Synthesis and biological activity of some cardiotonic compounds related to gitoxigenin.
The four diastereomeric 3,16-diacetates 6, 9, 10 and 11 were prepared from gitoxin 1 by the routes shown in Schemes 1 and 2 and tested for inotropic activity in the isolated guinea-pig atrial preparation. In line with earlier findings in the digitoxigenin series, derivatives with a 3 alpha-acetoxy function, viz 9 and 10, possessed high biological activity.
D000818:Animals; D002298:Cardenolides / Q000138:chemical synthesis* / Q000494:pharmacology; D002316:Cardiotonic Agents / Q000138:chemical synthesis* / Q000494:pharmacology / Q000633:toxicity; D006168:Guinea Pigs; D006325:Heart Atria / Q000187:drug effects; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D009200:Myocardial Contraction / Q000187:drug effects; D013329:Structure-Activity Relationship
D002298:Cardenolides; D002316:Cardiotonic Agents