Thiocardenolides II: synthesis and pharmacological evaluation of 3beta-thioacetyl-14beta-hydroxy-5beta-card-20(22)-enolide.

ABSTRACT

The synthesis of a 3beta-thioacetylcardenolide is described. The thioacetate exhibited effects similar to those seen with digitoxigenin acetate on the isolated frog and guinea pig hearts at 1 X 10(-7) dilution. In the intact rat heart, the lethal dose was 5 mg/kg for the thioacetate and 2.5 mg/kg for digitoxigenin acetate. The thioacetate inhibited sodium- and potassium-activated adenosine triphosphatase to the same extent as digitoxigenin, but it was somewhat less inhibitory than digitoxigenin acetate.