Carocci A, Catalano A, Bruno C, Lentini G, Franchini C, De Bellis M, De Luca A, Conte Camerino D
Synthesis and in vitro sodium channel blocking activity evaluation of novel homochiral mexiletine analogs. [JOURNAL ARTICLE]
Chirality 2009 Jun 18.
New chiral mexiletine analogs were synthesized in their optically active forms and evaluated in vitro as use-dependent blockers of skeletal muscle sodium channels. Tests carried out on sodium currents of single muscle fibers of Rana esculenta demonstrated that all of them exerted a higher use-dependent block than mexiletine. The most potent analog, (S)-3-(2,6-dimethylphenoxy)-1-phenylpropan-1-amine (S)-(5), was six-fold more potent than (R)-Mex in producing a tonic block. As observed with mexiletine, the newly synthesized compounds exhibit modest enantioselective behavior, that is more evident in 3-(2,6-dimethylphenoxy)butan-1-amine (3). Chirality, 2009. (c) 2009 Wiley-Liss, Inc.
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