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Recent Developments in the Chemistry of Potassium Channel Activators: The Cromakalim Analogs

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Potassium channels play a crucial role in controlling the cell membrane potential. Among the different varieties of K+ channels, the ATP-sensitive potassium channels (KATP channels) have been characterized in numerous cell types, such as skeletal and smooth muscle cells, endocrine cells, cardiac cells and central neurons. Several molecules are known to activate KATP channels and have been named “potassium channel openers” (PCOs). Such compounds may have a wide therapeutic potential and a few drugs are currently used as antihypertensive agents. Different chemical series of PCOs have been explored. This heterogeneous group of organic compounds comprises the benzopyran series including potent vasorelaxant drugs, such as cromakalim. The latter compound, a typical example of potassium channel opener, exerts its biological effect by activating KATP channels. This review presents recent developments in the chemistry of cromakalim analoges and reports chemical aspects governing their potency and tissue selectivity.

Keywords: benzopyran; cromakalim; katp channel; potassium channel openers

Document Type: Review Article


Affiliations: Department of Medicinal Chemistry, Universite de Liege, 1 av. de l'Hopital, tour 4 (+5) Sart- Tilman, B-4000 Liege, Belgium.

Publication date: May 1, 2004

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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