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ChemInform Abstract: Stereospecificity of Myofibrillar Calcium Sensitivity and PDE Inhibition in Cardiotonic Thiadiazinones.

✍ Scribed by G. NADLER; I. DELIMOGE; P. LAHOURATATE; I. LEGER; M. MORVAN; R. G. ZIMMERMANN

Publisher: John Wiley and Sons
Year: 2010
Weight: 31 KB
Volume: 28
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.199708152

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✦ Synopsis

Stereospecificity of Myofibrillar Calcium Sensitivity and PDE Inhibition in Cardiotonic Thiadiazinones.

-Enantiomers of the title compounds (V)-(VII) are prepared by stereoselective synthesis, cf. (R)-(+)-(V), or by standard resolution procedures using (-)-menthyl chloroformate or a chiral hydrazine derivative. In the thiadiazine series the (R)-configuration is essential for the Ca-sensitizing effect whereas the (S)-configuration supports the highest inhibition of PDE (phosphodiesterase) activity.

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