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Cardioselective anti-ischemic ATP-sensitive potassium channel (KATP) openers: benzopyranyl indoline and indole analogues by Sunkyung Lee; Kyu Yang Yi; Soo-Kyung Kim; Jeehee Suh; Nak Jeong Kim; Sung-eun Yoo; Byung Ho Lee; Ho Won Seo; Sun-Ok Kim; Hong Lim is a Chemistry article available to read on EtoBox.
What is Cardioselective anti-ischemic ATP-sensitive potassium channel (KATP) openers: benzopyranyl indoline and indole analogues about?
This paper describes the design, syntheses, and biological evaluations of novel ATP-sensitive potassium channel (K(ATP)) openers, benzopyranyl indoline and indole derivatives. Among those, two enantiomers of indoline-2-carboxylic ethyl esters (14, 18) showed the best cardioprotective activities both in vitro and in vivo, while their vasorelaxation potencies were very low (concentration for 50% inhibition of vasorelaxation >30 microM). The cardioprotective effect of 14 was completely reversed by 5-hydroxydecanoate, a selective mitochondrial K(ATP) blocker, indicating its provable protective mechanism through the mitochondrial K(ATP) opening. In addition, we performed conformational analyses using 2D-NMR, X-ray crystallography and molecular modeling to study the structure-activity relationships in this series of compounds.
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- Author
- Sunkyung Lee; Kyu Yang Yi; Soo-Kyung Kim; Jeehee Suh; Nak Jeong Kim; Sung-eun Yoo; Byung Ho Lee; Ho Won Seo; Sun-Ok Kim; Hong Lim
- Publisher
- Elsevier Science; Elsevier ; Elsevier BV (ISSN 0223-5234)
- Published
- 2003
- Language
- EN
- Field
- Chemistry (Physical Sciences)