A new series of antiallergic agents. II. Synthesis and activity of new 6,11-dihydrodibenz[b,e]oxepin-carboxylic acid derivatives

DOI: 10.1248/cpb.39.2729

Source and publish data:

Chemical and Pharmaceutical Bulletin p. 2729 - 2733 (1991)

Update date:2022-08-04

Topics:

Authors:

Kumazawa

Ohshima Ohshima

Harakawa

Sato Sato

Obase Obase

Oiji Oiji

Ishii Ishii

Ohmori Ohmori

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Article abstract of DOI:10.1248/cpb.39.2729

New methods for the preparation of multi-functionalized-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 activity of 1. The introduction of bromine atom at C-9 of 1 could elongate the duration of the action of the parent. Antiplatelet activity, a new pharmacological property of this series of compounds, was observed in one of the derivatives of 1.

Full text of DOI:10.1248/cpb.39.2729

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