Comparative platelet anti-aggregant activity of D-cysteinolic acid analogues.
D-Cysteinolic acid (1) analogues with an S-C-C-N skeleton showed increased platelet anti-aggregant activity in the following order: 2-aminoethanesulfonic acids, thiazolidines, 2-aminoethanethiols and 2-aminoethyl disulfides. Methyl substitutions at the 2-position potentiated the activity. Of these analogues, bis [(R)-2-aminopropyl] disulfide was the most potent inhibitor of platelet aggregation, with about 600-fold the activity of (1).
Sataka
M
M
Central Research Laboratory, Nippon Suisan Co. Ltd., Tokyo, Japan.
Chiba
Y
Y
Kohama
Y
Y
Yamamoto
K
K
Okabe
M
M
Mimura
T
T
Imanishi
T
T
Iwata
C
C
D000818:Animals; D003545:Cysteine / Q000031:analogs & derivatives* / Q000494:pharmacology; D004220:Disulfides / Q000494:pharmacology; D008297:Male; D015394:Molecular Structure; D010975:Platelet Aggregation Inhibitors; D051381:Rats; D011919:Rats, Inbred Strains; D013329:Structure-Activity Relationship; D013438:Sulfhydryl Compounds / Q000494:pharmacology
D004220:Disulfides; D010975:Platelet Aggregation Inhibitors; D013438:Sulfhydryl Compounds; C055419:cysteinolic acid; D003545:Cysteine