Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction

Zhihua Sui; Jihua Guan; Mark J Macielag; Weiqin Jiang; Suying Zhang; Yuhong Qiu; Patricia Kraft; Sheela Bhattacharjee; T Matthew John; Donna Haynes-Johnson; Joanna Clancy

doi:10.1021/jm025545d

Pyrimidinylpyrroloquinolones as highly potent and selective PDE5 inhibitors for treatment of erectile dysfunction

J Med Chem. 2002 Sep 12;45(19):4094-6. doi: 10.1021/jm025545d.

Authors

Zhihua Sui¹, Jihua Guan, Mark J Macielag, Weiqin Jiang, Suying Zhang, Yuhong Qiu, Patricia Kraft, Sheela Bhattacharjee, T Matthew John, Donna Haynes-Johnson, Joanna Clancy

Affiliation

¹ Johnson & Johnson Pharmaceutical Research & Development, Drug Discovery, 1000 Route 202, Raritan, NJ 08869, USA.

PMID: 12213052
DOI: 10.1021/jm025545d

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.

MeSH terms

3',5'-Cyclic-GMP Phosphodiesterases / antagonists & inhibitors*
Administration, Oral
Animals
Biological Availability
Cyclic Nucleotide Phosphodiesterases, Type 5
Dogs
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology
Erectile Dysfunction / drug therapy*
Male
Quinolones / chemical synthesis*
Quinolones / chemistry
Quinolones / pharmacology
Rats
Structure-Activity Relationship

Substances

Enzyme Inhibitors
Quinolones
3',5'-Cyclic-GMP Phosphodiesterases
Cyclic Nucleotide Phosphodiesterases, Type 5
Pde5a protein, rat