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Synthesis, antiarrhythmic activity, and toxicological evaluation of mexiletine analogues.

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.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Roselli M,Carocci A,Budriesi R,Micucci M,Toma M,Di Cesare Mannelli L,Lovece A,Catalano A,Cavalluzzi MM,Bruno C,De Palma A,Contino M,Perrone MG,Colabufo NA,Chiarini A,Franchini C,Ghelardini C,Habtemariam S,Lentini G

doi

10.1016/j.ejmech.2016.05.046

subject

Has Abstract

pub_date

2016-10-04 00:00:00

pages

300-307

eissn

0223-5234

issn

1768-3254

pii

S0223-5234(16)30444-5

journal_volume

121

pub_type

杂志文章

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