期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 12, 期 23, 页码 6209-6219出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2004.08.047
关键词
20-HETE; pyrazole
Improvement of the physical properties of pyrazole derivative 1, which we reported previously as a potent and selective 20-HETE synthase inhibitor (IC50 5.7nM), is described. Introduction of a sufficient substituted-amino group on the side chain enhanced the water-solubility of 1 (0.014mg/mL at pH6.8). Among the products, 2-piperazinoethoxy derivatives 3e and 6b showed solubility suitable for injection and potent inhibitory activity toward 20-HETE synthase (IC50 21.2 and 14.0 nM, respectively). (C) 2004 Elsevier Ltd. All rights reserved.
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