Villani F J, Mann T A, Wefer E A, Hannon J, Larca L L, Landon M J, Spivak W, Vashi D, Tozzi S, Danko G, del Prado M, Lutz R
J Med Chem. 1975 Jan;18(1):1-8. doi: 10.1021/jm00235a001.
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.
本文描述了四种异构氮杂蒽酮3及其一些芳环取代衍生物的制备方法。这些酮被转化为标题化合物，并对其生物学性质进行了研究。该系列中最有趣的化合物，即1-氮杂蒽的1-甲基-4-哌啶基亚基衍生物，显示出口服有效的强效支气管扩张剂以及中度抗组胺药的特性。将该化合物的生物学性质与多种抗组胺药以及已知的支气管扩张剂进行了比较。还讨论了构效关系。
