2. Academic Validation
  3. Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction

Substituted pyrazolopyridopyridazines as orally bioavailable potent and selective PDE5 inhibitors: potential agents for treatment of erectile dysfunction

  • J Med Chem. 2003 Feb 13;46(4):457-60. doi: 10.1021/jm0256068.
Guixue Yu 1,  Helen Mason,  Ximao Wu,  Jian Wang,  Saeho Chong,  Bruce Beyer,  Andrew Henwood,  Ronald Pongrac,  Laurie Seliger,  Bin He,  Diane Normandin,  Pam Ferrer,  Rongan Zhang,  Leonard Adam,  William G Humphrey,  John Krupinski,  John E Macor
Affiliations

Affiliation

  • 1 Discovery Chemistry, Drug Metabolism and Pharmacokinetics, Drug Safety, and Metabolic and Cardiovascular Drug Discovery, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543-5400, USA. guixue.yu@bms.com
PMID: 12570368 DOI: 10.1021/jm0256068
Abstract

Novel pyrazolopyridopyridazine derivatives have been prepared as potent and selective PDE5 inhibitors. Compound 6 has been identified as a more potent and selective PDE5 Inhibitor than sildenafil (1). It is as efficacious as sildenafil in in vitro and in vivo PDE5 inhibition models, and it is orally bioavailable in rats and dogs. The superior isozyme selectivity of 6 is expected to exert less adverse effects in humans when used for erectile dysfunction treatment.

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