Facile, alternative synthetic routes gave access to both pilsicainide [N-(2,6-dimethylphenyl)-2-tetrahydro-1H-pyrrolizin-7a(5H)-ylacetamide, 1], a well-known I-C antiarrhythmic drug, and its oxymethylene analog 2. Both compounds were tested on human skeletal muscle voltage-gated sodium channels, hNav1.4, transfected in tsA201 cells. 7a-[2-(2,6-Dimethylphenoxy)ethyl]hexahydro-1H-pyrrolizine (2) behaved as a bioisostere of 1, exerting a 4-fold more potent use-dependent block
Pilsicainide and its oxymethylene analog: Facile alternative synthesis and in vitro testing on human skeletal muscle sodium channels
CATALANO, ALESSIA;DESAPHY, Jean Francois;CAVALLUZZI, MARIA MADDALENA;CAROCCI, ALESSIA;FRANCHINI, Carlo;LENTINI, Giovanni;CONTE, Diana;
2007-01-01
Abstract
Facile, alternative synthetic routes gave access to both pilsicainide [N-(2,6-dimethylphenyl)-2-tetrahydro-1H-pyrrolizin-7a(5H)-ylacetamide, 1], a well-known I-C antiarrhythmic drug, and its oxymethylene analog 2. Both compounds were tested on human skeletal muscle voltage-gated sodium channels, hNav1.4, transfected in tsA201 cells. 7a-[2-(2,6-Dimethylphenoxy)ethyl]hexahydro-1H-pyrrolizine (2) behaved as a bioisostere of 1, exerting a 4-fold more potent use-dependent blockFile in questo prodotto:
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