The discovery of potent, selective, and orally bioavailable PDE9 inhibitors as potential hypoglycemic agents.
Starting from a non-selective pyrazolo-pyrimidone lead, the sequential use of parallel medicinal chemistry and directed synthesis led to the discovery of potent, highly selective, and orally bioavailable PDE9 inhibitors. The availability of these tools allowed for a thorough evaluation of the therapeutic potential of PDE9 inhibition.
Deninno
Michael P
MP
Pfizer Global Research and Development, Groton Laboratories, Groton, CT 06340, USA.
Andrews
Melissa
M
Bell
Andrew S
AS
Chen
Yue
Y
Eller-Zarbo
Cynthia
C
Eshelby
Nan
N
Etienne
John B
JB
Moore
Dianna E
DE
Palmer
Michael J
MJ
Visser
Michael S
MS
Yu
Li J
LJ
Zavadoski
William J
WJ
Michael Gibbs
E
E