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Synthesis, local anaesthetic and antiarrhythmic activities of N-alkyl derivatives of proline anilides

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Kalinin, D
Pantsurkin, Vladimir
Syropyatov, Boris
Kalinina, S
Rudakova, Irina
Vakhrin, Mikhail
Dolzhenko, Anton
Date
2013
Type
Journal Article

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Kalinin, Dmitrii and Pantsurkin, Vladimir and Syropyatov, Boris and Kalinina, Svetlana and Rudakova, Irina and Vakhrin, Mikhail and Dolzhenko, Anton. 2013. Synthesis, local anaesthetic and antiarrhythmic activities of N-alkyl derivatives of proline anilides. European Journal of Medicinal Chemistry 63: pp. 144-150.
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European Journal of Medicinal Chemistry
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NOTICE: this is the author’s version of a work that was accepted forpublication in the European Journal of Medicinal Chemistry. Changesresulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in the European Journal of Medicinal Chemistry, Vol. 63 (2013). DOI: 10.1016/j.ejmech.2013.02.003

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Abstract

We describe here the design, synthesis and evaluation of in vivo local anaesthetic and antiarrhythmic activities of a series of N-alkylproline anilides. Most of the compounds demonstrated surface anaesthetic activity higher than that of lidocaine, ropivacaine and bupivacaine. We established that the local anaesthetic activity was sensitive to structural variations in the substitution pattern at the aromatic ring and the type of alkyl group at the proline nitrogen atom. Some of the prepared N-alkylproline anilides possessed significant antiarrhythmic activity with higher therapeutic indexes than the reference drugs.