A QSAR study on a series of simplified digitalis-like compounds acting on Na<sup>+</sup>,K<sup>+</sup>-ATPase
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Title |
A QSAR study on a series of simplified digitalis-like compounds acting on Na+,K+-ATPase
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Creator |
Seelam, Jyostna
Satuluri, V S A Kumar Gupta, S P Anwer, Zaihra |
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Subject |
Quantitative structure-activity relationship
Na+ K+-ATPase inhibitors Perhydroindenes Cardiotonic agents |
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Description |
158-163
Among the cardiotonics (agents against congestive heart failure), the most important group is of the digitalis cardiac glycosides, but since these compounds suffer from a low therapeutic index, attention has been paid to investigating safer cardiotonic agents through the inhibition of Na+,K+-ATPase, the mechanism by which the digitalis cardiac glycosides elicit their action. Recently, a series of perhydroindenes were studied for their Na+,K+-ATPase inhibition activity. We report here a QSAR study on them to investigate the physicochemical and structural properties of the molecules that govern their activity in order to rationalize the structural modification to have more potent drugs. A multiple regression analysis reveals a significant correlation between the Na+,K+-ATPase inhibition activity of the compounds and Kier’s first order valence molecular connectivity index of their R5-substituents and some indicator parameters, suggesting that the R5-substituents of the compounds containing atoms with low valence and high saturation and the R1-substituents having =N−O− moiety will be conducive to the activity. |
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Date |
2011-06-16T09:10:46Z
2011-06-16T09:10:46Z 2011-06 |
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Type |
Article
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Identifier |
0975-0959 (Online); 0301-1208 (Print)
http://hdl.handle.net/123456789/11983 |
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Language |
en_US
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Rights |
CC Attribution-Noncommercial-No Derivative Works 2.5 India
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Publisher |
NISCAIR-CSIR, India
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Source |
IJBB Vol.48(3) [June 2011]
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