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. 2008 Dec 17:2:101-11.
doi: 10.2174/1874104500802010101.

Synthesis and Bronchodilator Studies of Some Novel 6-Alkyl/Aryl-1,2,4-Triazino[4,3-c]Quinazolines

Rajan Subramanian Kombu  1 , Raghu Prasad Mailavaram, Harikrishna Devalapally, Prabhakar Marsanapalli Chinnappa, Rama Krishna Devarakonda, Raghu Ram Rao Akkinepally
Affiliations

Synthesis and Bronchodilator Studies of Some Novel 6-Alkyl/Aryl-1,2,4-Triazino[4,3-c]Quinazolines

Rajan Subramanian Kombu et al. Open Med Chem J. .

Abstract

A series of alkyl- and aryl-1,2,4-triazino[4,3-c]quinazolines (5a-h and 8a-h) were synthesized and characterized. The title compounds were evaluated for their in vivo bronchodilator activity on guinea pigs. All the test compounds exhibited good protection against histamine-induced bronchospasm. The structure-activity relationships based on the results obtained for these series were studied. Incorporation of an aryl ring with halo substitution to the theophylline bioisostere increases its potency. Among the compounds tested, 5b was found to be the most potent with 88.7% protection against histamine-induced bronchospasm compared to the standard compound aminophylline (87.8%).

Keywords: 1,2,4-Triazino[4,3-c]quinazolines.; Bioisostere; Bronchodilators; Structure activity relationship studies.

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Figures

Fig. (1).
Fig. (1).
Proposed hypothetical model towards the development of xanthine-based but non-xanthine heterocycles.
Fig. (2).
Fig. (2).
Synthesis of 6-alkyl-1,2,4-triazino[4,3-c]quinazolines 5(a-h).
Fig. (3).
Fig. (3).
Synthesis of 6-aryl-1,2,4-triazino[4,3-c]quinazolines (8a-h).
See this image and copyright information in PMC

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