A quantitative structure-activity relationship study on some series of potassium channel blockers.

Abstract

There has been an increasing interest in compounds that modulate potassium ion channels (K(+)-channels) since they can be developed as important therapeutic agents against ischemic heart diseases. Of the diverse family of K(+)-channels, the voltage-gated potassium channel Kv1.3 constitutes an attractive target for the selective suppression of effector memory T cells in autoimmune diseases. For the development of antiarrythmic drugs, the blockade of the rapidly activating delayed rectifier (I(Kr)) and slowly activating delayed rectifier (I(Ks)) potassium currents has been specifically studied. Since the discovery of I(Ks)-channel, its blockers have been particularly more studied. In this communication, we present QSAR studies on a few series of Kv1.3-channel blockers and a series of I(Ks)-channel blockers in order to provide some guidelines to the drug development.

• Authors: V S A Kumar Satuluri, Jyostna Seelam, S P Gupta
• Journal: Medicinal chemistry (Shariqah (United Arab Emirates)) (Med Chem) Vol. 5 Issue 1 Pg. 87-92 (Jan 2009) ISSN: 1573-4064 [Print] Netherlands
• PMID: 19149654 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Potassium Channel Blockers
• Potassium Channels

Topics

• Binding Sites
• Molecular Structure
• Potassium Channel Blockers (chemistry, pharmacology)
• Potassium Channels (metabolism)
• Quantitative Structure-Activity Relationship
• Stereoisomerism