SYNTHESIS, ANTI-BRONCHOCONSTRICTIVE, AND ANTIBACTERIAL ACTIVITIES OF SOME NEW 8- SUBSTITUTED-1,3-DIMETHYLXANTHINE DERIVATIVES | ||||
| Bulletin of Pharmaceutical Sciences Assiut University | ||||
| Article 8, Volume 32, Issue 1, June 2009, Page 153-187 PDF (797.52 K) | ||||
| Document Type: Original Article | ||||
| DOI: 10.21608/bfsa.2009.63355 | ||||
 View on SCiNiTO | ||||
| Authors | ||||
| Walid A. Elgaher; Alaa M. Hayallah* ; Ola I. A. Salem; Abdel Alim M. Abdel Alim | ||||
| Department of Pharmaceutical Organic Chemistry, Faculty of Pharmacy, Assiut University, Assiut 71526, Egypt | ||||
| Abstract | ||||
| 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. | ||||
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