2. Academic Validation
  3. Design, synthesis and biological activity of beta-carboline-based type-5 phosphodiesterase inhibitors

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.
Graham N Maw 1,  Charlotte M N Allerton,  Eugene Gbekor,  William A Million
Affiliations

Affiliation

  • 1 Department of Discovery Chemistry, Pfizer Global Research and Development, Sandwich Laboratories (IPC351), Ramsgate Road, Sandwich, Kent, CT13 9NJ, UK. [email protected]
PMID: 12668004 DOI: 10.1016/s0960-894x(03)00159-8
Abstract

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.

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