Structure-activity relationship of cardiac steroids having a doubly linked sugar and related compounds for the inhibition of Na+,K+-adenosine triphosphatase.
Forty-three different cardiac steroids having a doubly linked sugar and related compounds were tested for inhibition of Na+,K+-adenosine triphosphatase from guinea pig heart, and the structure-activity relationship has been discussed. The doubly linked glycosides showed higher activities than the respective genins. The inhibitory activities of these compounds were also dependent upon the presence of ring C substituents. The bufadienolide rhamnosides exhibited greater than three times the inhibitory activity of the parent genin, while the glucosyl residue exerted no significant activity.
D000818:Animals; D001001:Anura; D002301:Cardiac Glycosides / Q000494:pharmacology*; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009206:Myocardium / Q000201:enzymology*; D000254:Sodium-Potassium-Exchanging ATPase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
D002301:Cardiac Glycosides; D000254:Sodium-Potassium-Exchanging ATPase