Cyclic AMP phosphodiesterase 4 isoenzyme inhibitory activity of (R)- and (S)-isomer of 7-methyl- or 8-alkyl-4,5,7,8-tetrahydroimidazo[2,1-i]- purin-5-one.
We investigated the structure-activity relationship of the (R)- and (S)-isomer of 7-methyl- and 8-alkyl-tetrahydroimidazo[2,1-i]purines for phosphodiesterase 4 (PDE4) inhibitors. (S)-8-Isopropyl-3,4-dipropyl-imizazo[2,1-i]purine (S)-2c exhibited both potent and selective PDE4 inhibitory activity.
Suzuki
Hirokazu
H
Department of Synthetic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University, Ho-3 Kanagawa-machi, Kanazawa, Japan. h-suzuki@hokuriku-u.ac.jp
Nomura
Masaaki
M
Miyamoto
Ken-ichi
K
Sawanishi
Hiroyuki
H
Yamamoto
Kenji
K
D015105:3',5'-Cyclic-AMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry*; D007527:Isoenzymes / Q000037:antagonists & inhibitors; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry*; D011687:Purines / Q000138:chemical synthesis / Q000737:chemistry*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D007093:Imidazoles; D007527:Isoenzymes; D010726:Phosphodiesterase Inhibitors; D011687:Purines; D015105:3',5'-Cyclic-AMP Phosphodiesterases; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4