Guarda V L, Perrissin M, Thomasson F, Ximenes E A, Galdino S L, Pitta I R, Luu-Duc C
Escola de Farmácia, Universidade Federal de Ouro Preto, MG, Brazil.
Farmaco. 2001 Sep;56(9):689-93. doi: 10.1016/s0014-827x(01)01113-2.
The synthesis and physicochemical properties of 4-butyl-2H-benzo[1,4]thiazin-3-one derivatives are described. These new compounds were synthesised by alkylation in 4-N position and acylation and/or alkylation of 6-NH2 by phase transfer catalysis. Acid hydrolysis of 6-alkylacylamino group yielded 6-alkylamino-4-butyl-2H-benzo[1,4]thiazin-3-ones. The antimicrobial in vitro activity was determined on five compounds.
描述了4-丁基-2H-苯并[1,4]噻嗪-3-酮衍生物的合成及其物理化学性质。这些新化合物是通过在4-N位进行烷基化以及通过相转移催化对6-NH2进行酰化和/或烷基化反应合成的。6-烷基酰氨基的酸水解产生了6-烷基氨基-4-丁基-2H-苯并[1,4]噻嗪-3-酮。对五种化合物测定了体外抗菌活性。
