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

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Kalinin DV,Pantsurkin VI,Syropyatov BY,Kalinina SA,Rudakova IP,Vakhrin MI,Dolzhenko AV

doi

10.1016/j.ejmech.2013.02.003

subject

Has Abstract

pub_date

2013-05-01 00:00:00

pages

144-50

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(13)00089-5

journal_volume

63

pub_type

杂志文章

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