Azaprostaglandin analogs. Synthesis and biological properties of 11-azaprostaglandin derivatives

New nitrogen analogues of prostaglandins (11, 11a, 12, and 12a) have been synthesized starting from a 4,5-disubstituted 2-pyrrolidinone nucleus (5 and 5a) containing one side chain and a suitable functionality for elaborating the second one. These analogues had no better activity than natural prosta...

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Veröffentlicht in:	Journal of medicinal chemistry 1981-05, Vol.24 (5), p.625-628
Hauptverfasser:	Barco, Achille, Benetti, Simonetta, Pollini, Gian Piero, Baraldi, Pier Giovanni, Guarneri, Mario, Gandolfi, Carmelo, Ceserani, Roberto, Longiave, Daniela
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Chemical Phenomena Chemistry Guinea Pigs In Vitro Techniques Muscle Contraction - drug effects Muscle, Smooth - drug effects Platelet Aggregation - drug effects Prostaglandins E - pharmacology Prostaglandins, Synthetic - chemical synthesis Prostaglandins, Synthetic - pharmacology Pyrrolidinones - chemical synthesis Pyrrolidinones - pharmacology Rats
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Beschreibung
Zusammenfassung:	New nitrogen analogues of prostaglandins (11, 11a, 12, and 12a) have been synthesized starting from a 4,5-disubstituted 2-pyrrolidinone nucleus (5 and 5a) containing one side chain and a suitable functionality for elaborating the second one. These analogues had no better activity than natural prostaglandins in vitro [guinea pig ileum and trachea, rat stomach fundus strip, uterus and portal vein, ADP-induced guinea pig platelet-rich plasma (PRP) aggregation]. They similarly lacked any interesting activity in vivo [anesthetized rat blood pressure, stress, and acetylsalycilic acid (ASA) induced gastric lesions in rat].
ISSN:	0022-2623 1520-4804
DOI:	10.1021/jm00137a027