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

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...

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Detalles Bibliográficos
Autores principales: Kombu, Rajan Subramanian, Mailavaram, Raghu Prasad, Devalapally, Harikrishna, Chinnappa, Prabhakar Marsanapalli, Devarakonda, Rama Krishna, Akkinepally, Raghu Ram Rao
Formato: Texto
Lenguaje:English
Publicado: Bentham Open 2008
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2705134/
https://www.ncbi.nlm.nih.gov/pubmed/19662150
http://dx.doi.org/10.2174/1874104500802010101
Descripción
Sumario: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%).

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