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

descriptionPublicationkeyboard_double_arrow_right Article 01 Jan 1975 English Publisher:American Chemical Society (ACS)Journal:Journal of Medicinal Chemistry, volume 18, pages 1-8 (issn: 0022-2623, eissn: 1520-4804,

Authors: F J, Villani; T A, Mann; E A, Wefer; J, Hannon; L L, Larca; M J, Landon; W, Spivak; +5 Authors

doi: 10.1021/jm00235a001

pmid: 45881

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

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Abstract

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.

Keywords

Male, Aza Compounds, Ovalbumin, Airway Resistance, Guinea Pigs, In Vitro Techniques, Histamine Release, Bronchodilator Agents, Antigen-Antibody Reactions, Structure-Activity Relationship, Dyspnea, Xanthenes, Ileum, Histamine H1 Antagonists, Animals, Spectrophotometry, Ultraviolet, Lung Compliance

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