77522-31-7Relevant academic research and scientific papers
Mesoionic Xanthine Analogues: Phosphodiesterase Inhibitory and Hypotensive Activity
Glennon, Richard A.,Rogers, Michael E.,Smith, J. Doyle,El-Said, M. K.,Egle, John L.
, p. 658 - 661 (2007/10/02)
Several mesoionic thiazolopyrimidines and mesoionic 1,3,4-thiadiazolopyrimidines were evaluated as inhibitors of cyclic-AMP phosphodiesterase.While small alkyl substituents at the 6 position have no significant effect on activity, phenyl and benzyl substituents enhance activity.Mesoionic structures such as 1 (R2 = H; R8 = Et) possess 20 to 40 times activity of theophylline when the R6 substituent is phenyl or 4-chlorobenzyl.Methyl and ethyl substitution at the 2 position essentially abolishes activity.Although plagued by solubility problems, several of the mesoionic derivatives were found to display weak hypotensive effects in vivo.
