9-Benzyladenines:  Potent and Selective cAMP Phosphodiesterase Inhibitors

• Published in: Journal of medicinal chemistry Vol. 40; no. 12; pp. 1768 - 1770
• Main Authors: Bourguignon, Jean-Jacques, Désaubry, Laurent, Raboisson, Pierre, Wermuth, Camille-Georges, Lugnier, Claire
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 06.06.1997; Amer Chemical Soc
• Subjects: 3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors; Adenine - analogs & derivatives; Adenine - chemical synthesis; Adenine - chemistry; Adenine - pharmacology; Adenosine Deaminase Inhibitors; Anticonvulsants; Biological and medical sciences; Chemistry, Medicinal; Cyclic AMP - pharmacology; Cyclic GMP - metabolism; Enzyme Inhibitors - chemical synthesis; Enzyme Inhibitors - chemistry; Enzyme Inhibitors - pharmacology; Isoenzymes - antagonists & inhibitors; Life Sciences & Biomedicine; Medical sciences; Miscellaneous; Muscle, Smooth, Vascular - enzymology; Neuropharmacology; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Purines - chemistry; Purines - pharmacology; Science & Technology; Structure-Activity Relationship; CYCLIC-NUCLEOTIDE PHOSPHODIESTERASES; ANTICONVULSANT ACTIVITY; ANALOGS; Purine derivatives; 3',5'-Cyclic-nucleotide phosphodiesterase; Structure activity relation; Enzyme; Isozyme; Enzyme inhibitor; Hydrolases; Esterases; Phosphoric diester hydrolases; In vitro
• ISSN: 0022-2623; 1520-4804
• DOI: 10.1021/jm960827x

In this paper, we report the behavior of BWA78U and some of its analogues toward PDE3 and PDE4 preparations. It appears that some of these compounds exhibit potent phosphodiesterase inhibition properties with high selectivity toward PDE4.