Adenosine a2b receptor agonists I, wherein R1 is an optionally substituted aryl or heteroaryl group; R2 is H or a halogen; R3 is hydroxy Me or alkyl substituted methylether, heterocyclic ring systems, or alkyl substituted amides; and n is 0 or 1 are prepd. as prodrugs treating diseases in mammals. Thus, II was prepd. and tested for its binding in cAMP assays on hA2b CHO cells (IC50 was 67 nM). Further, I may be employed for the treatment of diseases in mammals that are mediated by the A2B receptor including, but not limited to, septic shock, cystic fibrosis, impotence, diarrhea, and cardiac diseases Cardiac diseases include hyperplasia consequent to hypertension, arteriosclerosis, and heart attacks.
Preparation of adenosine a2b receptor agonists for use as prodrugs treating diseases in mammals
BARALDI, Pier Giovanni;BOREA, Pier Andrea;PRETI, Delia
2007
Abstract
Adenosine a2b receptor agonists I, wherein R1 is an optionally substituted aryl or heteroaryl group; R2 is H or a halogen; R3 is hydroxy Me or alkyl substituted methylether, heterocyclic ring systems, or alkyl substituted amides; and n is 0 or 1 are prepd. as prodrugs treating diseases in mammals. Thus, II was prepd. and tested for its binding in cAMP assays on hA2b CHO cells (IC50 was 67 nM). Further, I may be employed for the treatment of diseases in mammals that are mediated by the A2B receptor including, but not limited to, septic shock, cystic fibrosis, impotence, diarrhea, and cardiac diseases Cardiac diseases include hyperplasia consequent to hypertension, arteriosclerosis, and heart attacks.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
