SYNTHESIS AND EVALUATION OF PHOSPHODIESTERASE IV INHIBITORY POTENCY OF ISOCARBOSTYRIL DERIVATIVES OF NATURALLY OCCURRING ISOCOUMARINS, SCOPARTNES A AND B

摘要

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).