Imidazole derivatives as new potent and selective 20-HETE synthase inhibitors.

Bioorg Med Chem Lett

Medicinal Research Laboratories, Taisho Pharmaceutical Co., Ltd, 1-403 330-8530, Yoshino-cho, Ohmiya, Saitama, Japan.

Published: January 2004

In a previous paper, we reported that an imidazole derivative 1 exhibited a potent inhibitory activity of 20-HETE synthase (1; IC(50) value of 5.7 nM), but this compound also exhibited little selectivity for cytochrome P450s (CYPs). We examined some derivatives of imidazole 1 which had an amino group on the side chain, and found that a dimethylaminohexyloxy derivative (3g; IC(50) value of 8.8 nM) showed potent and selective inhibitory activity.

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http://dx.doi.org/10.1016/j.bmcl.2003.11.005DOI Listing

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