A New Series of Antiallergic Agents. II. Synthesis and Activity of New 6, 11-Dihydrodibenz[b, e]oxepin-carboxylic Acid Derivatives

New methods for the preparation of multi-functionallized-6, 11-dihydrodibenz[b, e]oxepins were developed. The structural requirements of KW-4994 (1), a promising orally active antiallergic agent, were defined. A carboxyl group at C-2 was critical for enhanced antiallergic of 1. The introduction of b...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Chemical & pharmaceutical bulletin 1991/10/25, Vol.39(10), pp.2729-2733
Hauptverfasser:	KUMAZAWA, Toshiaki, OHSHIMA, Etsuo, HARAKAWA, Hiroyuki, SATO, Hideyuki, OBASE, Hiroyuki, OIJI, Yoshimasa, ISHII, Akio, ISHII, Hidee, OHMORI, Kenji
Format:	Artikel
Sprache:	eng
Schlagworte:	6, 11-dihydrodibenz[b, e]oxepin anaphylaxis activity Animals anti-passive cutaneous antiallergic agent antiasthmatic agent antiplatelet activity Benzoxepins - chemical synthesis Benzoxepins - pharmacology Benzoxepins - therapeutic use Chemistry Corpus Striatum - metabolism Exact sciences and technology Guinea Pigs H1-antihistaminic activity Heterocyclic compounds Heterocyclic compounds with o, s, se, te hetero atom and condensed derivatives Histamine H1 Antagonists - chemical synthesis Histamine H1 Antagonists - pharmacology Histamine H1 Antagonists - therapeutic use Hypersensitivity, Delayed - drug therapy Male Organic chemistry Preparations and properties Rats Rats, Inbred Strains receptor antagonist Receptors, Cholinergic - drug effects Receptors, Cholinergic - metabolism Structure-Activity Relationship
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	New methods for the preparation of multi-functionallized-6, 11-dihydrodibenz[b, e]oxepins were developed. The structural requirements of KW-4994 (1), a promising orally active antiallergic agent, were defined. A carboxyl group at C-2 was critical for enhanced antiallergic of 1. The introduction of bromine atom at C-9 of 1 could elongate the duration of the action of the parent. Antiplatelet acetivity, a new pharmacological property of this series of compounds, was observed in one of the derivatives of 1.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.39.2729