[Relationship between the structure, affinity for phospholipid membranes and anti-arrhythmic activity of 10-acylaminopropionyl derivatives of phenothiazines].
The interaction of thirteen 10-acylaminopropionyl derivatives of phenothiazine with phospholipid membranes was investigated. A correlation between the affinity of these substances to membranes and their antiarrhythmic activity was found. A molecular model of a complex of the substance-membrane is proposed. It shows how the molecular structure of the study substances affects their affinity to phospholipids and thus influences the activity of the former. The affinity chiefly depends on the accordance between the structure and the disposition of the lateral substitute, on the one hand, and the structure of the phospholipid bis-layer, and also of the hydrophobic nature of the 10-acylaminopropionyl group, on the other.
D000157:Aconitine / Q000037:antagonists & inhibitors; D000818:Animals; D000889:Anti-Arrhythmia Agents; D001145:Arrhythmias, Cardiac / Q000139:chemically induced; D055598:Chemical Phenomena; D002621:Chemistry; D008567:Membranes, Artificial; D008956:Models, Chemical; D010640:Phenothiazines; D010743:Phospholipids; D013329:Structure-Activity Relationship
D000889:Anti-Arrhythmia Agents; D008567:Membranes, Artificial; D010640:Phenothiazines; D010743:Phospholipids; D000157:Aconitine
Sviaz' mezhdu strukturoĭ, srodstvom i fosfolipidnym membranam i antiaritmicheskoí aktivnost'iu 10-atsilaminopropionil'nykh proizvodnykh fenotiazina.