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Synthesis and platelet aggregation inhibiting activity of prostaglandin D analogues.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 1983 Jun; Vol. 26 (6), pp. 790-9. - Publication Year :
- 1983
-
Abstract
- Several prostaglandin D (PGD) analogues have been synthesized, incorporating the following variations: (a) varying degrees of side-chain unsaturation, (b) C-9 hydroxy removed or in the unnatural 9 beta configuration, (c) metabolically stabilized analogues (e.g., 15-methyl, 16,16-dimethyl, 17-phenyl, etc.), and (d) delta 12 isomers resulting from decomposition of PGD2. With regard to their ability to inhibit adenosine diphosphate (ADP) induced human platelet aggregation: (a) PGD3 greater than or equal to PGD2 greater than PGD1 greater than 13,14-dihydro-PGD1, (b) the 9 beta- and 9-deoxy-PGD2 analogues are more potent than PGD2, (c) metabolically stabilized analogues with bulky substituents at or near C-15 have substantially reduced antiaggregatory activity relative to PGD2 and (d) the delta 12 isomers of PGD2 are much less active than PGD2.
- Subjects :
- Animals
Blood Pressure drug effects
Colon drug effects
Cricetinae
Diarrhea chemically induced
Fertility drug effects
Gerbillinae
Humans
Prostaglandins D chemical synthesis
Prostaglandins D pharmacology
Prostaglandins, Synthetic pharmacology
Rats
Platelet Aggregation drug effects
Prostaglandins, Synthetic chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 26
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 6854581
- Full Text :
- https://doi.org/10.1021/jm00360a003