The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A3 receptor.
Using a combination of parallel and directed synthesis, the discovery of a highly potent and selective series of adenosine A3 agonists was achieved. High aqueous solubility, required for the intended parenteral route of administration, was achieved by the presence of one or two basic amine functional groups.
DeNinno
Michael P
MP
Pfizer Global Research and Development, Groton/NewLondon Laboratories, Groton, CT 06340, USA. michael.p.deninno@pfizer.com
Masamune
Hiroko
H
Chenard
Lois K
LK
DiRico
Kenneth J
KJ
Eller
Cynthia
C
Etienne
John B
JB
Tickner
Jeanene E
JE
Kennedy
Scott P
SP
Knight
Delvin R
DR
Kong
Jimmy
J
Oleynek
Joseph J
JJ
Tracey
W Ross
WR
Hill
Roger J
RJ
D000241:Adenosine / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology*; D058909:Adenosine A3 Receptor Agonists; D006801:Humans; D008968:Molecular Conformation; D012995:Solubility; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D014867:Water / Q000737:chemistry
D058909:Adenosine A3 Receptor Agonists; D014867:Water; D000241:Adenosine