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Kombu RS, Mailavaram RP, Devalapally H, et al. Synthesis and Bronchodilator Studies of Some Novel 6-Alkyl/Aryl-1,2,4-Triazino[4,3-c]Quinazolines. Open Med Chem J. 2008;2:101-11doi: 10.2174/1874104500802010101.
Kombu, R. S., Mailavaram, R. P., Devalapally, H., Chinnappa, P. M., Devarakonda, R. K., & Akkinepally, R. R. (2008). Synthesis and Bronchodilator Studies of Some Novel 6-Alkyl/Aryl-1,2,4-Triazino[4,3-c]Quinazolines. The open medicinal chemistry journal, 2101-11. https://doi.org/10.2174/1874104500802010101
Kombu, Rajan Subramanian, et al. "Synthesis and Bronchodilator Studies of Some Novel 6-Alkyl/Aryl-1,2,4-Triazino[4,3-c]Quinazolines." The open medicinal chemistry journal vol. 2 (2008): 101-11. doi: https://doi.org/10.2174/1874104500802010101
Kombu RS, Mailavaram RP, Devalapally H, Chinnappa PM, Devarakonda RK, Akkinepally RR. Synthesis and Bronchodilator Studies of Some Novel 6-Alkyl/Aryl-1,2,4-Triazino[4,3-c]Quinazolines. Open Med Chem J. 2008 Dec 17;2:101-11. doi: 10.2174/1874104500802010101. PMID: 19662150; PMCID: PMC2705134.
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Open Med Chem J. 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.

The open medicinal chemistry journal

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

Affiliations

  1. Medicinal Chemistry Research Division, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, AP-506 009, India.

PMID: 19662150 PMCID: PMC2705134 DOI: 10.2174/1874104500802010101

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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