Thiocardenolides II: synthesis and pharmacological evaluation of 3beta-thioacetyl-14beta-hydroxy-5beta-card-20(22)-enolide.
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.
D000251:Adenosine Triphosphatases / Q000037:antagonists & inhibitors; D000818:Animals; D001001:Anura; D001921:Brain / Q000201:enzymology; D004073:Digitoxigenin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D006168:Guinea Pigs; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D008722:Methods; D009200:Myocardial Contraction / Q000187:drug effects; D051381:Rats
D004073:Digitoxigenin; D000251:Adenosine Triphosphatases