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Identification of Some Novel Xanthine-Based Derivatives With Bronchodilator Activity

Identification of Some Novel Xanthine-Based Derivatives With Bronchodilator Activity

Abdalla R Mohamed, Hanan H Georgey, Riham F George, Wafaa I El-Eraky, Dalia O Saleh, Nagwa M Abdel Gawad

Future Med Chem. 2017 Oct;9(15):1731-1747.

PMID: 28871831

Abstract:

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].

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP10381756	8-Bromotheophylline		10381-75-6	Price

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