Synthesis and evaluation of voltage-gated sodium channel blocking pyrroline derivatives endowed with both antiarrhythmic   and antioxidant activities.

Synthesis and evaluation of voltage-gated sodium channel blocking pyrroline derivatives endowed with both antiarrhythmic  and antioxidant activities.
ChemMedChem. 2020 Oct 04;:
Authors: Carocci A, Budriesi R, Micucci M, Cavalluzzi MM, Milani G, Catalano A, De Palma A, Corbo F, Franchini C, Habtemariam S, Giovanni L
Abstract
Under the hypothesis that cardioprotecting agents might benefit from a 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 (2a-e, Fig. 1) were more potent as antiarrhythmic agents than mexiletine and displayed antioxidant activity.
PMID: 33015979 [PubMed - as supplied by publisher]

Source: ChemMedChem - October 3, 2020 Category: Chemistry Authors: Carocci A, Budriesi R, Micucci M, Cavalluzzi MM, Milani G, Catalano A, De Palma A, Corbo F, Franchini C, Habtemariam S, Giovanni L Tags: ChemMedChem Source Type: research