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Vol. 26 No. 24 (2014)

Copyright (c) 2014 R.A. Al-Salahi1, I.A. Alswaidan1, M.S. Marzouk1, W. El-Eraky3, D. Saleh3

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This work is licensed under a Creative Commons Attribution 4.0 International License.

Antihistamine Activity of 1,2,4-Triazolo[1,5-a]quinazolines

https://doi.org/10.14233/ajchem.2014.18581
R.A. Al-Salahi1
1Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia 2Chemistry of Natural Products Group, Center of Excellence for Advanced Analytical Sciences, National Research Center, Dokki 12622, Cairo, Egypt 3Pharmacology Depatement, National Research Center, Dokki 12622, Cairo, Egypt *Corresponding author: E-mail: msmarzouk@yahoo.co.uk
I.A. Alswaidan1
1Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia 2Chemistry of Natural Products Group, Center of Excellence for Advanced Analytical Sciences, National Research Center, Dokki 12622, Cairo, Egypt 3Pharmacology Depatement, National Research Center, Dokki 12622, Cairo, Egypt *Corresponding author: E-mail: msmarzouk@yahoo.co.uk
M.S. Marzouk1
1Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia 2Chemistry of Natural Products Group, Center of Excellence for Advanced Analytical Sciences, National Research Center, Dokki 12622, Cairo, Egypt 3Pharmacology Depatement, National Research Center, Dokki 12622, Cairo, Egypt *Corresponding author: E-mail: msmarzouk@yahoo.co.uk
W. El-Eraky3
1Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia 2Chemistry of Natural Products Group, Center of Excellence for Advanced Analytical Sciences, National Research Center, Dokki 12622, Cairo, Egypt 3Pharmacology Depatement, National Research Center, Dokki 12622, Cairo, Egypt *Corresponding author: E-mail: msmarzouk@yahoo.co.uk
D. Saleh3
1Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451, Saudi Arabia 2Chemistry of Natural Products Group, Center of Excellence for Advanced Analytical Sciences, National Research Center, Dokki 12622, Cairo, Egypt 3Pharmacology Depatement, National Research Center, Dokki 12622, Cairo, Egypt *Corresponding author: E-mail: msmarzouk@yahoo.co.uk

Corresponding Author(s) : R.A. Al-Salahi1

Asian Journal of Chemistry, Vol. 26 No. 24 (2014)

Abstract

This work was aimed to study and evaluate the antihistamine activity (bronchodilation) for prepared series of 1,2,4-triazolo[1,5-a]quinazolines. Screening of the bronchodilation activity of 1,2,4-riazoloquinazolines (1-27) was investigated in vitro using isolated thoracic tracheal rings of male guinea pigs pre-contracted with histamine. Screening procedure of bronchodilation test was performed in light to the standard reported method by examining the effects of the target molecules on isolated thoracic tracheal rings of male guinea pigs. The observed bronchodilation screening results are recorded and the potency (IC50) was determined in mM in comparison with theophylline as a reference drug. The tested triazoloquinazolines have exhibited promising antihistaminic activity against histamine-induced bronchospasm. Our findings have shown that compounds 2, 3, 11, 20 and 21 were found to possess the highest activity and could be useful as templates for further development through modification or derivatization to design more potent antihistamine.

Keywords

Triazoloquinazolines Bronchodilation Histamine Theophylline Bronchospasm Tracheal rings.
Al-Salahi1, R., Alswaidan1, I., Marzouk1, M., El-Eraky3, W., & Saleh3, D. (2014). Antihistamine Activity of 1,2,4-Triazolo[1,5-a]quinazolines. Asian Journal of Chemistry, 26(24), 8625–8627. https://doi.org/10.14233/ajchem.2014.18581
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