PMID: 45881Jan 1, 1975

Benzopyranopyridine derivatives. 1. Aminoalkyl derivatives of the azaxanthenes as bronchodilating agents

Journal of Medicinal Chemistry
F J VillaniR Lutz


The preparation of the four isomeric azaxanthones 3 and a number of their aromatic ring substituted derivatives is described. These ketones were converted into the title compounds which were examined for their biological properties. The most interesting compound in this series, the 1-methyl-4-piperidylidene derivative of 1-azaxanthene, shows the profile of an orally effective potent bronchodilating agent as well as a moderate antihistamine. Biological properties of this compound were compared to a number of antihistamines as well as known bronchodilating agents. Structure-activity relationships are also discussed.

Related Concepts

Aza Compounds
Structure-Activity Relationship
Airway Resistance
Broncholytic Effect
Antihistamines, Classical
Antigen-Antibody Reactions
Spectrophotometry, Ultraviolet
Lung Compliance

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