新型功能化1,3,4-噻二唑-2-芳基腙衍生物的合成及其抗锥虫活性，设计为非诱变的美唑类似物。
Synthesis and antitrypanosomal profile of new functionalized 1,3,4-thiadiazole-2-arylhydrazone derivatives, designed as non-mutagenic megazol analogues.
作者信息
Carvalho Samir A, da Silva Edson F, Santa-Rita Ricardo M, de Castro Solange L, Fraga Carlos A M
机构信息
Instituto de Química, Universidade Federal do Rio de Janeiro, 21949900 Rio de Janeiro, RJ, Brazil.
出版信息
Bioorg Med Chem Lett. 2004 Dec 20;14(24):5967-70. doi: 10.1016/j.bmcl.2004.10.007.
In this work we reported the synthesis and the trypanocidal profile of new 1,3,4-thiadiazole-2-arylhydrazone derivatives of nitroimidazole series (4) or phenyl series (5), designed by exploring the molecular hybridization approach between megazol (2) and guanyl hydrazone derivative (3). The evaluation of the activity against bloodstream trypomastigote forms of Trypanosoma cruzi forms lead us to identify a new potent trypamomicide prototype, that is, brazilizone A (4k), which present an IC50/24 h=5.3 microM.
在本研究中，我们报道了通过探索美他唑（2）与胍基腙衍生物（3）之间的分子杂交方法设计的新型硝基咪唑系列（4）或苯基系列（5）的1,3,4 - 噻二唑 - 2 - 芳基腙衍生物的合成及其杀锥虫活性。对克氏锥虫血液中锥鞭毛体形式的活性评估使我们鉴定出一种新的强效杀锥虫原型，即巴西利酮A（4k），其24小时半数抑制浓度（IC50）=5.3微摩尔。
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