Synthesis and pharmacological activities of 13-Dehydro derivatives of primary prostaglandins

13-Dehydro derivatives of prostaglandin E 1, E 2, E 3, F 1α and F 2α were synthesized. Compared with natural prostaglandins, 13-dehydro analogues were found to exhibit more potent inhibitory activity against human platelet aggregation and relaxation of guinea-pig isolated trachea, while they showed...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-06, Vol.8 (12), p.1507-1510
Hauptverfasser:	Tanami, Tohru, Kameo, Kazuya, Ono, Naoya, Nakagawa, Takashi, Annou, Shigesato, Tsuboi, Mie, Tani, Kousuke, Okamoto, Sentaro, Sato, Fumie
Format:	Artikel
Sprache:	eng
Schlagworte:	agonists Animals Biological and medical sciences Blood. Blood coagulation. Reticuloendothelial system Guinea Pigs Humans Ileum - drug effects Ileum - physiology Magnetic Resonance Spectroscopy Medical sciences Molecular Structure Muscle Muscle Contraction - drug effects Pharmacology. Drug treatments Platelet Aggregation Inhibitors - chemical synthesis Platelet Aggregation Inhibitors - pharmacology prostaglandins Prostaglandins - chemical synthesis Prostaglandins - chemistry Prostaglandins - pharmacology
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Zusammenfassung:	13-Dehydro derivatives of prostaglandin E 1, E 2, E 3, F 1α and F 2α were synthesized. Compared with natural prostaglandins, 13-dehydro analogues were found to exhibit more potent inhibitory activity against human platelet aggregation and relaxation of guinea-pig isolated trachea, while they showed less potent activity of contraction of guinea-pig isolated ileum. 13-Dehydro derivatives of prostaglandin E 1, E 2, E 3, F 1α and F 2α were synthesized. Compared with natural prostagladins, 13-dehydro analogues were found to exhibit more potent inhibitory activity against human platelet aggregation and relaxation of guinea-pig isolated trachea, while they showed less potent activity of contraction of guinea-pig isolated ileum.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00247-9