Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors
- Bioorg Med Chem Lett. 2003 Apr 17;13(8):1425-8. doi: 10.1016/s0960-894x(03)00159-8.
- 1. Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich Laboratories (IPC351), Ramsgate Road, Sandwich, Kent, CT13 9NJ, UK. [email protected]
The SAR of a series of beta-carboline derived type 5 phosphodiesterase inhibitors has been explored and we have discovered compounds with excellent levels of PDE5 potency and selectivity over PDE6. However, the series exhibits low levels of selectivity over PDE11, a phosphodiesterase with unknown function.