Synthesis and evaluation of potent and selective c-GMP phosphodiesterase inhibitors.
Syntheses and structure-activity relationships (SAR) of cGMP selective phosphodiesterase inhibitors are discussed. Potent and selective inhibitors are produced when the C-2 position of tetracyclic guanine 1 is substituted with alkyl chains containing six carbon atoms.
Ho
G D
GD
Schering-Plough Research Institute, Kenilworth, NJ 07033, USA.
Silverman
L
L
Bercovici
A
A
Puchalski
C
C
Tulshian
D
D
Xia
Y
Y
Czarniecki
M
M
Green
M
M
Cleven
R
R
Zhang
H
H
Fawzi
A
A
D015106:3',5'-Cyclic-GMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D004353:Drug Evaluation, Preclinical; D006147:Guanine / Q000737:chemistry; D007093:Imidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007527:Isoenzymes; D010726:Phosphodiesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D011687:Purines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship