Abstract

ATP-sensitive potassium channels (KATP-channels) provide a vital link between cellular metabolism and electrical activity and the opening of these channels leads to an efflux of K+ ions from the cell with a simultaneous transmembrane hyperpolarization that restricts the entry of ca2+ ions through voltage-gated (L-type) calcium channels and inhibits intracellular ca2+ ion release, thereby damping cellular excitability. Thus, the compound that can act as KATPchannel opener may possess a broad spectrum of potential therapeutic applications. In order to find highly potent KATPchannel openers, a quantitative structure-activity relationship (QSAR) study is made on some recently studied series of them, which provides the rationale to structure modification for the better efficacy and throws light on the mechanism of their action. The series of compounds are comprised of cromakalim analogs, 4-(N-aryl)-substituted benzopyran derivatives and 1,4-benzothiazine derivatives, respectively.

Keywords: QSAR study, Cromakalim analogs, 4-(N-aryl)-substituted benzopyran derivatives, 1,4-benzothiazine derivatives, KATP-channel openers, ATP-sensitive potassium channel openers