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Synthesis, antiarrhythmic activity, and toxicological evaluation of mexiletine analogues

Synthesis, antiarrhythmic activity, and toxicological evaluation of mexiletine analogues

Roselli, Mariagrazia, Carocci, Alessia, Budriesi, Roberta, Micucci, Matteo, Toma, Maddalena, Di Cesare Mannelli, Lorenzo, Lovece, Angelo, Catalano, Alessia, Cavalluzzi, Maria Maddalena, Bruno, Claudio, De Palma, Annalisa, Contino, Marialessandra, Perrone, Maria Grazia, Colabufo, Nicola Antonio, Chiarini, Alberto, Franchini, Carlo, Ghelardini, Carla, Habtemariam, Solomon and Lentini, Giovanni (2016) Synthesis, antiarrhythmic activity, and toxicological evaluation of mexiletine analogues. European Journal of Medicinal Chemistry, 121. pp. 300-307. ISSN 0223-5234 (doi:10.1016/j.ejmech.2016.05.046)

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Abstract

Four mexiletine analogues have been tested for their antiarrhythmic, inotropic, and chronotropic effects on isolated guinea pig heart tissues and to assess calcium antagonist activity, in comparison with the parent compound mexiletine. All analogues showed from moderate to high antiarrhythmic activity. In particular, three of them (1b,c,e) were more active and potent than the reference drug, while exhibiting only modest or no negative inotropic and chronotropic effects and vasorelaxant activity, thus showing high selectivity of action. All compounds showed no cytotoxicity and 1b,c,d did not impair motor coordination. All in, these new analogues exhibit an interesting cardiovascular profile and deserve further investigation.

Item Type: Article
Uncontrolled Keywords: Mexiletine; Antiarrhythmics; P-glycoprotein; Inotropism; MW-assisted synthesis
Subjects: Q Science > QC Physics
Q Science > QD Chemistry
Faculty / Department / Research Group: Faculty of Engineering & Science
Faculty of Engineering & Science > Department of Pharmaceutical, Chemical & Environmental Sciences
Last Modified: 26 Oct 2017 15:29
Selected for GREAT 2016: None
Selected for GREAT 2017: None
Selected for GREAT 2018: None
URI: http://gala.gre.ac.uk/id/eprint/17600

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