Quantitative structure-inotropy relationship applied to substituted grayanotoxins.

N Shirai; J Sakakibara; T Kaiya; S Kobayashi; Y Hotta; K Takeya

doi:10.1021/jm00360a012

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Quantitative structure-inotropy relationship applied to substituted grayanotoxins.

N Shirai·J Sakakibara·T Kaiya·S Kobayashi·Y Hotta·K Takeya

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Abstract

Nine 14 beta-O-acylated grayanotoxins were synthesized by ozonolysis of 14,16-alkylidenegrayanotoxin III. The correlation between positive inotropic potency (PIE) in guinea pigs and physicochemical parameters (Vw, Mw, and Rm50) in 14 14-substituted grayanotoxins were quantitatively analyzed. It became clear that a parabolic relation existed between the bulkiness of the 14-substituents and PIE and that some electronic factor and the hydrophilic-hydrophobic balance would be related to the development of PIE.

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Animals Cardiotonic Agents Diterpenes Guinea Pigs Lethal Dose 50 Male Mathematics Myocardial Contraction Ozone Stimulation, Chemical Structure-Activity Relationship Journal Article Research Support, Non-U.S. Gov't

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N Shirai, J Sakakibara, T Kaiya, S Kobayashi, Y Hotta, K Takeya. 1983. Quantitative structure-inotropy relationship applied to substituted grayanotoxins.. https://doi.org/10.1021/jm00360a012

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