Abstract
ATP-Sensitive potassium channel openers (KATPCOs) are a group of compounds with a broad spectrum of potential therapeutic applications, as they constitute efficient tools for dampening cell excitability. Interest in the KATPCOs was triggered in the early 1980s by the discovery of the benzopyran-based structure cromakalim (CRK), which is a powerful smooth muscle relaxant. CRK can be considered the archetype of KATPCOs and is by far the most mimicked structure. In many structure-activity studies various substitutions have been made at the different positions of the benzopyran ring permitting the optimal activity to be correlated with a specific set of structural characteristics and stereochemical features of the molecule. Thus, many potent benzopyran derivatives have been identified. The benzopyran nucleus itself has also been modified in both the aromatic ring and in the pyran moiety. The intention of this review is to bring together all the different structural classes of KATPCOs arising from the replacement of CRK benzopyran-based structure with various ring systems; design, structure-activity relationship, and synthesis will be given.
Keywords: KATP channels, cromakalim analogues, thienopyrans, pyranopyridines, benzoxepines, indanes, benzothiopyrans, quinolines, naphthalenes, benzoxazines
Current Topics in Medicinal Chemistry
Title: From Cromakalim to Different Structural Classes of KATP Channel Openers
Volume: 6 Issue: 10
Author(s): Violetta Cecchetti, Oriana Tabarrini and Stefano Sabatini
Affiliation:
Keywords: KATP channels, cromakalim analogues, thienopyrans, pyranopyridines, benzoxepines, indanes, benzothiopyrans, quinolines, naphthalenes, benzoxazines
Abstract: ATP-Sensitive potassium channel openers (KATPCOs) are a group of compounds with a broad spectrum of potential therapeutic applications, as they constitute efficient tools for dampening cell excitability. Interest in the KATPCOs was triggered in the early 1980s by the discovery of the benzopyran-based structure cromakalim (CRK), which is a powerful smooth muscle relaxant. CRK can be considered the archetype of KATPCOs and is by far the most mimicked structure. In many structure-activity studies various substitutions have been made at the different positions of the benzopyran ring permitting the optimal activity to be correlated with a specific set of structural characteristics and stereochemical features of the molecule. Thus, many potent benzopyran derivatives have been identified. The benzopyran nucleus itself has also been modified in both the aromatic ring and in the pyran moiety. The intention of this review is to bring together all the different structural classes of KATPCOs arising from the replacement of CRK benzopyran-based structure with various ring systems; design, structure-activity relationship, and synthesis will be given.
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Cite this article as:
Cecchetti Violetta, Tabarrini Oriana and Sabatini Stefano, From Cromakalim to Different Structural Classes of KATP Channel Openers, Current Topics in Medicinal Chemistry 2006; 6 (10) . https://dx.doi.org/10.2174/156802606777323683
DOI https://dx.doi.org/10.2174/156802606777323683 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
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