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Novel bronchodilators: Synthesis, transamination reactions, and pharmacology of a series of pyrazino[2,3-c][1,2,6]thiadiazine 2,2-dioxides

AuthorsCampillo, Nuria E. ; García, Concepción; Goya, Pilar ; Alkorta, Ibon ; Páez, Juan A.
Issue Date2-Nov-2000
PublisherAmerican Chemical Society
CitationJournal of Medicinal Chemistry 43 : 4219-4227 (2000)
AbstractThe synthesis, pharmacological evaluation, and structure-activity relationships of a new class of bronchodilator agents, derivatives of pyrazino[2,3-c][1,2,6]thiadiazine 2,2-dioxides are described. The compounds were prepared by reaction of 3,4,5-triamino-1,2,6-thiadiazine 1,1- dioxide with suitable 1,2-dicarbonyl compounds or R-hydroxyiminoketones and subsequent N-alkylation. A transamination procedure for synthesizing derivatives with different substituents at the 4-amino group is reported for the first time. The pyrazino[2,3-c][1,2,6]thiadiazine derivatives were screened for tracheal relaxing activity in vitro, and the active compounds were evaluated in vivo in guinea pigs as bronchodilator agents in comparison to theophylline. Among the compounds studied, the most interesting properties were displayed by the 4-amino- 1-ethyl-6-methyl derivative (21). The toxicological evaluation of this derivative is also reported.
Publisher version (URL)http://dx.doi.org/10.1021/jm000970x
Appears in Collections:(IQM) Artículos
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