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Updated: Feb 23, 2026
Bronchial Thermoplasty: A Novel Therapeutic Approach to Severe Asthma
Published on: November 4, 2010
Identification of some novel xanthine-based derivatives with bronchodilator activity
Abdalla R Mohamed1, Hanan H Georgey2, Riham F George2
1Pharmaceutical Chemistry Department, Faculty of Pharmacy, Egyptian Russian University, Badr City, Cairo 11829, Egypt.
Aim:
The discovery of new bronchodilators with higher efficacy than theophylline is an important issue for asthmatic patients.
Materials & Methods:
Theophylline 2, 8-bromotheophylline 4 and theobromine 6 were reacted with different 2/3-chloro-N-phenylacetamides 1a-d or their propanamide analogs 1e-g to obtain 3a-g, 5a-g and 7a-g, respectively. The target compounds were screened for their in vitro bronchodilator activity using isolated guinea pig tracheal rings precontracted with histamine and compared with their precursors.
Results:
Many compounds exhibited promising activity especially 3d, 3f, 5d, 7d and 7e. 2D-QSAR study resulted in a significant model (N = 24, n = 5, R 2 = 0.848, R 2cvOO = 0.748, R 2cvMO = 0.745, F = 21.215, s 2 = 0.0002) using CODESSA-Pro software.
Conclusion:
These compounds can be considered as promising hits for potent bronchodilators that may be useful for further investigations. [Formula: see text].
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