合成及一些新的噻二唑并[3,4-b:4′,5′-d]噻唑磷杂环戊二烯、噻二唑并[3,4-b:4′,5′-d]三唑磷杂环戊二烯和噻二唑并[3,4-b:4′,5′-d]四唑磷杂环戊二烯中 1,2,4-三嗪酮部分的抗菌活性。
Synthesis and antibacterial activity of some new thiadiaza/triazaphospholes, thiadiaza/triaza/tetrazaphosphinines and thiadiaza/tetrazaphosphepines containing 1,2,4-triazinone moiety.
机构信息
Department of Chemistry, Faculty of Education, Ain Shams University, Roxy, 11711 Cairo, Egypt.
出版信息
Eur J Med Chem. 2009 Nov;44(11):4539-46. doi: 10.1016/j.ejmech.2009.06.022. Epub 2009 Jun 27.
Some new thiadiaza/triazaphospholes, thiadiaza/triaza/tetrazaphosphinines and thiadiaza/tetrazaphosphepines fused with 6-methyl-1,2,4-triazin-5-one moiety were synthesized via reactions of alpha,beta-bifunctional compounds derived from 4-amino-3-mercapto-6-methyl-1,2,4-triazin-5(4H)-one (1) with various phosphorus reagents. The in vitro antibacterial activities of the synthesized compounds were evaluated against some bacterial strains. Compounds 16 and 21 exhibited good inhibitory activities against most the tested organisms with MIC values in the range 6.25-12.5 microg/mL and lower cytotoxicity in comparison with the reference drugs.
一些新的噻二唑/三唑磷杂环戊烯、噻二唑/三唑/四氮磷杂环戊二烯和噻二唑/四氮磷杂环戊二烯与 6-甲基-1,2,4-三嗪-5-酮部分融合，通过α，β-官能化化合物与各种磷试剂反应合成，该化合物衍生自 4-氨基-3-巯基-6-甲基-1,2,4-三嗪-5(4H)-酮（1）。合成化合物的体外抗菌活性针对一些细菌菌株进行了评估。化合物 16 和 21 对大多数测试的生物体表现出良好的抑制活性，MIC 值在 6.25-12.5μg/mL 范围内，与参比药物相比细胞毒性较低。
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