Synthesis, antiarrhythmic activity, and toxicological evaluation of mexiletine analogues
| Autor: | Carlo Franchini, Annalisa De Palma, Nicola Antonio Colabufo, Maria Maddalena Cavalluzzi, Lorenzo Di Cesare Mannelli, Alessia Carocci, Alessia Catalano, Alberto Chiarini, Claudio Bruno, Mariagrazia Roselli, Matteo Micucci, Solomon Habtemariam, Giovanni Lentini, Marialessandra Contino, Angelo Lovece, Maddalena Toma, Roberta Budriesi, Carla Ghelardini, Maria Grazia Perrone |
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| Přispěvatelé: | 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, Lentini, Giovanni |
| Jazyk: | angličtina |
| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Chronotropic Inotrope Cell Survival Muscle Relaxation Guinea Pigs chemistry.chemical_element Antiarrhythmic Mexiletine Chemistry Techniques Synthetic Calcium Pharmacology P-glycoprotein Antiarrhythmics Inotropism MW-assisted synthesis Madin Darby Canine Kidney Cells 03 medical and health sciences 0302 clinical medicine Dogs Drug Discovery medicine Animals Humans Heart Atria Cytotoxicity Aorta Anti-Arrhythmia Agents Hep G2 Cells Chemistry Synthetic Organic Chemistry Antagonist Chemistry Techniques General Medicine MW-assisted synthesi 030104 developmental biology Muscle relaxation 030217 neurology & neurosurgery medicine.drug |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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