Год выпуска: 2011 Автор: Walid Ali Mahmoud Elgaher Издательство: LAP Lambert Academic Publishing Страниц: 204 ISBN: 9783845401331
Описание
Methylxanthines especially theophylline have been recognized as potent bronchodilators for the relief of acute asthma for over 65 years. Recently, it was found that bacterial infection plays a role in asthma pathogenesis. Accordingly, the present work involves the synthesis of different series of 8-substituted theophylline derivatives as novel antiasthmatic candidates with potential antibacterial activity. A pharmacophore model was constructed to get useful insight into the essential structural features of bronchodilator activity. Forty-six of the target compounds were investigated for in vivo antiasthmatic activity using aminophylline as a reference standard. Antibacterial activity of all the target compounds was investigated in vitro against both Gram-positive and Gram-negative bacterial strains using ampicillin as a reference standard. Acute toxicity study was also performed. It is noteworthy to mention that compounds 6c, 8i1, and 14c combined both promising antiasthmatic and...
