Long-acting contraceptive agents: aliphatic and alicyclic carboxylic esters of levonorgestrel.
Esters of levonorgestrel (13 beta-ethyl-17 alpha-ethynyl-17 beta-hydroxygon-4-en-3-one) with a variety of aliphatic and alicyclic carboxylic acids have been prepared and characterised. In tests for the suppression of estrus in rats, esters with short-chain aliphatic acids and with cyclobutane-carboxylic acid were considerably more active than the standard, norethisterone enanthate (17 alpha-ethynyl-17 beta-hydroxyestr-4-en-3-one). Such esters show great promise for development as long-acting progestogens.
D002264:Carboxylic Acids; D003276:Contraceptives, Oral / Q000138:chemical synthesis*; D003277:Contraceptives, Oral, Combined / Q000138:chemical synthesis*; D003692:Delayed-Action Preparations; D004952:Esters; D007202:Indicators and Reagents; D016912:Levonorgestrel; D009644:Norgestrel / Q000138:chemical synthesis*; D013053:Spectrophotometry; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D002264:Carboxylic Acids; D003276:Contraceptives, Oral; D003277:Contraceptives, Oral, Combined; D003692:Delayed-Action Preparations; D004952:Esters; D007202:Indicators and Reagents; D009644:Norgestrel; D016912:Levonorgestrel