Antifertility activity of N-protected glycine activated esters.
A series of N-protected glycine activated esters was found to have antifertility activity in mice when administered intravaginally. The N-carbobenzoxyglycine vinyl ester and N-carbobenzoxyglycine 1,2-dibromoethyl ester analogs possessed the best activity in inhibiting pregnancy but were much less active when administered intraperitoneally. The acrosin enzymatic activity of sperm also was inhibited by these N-protected glycine activated esters, as measured by N-alpha-benzoyl-L-arginine ethyl ester and azocasein hydrolysis. The ability to inhibit N-alpha-benzoyl-L-arginine ethyl ester hydrolysis, a trypsin-like activity, appeared to have a positive correlation with antifertility activity when the agents were administered intravaginally.
D000176:Acrosin / Q000037:antagonists & inhibitors; D000818:Animals; D003271:Contraceptive Agents, Female; D004353:Drug Evaluation, Preclinical; D005260:Female; D005998:Glycine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000494:pharmacology; D066298:In Vitro Techniques; D007274:Injections, Intraperitoneal; D008297:Male; D051379:Mice; D011247:Pregnancy; D014621:Vagina
D003271:Contraceptive Agents, Female; D000176:Acrosin; D005998:Glycine