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Note | Regular issue | Vol 81, No. 11, 2010, pp.2635-2647
Published online, 28th September, 2010
DOI: 10.3987/COM-10-12057
Synthesis and Evaluation of Phosphodiesterase IV Inhibitory Potency of Isocarbostyril Derivatives of Naturally Occurring Isocoumarins, Scoparines A and B

Kumiko Taguchi, Koichi Kobayashi, Keiko Ishida, Katsuo Kamata, and Toshio Honda*

*Faculty of Pharmaceutical Sciences, Hoshi University, 2-4-41 Ebara, Shinagawa-ku, Tokyo 142-8501, Japan

Abstract

Eight isocarbostyril derivatives bearing n-propyl substituent at the 3-position were prepared from the naturally occurring isocoumarins, scoparines A and B. Their phosphodiesterase IV (PD-4) inhibitory potency were evaluated by the vascular relaxation response in the mesenteric artery. Eight derivatives showed vascular relaxation response, probably relating with PD-4 inhibitory. However, these responses were weaker than the known PD-4 inhibitor (Ro201724).