Abstract
Theophylline derivatives have long been recognized as potent bronchodilators for the relief of acute asthma. Recently, it was found that bacterial infection has a role in asthma pathogenesis. The present work involves the design and synthesis of 8-substituted theophylline derivatives as bronchodilators and antibacterial agents. The chemical structures of these compounds were elucidated by IR, 1H-NMR, mass spectrometry, and elemental analyses. The bronchodilator activity was evaluated using acetylcholine-induced bronchospasm in guinea pigs, and most of the compounds showed significant anti-bronchoconstrictive activity in comparison with standard aminophylline. In addition, the antibacterial activity of all the target compounds was investigated in vitro against Gram-positive and Gram-negative bacteria using ampicillin as a reference drug. Results showed that some of the tested compounds possessed significant antibacterial activity. A pharmacophore model was computed to obtain useful insight into the essential structural features of bronchodilator activity. A structure activity relationship was also discussed.
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Hayallah, A.K.M., Talhouni, A.A. & Alim, A.A.M.A. Design and synthesis of new 8-anilide theophylline derivatives as bronchodilators and antibacterial agents. Arch. Pharm. Res. 35, 1355–1368 (2012). https://doi.org/10.1007/s12272-012-0805-4
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DOI: https://doi.org/10.1007/s12272-012-0805-4