title: Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction.
abstract: 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.
authors.affiliation: Johnson & Johnson Pharmaceutical Research & Development, Drug Discovery, 1000 Route 202, Raritan, NJ 08869, USA.
authors.forename: Zhihua
authors.initials: Z
authors.lastname: Sui
authors.forename: Jihua
authors.initials: J
authors.lastname: Guan
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Macielag
authors.forename: Weiqin
authors.initials: W
authors.lastname: Jiang
authors.forename: Suying
authors.initials: S
authors.lastname: Zhang
authors.forename: Yuhong
authors.initials: Y
authors.lastname: Qiu
authors.forename: Patricia
authors.initials: P
authors.lastname: Kraft
authors.forename: Sheela
authors.initials: S
authors.lastname: Bhattacharjee
authors.forename: T Matthew
authors.initials: TM
authors.lastname: John
authors.forename: Donna
authors.initials: D
authors.lastname: Haynes-Johnson
authors.forename: Joanna
authors.initials: J
authors.lastname: Clancy
mesh_terms: 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
chemical_list: D004791:Enzyme Inhibitors; D015363:Quinolones; D015106:3',5'-Cyclic-GMP Phosphodiesterases; D054706:Cyclic Nucleotide Phosphodiesterases, Type 5; C517384:Pde5a protein, rat