Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction.
A series of N-pyrimidinylpyrroloquinolones were discovered as extremely potent and selective PDE5 inhibitors. Representative compounds demonstrated in vivo efficacy in dog erectile dysfunction models and are orally bioavailable.
Sui
Zhihua
Z
Johnson & Johnson Pharmaceutical Research & Development, Drug Discovery, 1000 Route 202, Raritan, NJ 08869, USA.
Guan
Jihua
J
Macielag
Mark J
MJ
Jiang
Weiqin
W
Zhang
Suying
S
Qiu
Yuhong
Y
Kraft
Patricia
P
Bhattacharjee
Sheela
S
John
T Matthew
TM
Haynes-Johnson
Donna
D
Clancy
Joanna
J
D015106:3',5'-Cyclic-GMP Phosphodiesterases / Q000037:antagonists & inhibitors*; D000284:Administration, Oral; D000818:Animals; D001682:Biological Availability; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5; D004285:Dogs; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007172:Erectile Dysfunction / Q000188:drug therapy*; D008297:Male; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D013329:Structure-Activity Relationship
D004791:Enzyme Inhibitors; D015363:Quinolones; D015106:3',5'-Cyclic-GMP Phosphodiesterases; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5; C517384:Pde5a protein, rat