A Quantitative Structure-Activity Relationship Study on Some Series of Potassium Channel Blockers

V.   S.A.   Kumar Satuluri; Jyostna      Seelam; S.   P.   Gupta

doi:10.2174/157340609787049244

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 (IKr) and slowly activating delayed rectifier (IKs) potassium currents has been specifically studied. Since the discovery of IKs-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 IKs-channel blockers in order to provide some guidelines to the drug development.

Keywords: Quantitative structure-activity relationship study, potassium channel blockers, Kv1.3-channel blockers, IKschannel blockers, khellinone analogs, chromanols

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