Antifertility and Antiproteolytic Activity of Activated N‐Carbobenzoxy Amino Acid Esters

N‐Carbobenzoxy L‐phenylalanine, glycine, L‐leucine, and L‐proline derivatives, their vinyl esters, and their 1, 2‐dibromoethyl esters were tested for antifertility activity in mice. Intraperitoneal administration reduced the pregnancy percentage and the number of fetuses per litter, Intravaginal adm...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1979-06, Vol.68 (6), p.696-698
Main Authors: Hall, I.H., Drew, J.H., Sajadi, Z., Loeffler, L.J.
Format: Article
Language:English
Subjects:
Acrosin - antagonists & inhibitors
Amino Acids - administration & dosage
Amino Acids - pharmacology
Animals
antiproteolytic activity
Carbobenzpxy amino acid esters-contraceptive activity
Carbobenzpxy amino acid esters—contraceptive activity, antiproteolytic activity, mice
Contraceptives
Contraceptives, potential—activated N‐Carbobenzoxy amino acid esters, mice
effect of N-Carbobenzoxy amino acid esters
Enzyme activity-effect of activated N-Carbobenzoxy amino acid esters on sperm proteolysis
Enzyme activity—effect of activated N‐Carbobenzoxy amino acid esters on sperm proteolysis, mice
Esters - administration & dosage
Esters - pharmacology
Female
Fertility - drug effects
In Vitro Techniques
Injections, Intraperitoneal
Male
Mice
potential-activated N-Carbobenzoxy amino acid esters
Pregnancy
Protease Inhibitors
Rats
Sperm-enzymes
Spermatozoa - enzymology
Sperm—enzymes, effect of N‐Carbobenzoxy amino acid esters, mice
Vagina
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Description
Summary:N‐Carbobenzoxy L‐phenylalanine, glycine, L‐leucine, and L‐proline derivatives, their vinyl esters, and their 1, 2‐dibromoethyl esters were tested for antifertility activity in mice. Intraperitoneal administration reduced the pregnancy percentage and the number of fetuses per litter, Intravaginal administration reduced the pregnancy percentage significantly, with N‐carbobenzoxyglycine vinyl ester, N‐carbobenzox‐yglycine‐1,2‐dibromoethyl ester, N‐carbobenzoxy‐L‐leucine‐ 1,2‐dibromoethyl ester, and N‐carbobenzoxy‐L‐proline‐1,2‐dibromoethyl ester producing 100% inhibition at 10 mg/kg/day. Sperm enzyme hydrolysis of the nonspecific substrate azocasein was inhibited significantly by certain N‐Carbobenzoxy amino acid esters in vitro. Specific substrate N‐benzoyl‐L‐arginine ethyl ester hydrolysis was also inhibited. Compounds that inhibited N‐benzoyl‐L‐arginine ethyl ester hydrolysis also demonstrated in vivo intravaginal antifertility activity.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600680610