Synthesis, local anaesthetic and antiarrhythmic activities of N-alkyl derivatives of proline anilides
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...
| Main Authors: | , , , , , , |
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| Format: | Journal Article |
| Published: |
Elsevier Masson
2013
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| Online Access: | http://www.elsevier.com/locate/ejmech http://hdl.handle.net/20.500.11937/20875 |
| _version_ | 1848750432162152448 |
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| author | Kalinin, D Pantsurkin, Vladimir Syropyatov, Boris Kalinina, S Rudakova, Irina Vakhrin, Mikhail Dolzhenko, Anton |
| author_facet | Kalinin, D Pantsurkin, Vladimir Syropyatov, Boris Kalinina, S Rudakova, Irina Vakhrin, Mikhail Dolzhenko, Anton |
| author_sort | Kalinin, D |
| building | Curtin Institutional Repository |
| collection | Online Access |
| description | 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. |
| first_indexed | 2025-11-14T07:36:44Z |
| format | Journal Article |
| id | curtin-20.500.11937-20875 |
| institution | Curtin University Malaysia |
| institution_category | Local University |
| last_indexed | 2025-11-14T07:36:44Z |
| publishDate | 2013 |
| publisher | Elsevier Masson |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | curtin-20.500.11937-208752019-02-19T04:26:05Z Synthesis, local anaesthetic and antiarrhythmic activities of N-alkyl derivatives of proline anilides Kalinin, D Pantsurkin, Vladimir Syropyatov, Boris Kalinina, S Rudakova, Irina Vakhrin, Mikhail Dolzhenko, Anton 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. 2013 Journal Article http://hdl.handle.net/20.500.11937/20875 10.1016/j.ejmech.2013.02.003 http://www.elsevier.com/locate/ejmech Elsevier Masson fulltext |
| spellingShingle | Kalinin, D Pantsurkin, Vladimir Syropyatov, Boris Kalinina, S Rudakova, Irina Vakhrin, Mikhail Dolzhenko, Anton Synthesis, local anaesthetic and antiarrhythmic activities of N-alkyl derivatives of proline anilides |
| title | Synthesis, local anaesthetic and antiarrhythmic activities of N-alkyl derivatives of proline anilides |
| title_full | Synthesis, local anaesthetic and antiarrhythmic activities of N-alkyl derivatives of proline anilides |
| title_fullStr | Synthesis, local anaesthetic and antiarrhythmic activities of N-alkyl derivatives of proline anilides |
| title_full_unstemmed | Synthesis, local anaesthetic and antiarrhythmic activities of N-alkyl derivatives of proline anilides |
| title_short | Synthesis, local anaesthetic and antiarrhythmic activities of N-alkyl derivatives of proline anilides |
| title_sort | synthesis, local anaesthetic and antiarrhythmic activities of n-alkyl derivatives of proline anilides |
| url | http://www.elsevier.com/locate/ejmech http://hdl.handle.net/20.500.11937/20875 |