Introduction of a conformational switching element on a pyrrolidine ring. Synthesis and evaluation of methyl (R,R)-(.+-.)-3-acetyl-4-[3- (cyclopentyloxy)-4-methoxyphenyl]-3- methyl-1-pyrrolidinecarboxylate, a potent and selective inhibitor of cAMP-specific phosphodiesterase

• Published in: Journal of medicinal chemistry Vol. 38; no. 26; pp. 4972 - 4975
• Main Authors: Stafford, Jeffrey A, Veal, James M, Feldman, Paul L, Valvano, Nicole L, Baer, Philip G, Brackeen, Marcus F, Brawley, E. Sloan, Connolly, Kevin M, Domanico, Paul L
• Format: Journal Article
• Language: English
• Published: Washington, DC American Chemical Society 01-12-1995
• Subjects: 3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors; 3',5'-Cyclic-AMP Phosphodiesterases - metabolism; Animals; Biological and medical sciences; Bones, joints and connective tissue. Antiinflammatory agents; Cattle; Humans; Kinetics; Magnetic Resonance Spectroscopy; Medical sciences; Models, Molecular; Molecular Conformation; Pharmacology. Drug treatments; Phosphodiesterase Inhibitors - chemical synthesis; Phosphodiesterase Inhibitors - chemistry; Phosphodiesterase Inhibitors - pharmacology; Pyrrolidines - chemical synthesis; Pyrrolidines - chemistry; Pyrrolidines - pharmacology; Pyrrolidinones - pharmacology; Rolipram; Structure-Activity Relationship; 3',5'-Cyclic-nucleotide phosphodiesterase; Enzyme; Nitrogen heterocycle; Isozyme; Enzyme inhibitor; Esterases; Phosphoric diester hydrolases; Pyrrolidine derivatives; Structure activity relation; Trans stereoisomer; Racemate; Hydrolases; Chemical synthesis; Cyclopentane derivatives; Conformation
• ISSN: 0022-2623; 1520-4804
• DOI: 10.1021/jm00026a003