Nucleosides I, wherein Ar is aryl; R and R1 are independently H, alkyl, aryl, heteroaryl, alkenyl, cyclo-alkenyl, cycloalkyl, alkynyl; R and R1 together with the nitrogen atom to which they are attached form an optionally substituted satd. or unsatd. 3 to 20-membered ring system having a single ring or multiple condensed rings which may optionally contain 1 to 4 addnl. heteroatoms selected from O, S and N; provided that R and R1 are not both H when Ar is Ph and the sulfonamide group is located at the 4-position; or, either R or R1 is not pyridin-2-yl, pyrimidin-2-yl or 5-methyl-isoxazol-3-yl when the other is hydrogen, Ar is Ph and the sulfonamide group is located at the 4-position; were prepd. and tested as adenosine A3 receptor agonists. Accordingly, nucleosides I may be employed for treatment of behavioral depression, cerebral ischemia, hypotension, chem. induced seizures, inflammatory diseases, asthma, and cancer diseases expressing the adenosine A3 receptor. Thus, nucleoside II was prepd. and tested as adenosine A3 receptor agonist.
Preparation of nucleosides as adenosine A3 receptor agonists
BARALDI, Pier Giovanni;BOREA, Pier Andrea
2009
Abstract
Nucleosides I, wherein Ar is aryl; R and R1 are independently H, alkyl, aryl, heteroaryl, alkenyl, cyclo-alkenyl, cycloalkyl, alkynyl; R and R1 together with the nitrogen atom to which they are attached form an optionally substituted satd. or unsatd. 3 to 20-membered ring system having a single ring or multiple condensed rings which may optionally contain 1 to 4 addnl. heteroatoms selected from O, S and N; provided that R and R1 are not both H when Ar is Ph and the sulfonamide group is located at the 4-position; or, either R or R1 is not pyridin-2-yl, pyrimidin-2-yl or 5-methyl-isoxazol-3-yl when the other is hydrogen, Ar is Ph and the sulfonamide group is located at the 4-position; were prepd. and tested as adenosine A3 receptor agonists. Accordingly, nucleosides I may be employed for treatment of behavioral depression, cerebral ischemia, hypotension, chem. induced seizures, inflammatory diseases, asthma, and cancer diseases expressing the adenosine A3 receptor. Thus, nucleoside II was prepd. and tested as adenosine A3 receptor agonist.I documenti in SFERA sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
