Nitrogen bridgehead compounds. 66. Bronchodilator nitrogen bridgehead compounds with a pyrimidinone moiety

New types of bronchodilator agents, bi- and tricyclic nitrogen bridgehead compounds with a pyrimidin-4(3H)-one ring, were synthesized and evaluated for bronchodilator activity against serotonin-, histamine-, and acetylcholine-induced spasms in the guinea pig Konzett-Rössler test. The structure-activ...

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Published inJournal of medicinal chemistry Vol. 30; no. 9; pp. 1543 - 1549
Main Authors Hermecz, Istvan, Vasvari-Debreczy, Lelle, Horvath, Agnes, Balogh, Maria, Kokosi, Jozsef, DeVos, Christine, Rodriguez, Ludovic
Format Journal Article
LanguageEnglish
Published United States American Chemical Society 01.09.1987
Subjects
Animals
Bronchi - drug effects
Bronchodilator Agents - metabolism
Chemical Phenomena
Chemistry, Physical
Dogs
Dose-Response Relationship, Drug
Female
Guinea Pigs
Humans
Male
Nitrogen - metabolism
Pilocarpine - pharmacology
Spasm - chemically induced
Trachea - drug effects
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Summary:New types of bronchodilator agents, bi- and tricyclic nitrogen bridgehead compounds with a pyrimidin-4(3H)-one ring, were synthesized and evaluated for bronchodilator activity against serotonin-, histamine-, and acetylcholine-induced spasms in the guinea pig Konzett-Rössler test. The structure-activity relationships are discussed. The effects of some bi- and tricyclic derivatives on the human bronchus were also investigated. The homologous tricyclic compounds 68 and 69 were tested on isolated guinea pig ileum and trachea, and the effects of compound 69 were investigated in pilocarpine-treated dogs. Azepino[2,1-b]quinazoline (69; CHINOIN-1289) was selected for further biochemical and clinical investigations.
Bibliography:istex:BDC6D5A57DF5DAFDA0F580085481FEF70A60B537
ark:/67375/TPS-KXHBMQZS-R
ISSN:0022-2623
1520-4804
DOI:10.1021/jm00392a003