Structure-Activity Relationships of KATP Channel Openers

Author(s): Raimund Mannhold.

Journal Name: Current Topics in Medicinal Chemistry

Volume 6 , Issue 10 , 2006

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Abstract:

Given their many physiological functions, KATP channels represent promising drug targets. Sulfonylureas like glibenclamide block KATP channels; they are used in the therapy of type 2 diabetes. Openers of KATP channels (KCOs) e.g. relax smooth muscle and induce hypotension. KCOs are chemically heterogeneous and include as different classes as the benzopyrans, cyanoguanidines, thioformamides, thiadiazines and pyridyl nitrates. Examples for new chemical entities more recently developed as KCOs include cyclobutenediones, dihydropyridine related structures, and tertiary carbinols. Structure-activity relationships of the main chemical classes of KCOs are discussed.

Keywords: KATP channel openers (KCOs), structure-activity relationships, benzopyrans, cyanoguanidines, thioformamides, diazoxide, cyclobutenediones, dihydropyridine related structures, tertiary carbinols

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Article Details

VOLUME: 6
ISSUE: 10
Year: 2006
Page: [1031 - 1047]
Pages: 17
DOI: 10.2174/156802606777323647
Price: $58

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