AI Article Synopsis
- Novel pyrazolopyridopyridazine derivatives have been developed, showing potential as strong PDE5 inhibitors.
- Compound 6 has demonstrated greater potency and selectivity compared to sildenafil, performing similarly in various testing models.
- The enhanced selectivity of compound 6 suggests it may lead to fewer side effects for humans undergoing treatment for erectile dysfunction.
Article 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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| http://dx.doi.org/10.1021/jm0256068 | DOI Listing |
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