Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues.
The in vitro evaluation of a series of saturated prostaglandins revealed that compounds with omega chain aromatic rings retain nanomolar potency for the human prostaglandin F receptor (hFP receptor), exemplified by compound 8. In contrast, the double bonds are required for activity in the series with an acyclic omega chain as in PGF2alpha.
deLong
M A
MA
Procter & Gamble Pharmaceuticals, Mason, OH 45040, USA. delong.ma@pg.com
Amburgey
J
J
Taylor
C
C
Wos
J A
JA
Soper
D L
DL
Wang
Y
Y
Hicks
R
R
D006801:Humans; D007700:Kinetics; D008961:Models, Structural; D008968:Molecular Conformation; D011453:Prostaglandins / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism*; D011982:Receptors, Prostaglandin / Q000378:metabolism*; D013329:Structure-Activity Relationship
D011453:Prostaglandins; D011982:Receptors, Prostaglandin; C034671:prostaglandin F2alpha receptor