TY - JOUR
T1 - Synthesis, local anaesthetic and antiarrhythmic activities of N-alkyl derivatives of proline anilides
AU - Kalinin, Dmitrii V
AU - Pantsurkin, Vladimir I
AU - Syropyatov, Boris Ya
AU - Kalinina, Svetlana A
AU - Rudakova, Irina P
AU - Vakhrin, Mikhail I
AU - Dolzhenko, Anton V
PY - 2013
Y1 - 2013
N2 - 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.
AB - 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.
UR - http://www.sciencedirect.com/science/article/pii/S0223523413000895
U2 - 10.1016/j.ejmech.2013.02.003
DO - 10.1016/j.ejmech.2013.02.003
M3 - Article
VL - 63
SP - 144
EP - 150
JO - European Journal of Medicinal Chemistry
JF - European Journal of Medicinal Chemistry
SN - 0223-5234
ER -