Alaa M. Hayallah, Suzan A. Isper and Amira S. Al-Okosh.
Chronic airway inflammation plays a key role in asthma. This fundamental feature has been included in the most recent definitions of the disease. 8-substituted ronchodi especially theophylline derivatives are well known as potent bronchodilators for the relief of acute asthma and play pronounced role in inflammation process. The present work involves the design and synthesis of new 8-substituted theophylline derivatives. The chemical structures of these compounds were elucidated by IR, 1H NMR, elemental analyses, and FAB-MS spectral data. 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 aminophylline as a standard. Also, anti-inflammatory activity of the target compounds was investigated using indomethacin as a reference drug. Results showed that some of the tested compounds have good anti-inflammatory activity. A pharmacophore model was computed to get useful insight on the essential structural features of bronchodilator activity.
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