The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines
The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines
复制标题
DOI：
10.1016/j.ejmech.2017.07.060
复制
发表时间：
2017-09-29
影响因子：
6.7
通讯作者：
Kaiser, Marcel
中科院分区：
文献类型：
--
作者：
Papadopoulou, Maria V.;Bloomer, William D.;Kaiser, Marcel
合成了有限数量的新型 3-硝基三唑和 2-硝基咪唑连接的喹啉和喹唑啉，并筛选其体外抗锥虫和抗结核活性以及正常细胞的细胞毒性。所有化合物均对克氏锥虫无鞭毛体有活性，而除一种外，所有化合物均对锥虫有活性或中等活性。罗德西亚。然而，只有两种氯喹啉对克氏锥虫表现出令人满意的选择性指数（SI），并且只有其中一种对T.b表现出令人满意的SI。罗德西亚。所有测试的化合物对需氧 Mtb 的最低抑制浓度 (MIC) >= 200 mu M。然而，基于 2-硝基咪唑的类似物对低氧 Mtb 具有活性，MIC 值为 2.89-9.18 μM。目前的数据支持我们之前的观察结果，即基于 2-硝基咪唑的芳香胺对非复制型 Mtb 具有选择性活性，而基于 3-硝基三唑的芳香胺是有效的抗恰加斯剂。 (C) 2017 Elsevier Masson SAS。版权所有。
A limited number of novel 3-nitrotriazole- and 2-nitroimidazole-linked quinolines and quinazolines were synthesized and screened for in vitro antitrypanosomal and antitubercular activities as well as cytotoxicity in normal cells. All compounds were active against T. cruzi amastigotes, while all but one were active or moderately active against T.b. rhodesiense. However, only two chloroquinolines exhibited satisfactory selectivity indices (SI) against T cruzi and only one of them demonstrated a satisfactory SI against T.b. rhodesiense. All tested compounds demonstrated a Minimum Inhibitory Concentration (MIC) >= 200 mu M against aerobic Mtb. However, the 2-nitroimidazole-based analogs were active against hypoxic Mtb with MIC values 2.89-9.18 mu M. The present data support our previous observations that 2-nitroimidazole-based aromatic amines are selectively active against nonreplicating Mtb, while 3-nitrotriazole-based aromatic amines are potent antichagasic agents. (C) 2017 Elsevier Masson SAS. All rights reserved.