93968-89-9Relevant articles and documents
Synthesis and Evaluation of Voltage-Gated Sodium Channel Blocking Pyrroline Derivatives Endowed with Both Antiarrhythmic and Antioxidant Activities
Carocci, Alessia,Roselli, Mariagrazia,Budriesi, Roberta,Micucci, Matteo,Desaphy, Jean-Fran?ois,Altamura, Concetta,Cavalluzzi, Maria Maddalena,Toma, Maddalena,Passeri, Giovanna Ilaria,Milani, Gualtiero,Lovece, Angelo,Catalano, Alessia,Bruno, Claudio,De Palma, Annalisa,Corbo, Filomena,Franchini, Carlo,Habtemariam, Solomon,Lentini, Giovanni
, p. 578 - 588 (2021)
Under the hypothesis that cardioprotective agents might benefit from synergism between antiarrhythmic activity and antioxidant properties, a small series of mexiletine analogues were coupled with the 2,2,5,5-tetramethylpyrroline moiety, known for its antioxidant effect, in order to obtain dual-acting drugs potentially useful in the protection of the heart against post-ischemic reperfusion injury. The pyrroline derivatives reported herein were found to be more potent as antiarrhythmic agents than mexiletine and displayed antioxidant activity. The most interesting tetramethylpyrroline congener, a tert-butyl-substituted analogue, was at least 100 times more active as an antiarrhythmic than mexiletine.