, Noriyuki,Taniguchi, Kazuo,Koda, Ayumi,Sato, Masakazu
, p. 6209 - 6219 (2004)
Introduction of a piperazino group to the selective and potent 20-HETE synthase inhibitor 1 to obtain potential therapeutic agents with suitable water-solubility for injectable formulation is described. Improvement of the physical properties of pyrazole derivative 1, which we reported previously as a potent and selective 20-HETE synthase inhibitor (IC50 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).
