3-Thio-quinolinone maxi-K openers for the treatment of erectile dysfunction

Bioorg Med Chem Lett. 2004 Oct 18;14(20):5089-93. doi: 10.1016/j.bmcl.2004.07.080.

Abstract

A series of Maxi-K openers for the treatment of erectile dysfunction based on the 3-thio-quinolinone core is described. Significant levels of channel opening (up to 550% of control) are seen in transfected oocytes. Functional activity in rabbit corpus cavernosum tissue strips confirms the potential to effect therapy for ED, the effect being maximal for the 3-amino-2-hydroxy thiol side chain.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Erectile Dysfunction / drug therapy
  • Humans
  • In Vitro Techniques
  • Ion Channel Gating*
  • Large-Conductance Calcium-Activated Potassium Channels
  • Male
  • Muscle Relaxation / drug effects
  • Muscle Relaxation / physiology
  • Muscle, Smooth, Vascular / drug effects
  • Oocytes / drug effects
  • Oocytes / physiology
  • Patch-Clamp Techniques
  • Penile Erection / drug effects*
  • Penile Erection / physiology
  • Penis / blood supply
  • Potassium Channels, Calcium-Activated / drug effects*
  • Quinolines / chemical synthesis*
  • Quinolines / chemistry
  • Quinolines / pharmacology
  • Rabbits
  • Structure-Activity Relationship
  • Sulfides / chemical synthesis*
  • Sulfides / chemistry
  • Sulfides / pharmacology
  • Vasodilator Agents / chemical synthesis*
  • Vasodilator Agents / chemistry
  • Vasodilator Agents / pharmacology

Substances

  • Large-Conductance Calcium-Activated Potassium Channels
  • Potassium Channels, Calcium-Activated
  • Quinolines
  • Sulfides
  • Vasodilator Agents