Syntheses and Anti-histaminic and Anti-allergic Activities of Hexahydro-4-hydroxy-1-benzofuran-2-ones

The hexahydro-4-hydroxy-1-benzofuran-2-ones 3a, 4a, and 5a (related to the 6β-hydroxyeremophilenolides 1 and 2, which show anti-histaminic and anti-allergic activities) were synthesized from dimedone through the compounds 18a, 23a, and 24a, followed by dehydration reactions. Pharmacological investig...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Chemical & pharmaceutical bulletin 1984/06/25, Vol.32(6), pp.2249-2261
Hauptverfasser:	TAKEUCHI, NAOKI, KASAMA, TOSHIO, IKEDA, RIKA, SHIMIZU, KAZUE, HATAKEYAMA, KUMIKO, AIDA, YOKO, KANEKO, YOKO, TOBINAGA, SEISHO
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzofurans - chemical synthesis Benzofurans - pharmacology Chemical Phenomena Chemistry Exact sciences and technology Guinea Pigs Heterocyclic compounds Heterocyclic compounds with o, s, se, te hetero atom and condensed derivatives Histamine Antagonists - chemical synthesis Hypersensitivity - prevention & control In Vitro Techniques Male Muscle Contraction - drug effects Muscle, Smooth - drug effects Organic chemistry Passive Cutaneous Anaphylaxis - drug effects Preparations and properties Rats Rats, Inbred Strains Schultz-Dale reaction
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	The hexahydro-4-hydroxy-1-benzofuran-2-ones 3a, 4a, and 5a (related to the 6β-hydroxyeremophilenolides 1 and 2, which show anti-histaminic and anti-allergic activities) were synthesized from dimedone through the compounds 18a, 23a, and 24a, followed by dehydration reactions. Pharmacological investigations of 3a, 4a, 5a, 18a, 23a, and 24a showed that compounds 4a and 5a have anti-histaminic activity and cause marked inhibition in the Schultz-Dale reaction.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.32.2249