Methylxanthines especially theophylline have been recognized as potent bronchodilators for the relief of acute asthma for over 50 years. Recently, it was found that bacterial infection has a role in asthma pathogenesis. Accordingly, the present work involves the synthesis of different series of 8-substituted (aryl, aralkyl, cycloalkyl, and heteroaryl)-1,3-dimethylxanthines. The chemical structures of these compounds were elucidated by IR, 1H NMR, 13C NMR, elemental analyses, and high resolution EI-MS or FAB-MS for some compounds. 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, 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 have potent antibacterial activity. A pharmacophore model was computed to get useful insight on the essential structural features of bronchodilator activity.
Elgaher, W., Hayallah, A., Salem, O., & Abdel Alim, A. A. (2009). SYNTHESIS, ANTI-BRONCHOCONSTRICTIVE, AND ANTIBACTERIAL ACTIVITIES OF SOME NEW 8- SUBSTITUTED-1,3-DIMETHYLXANTHINE DERIVATIVES. Bulletin of Pharmaceutical Sciences Assiut University, 32(1), 153-187. doi: 10.21608/bfsa.2009.63355
MLA
Walid A. Elgaher; Alaa M. Hayallah; Ola I. A. Salem; Abdel Alim M. Abdel Alim. "SYNTHESIS, ANTI-BRONCHOCONSTRICTIVE, AND ANTIBACTERIAL ACTIVITIES OF SOME NEW 8- SUBSTITUTED-1,3-DIMETHYLXANTHINE DERIVATIVES". Bulletin of Pharmaceutical Sciences Assiut University, 32, 1, 2009, 153-187. doi: 10.21608/bfsa.2009.63355
HARVARD
Elgaher, W., Hayallah, A., Salem, O., Abdel Alim, A. A. (2009). 'SYNTHESIS, ANTI-BRONCHOCONSTRICTIVE, AND ANTIBACTERIAL ACTIVITIES OF SOME NEW 8- SUBSTITUTED-1,3-DIMETHYLXANTHINE DERIVATIVES', Bulletin of Pharmaceutical Sciences Assiut University, 32(1), pp. 153-187. doi: 10.21608/bfsa.2009.63355
VANCOUVER
Elgaher, W., Hayallah, A., Salem, O., Abdel Alim, A. A. SYNTHESIS, ANTI-BRONCHOCONSTRICTIVE, AND ANTIBACTERIAL ACTIVITIES OF SOME NEW 8- SUBSTITUTED-1,3-DIMETHYLXANTHINE DERIVATIVES. Bulletin of Pharmaceutical Sciences Assiut University, 2009; 32(1): 153-187. doi: 10.21608/bfsa.2009.63355
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