...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Archiv der Pharmazie >Synthesis and antibacterial activity of novel fused 1,3-thiazoles and 1,3-thiazines incorporating a 2,4-dihydroxyphenyl residue
【24h】

Synthesis and antibacterial activity of novel fused 1,3-thiazoles and 1,3-thiazines incorporating a 2,4-dihydroxyphenyl residue

机译：新型2,4-二羟基苯基残基稠合的1,3-噻唑和1,3-噻嗪的合成及其抗菌活性

获取原文
获取原文并翻译 | 示例
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

In an attempt to find a new class of antimicrobial agents, a series of benzothiazoles, 1,3-thiazolo[5,4-b]pyridines, 4H-3,1-benzothiazines, naphtho[2,3-d][1,3]thiazole-4,9-diones and other related compounds containing a 2,4-dihydroxyphenyl moiety were prepared. They were obtained via the reaction of aryl-modified sulfinyl[bis(2,4-dihydroxyphenylmethanethione)]s with appropriate commercial chemical reagents in the endocyclization processes. The MIC values of the compounds towards eight reference bacterial strains were assessed by the two-fold serial micro-dilution broth method. They exhibited inhibitory effects against the Gram-positive strains tested opposite to Gram-negative ones. Some compounds were more effective than the reference drug. 4-(6-Chloro-4H-3,1- benzothiazin-2-yl)-6-methylbenzene-1,3-diol (5b) due to its very good activity (MIC from 1.56 to 3.13 μg/mL) and low cytotoxicity (IC 50 50 μg/mL) may be regarded as a promising precursor for the development of novel antibacterial agents. A series of benzothiazoles, 1,3-thiazolo[5,4-b]pyridines, 4H-3,1-benzothiazines, naphtho[2,3-d][1,3]thiazole-4,9-diones and other related compounds containing a 2,4-dihydroxyphenyl moiety were prepared and their MIC values towards eight reference bacterial strains were determined. 4-(6-Chloro-4H-3,1-benzothiazin-2-yl)-6-methylbenzene-1,3-diol may be regarded as a promising precursor for the development of novel antibacterial agents.
机译：为了找到一类新的抗菌剂，一系列苯并噻唑，1,3-噻唑并[5,4-b]吡啶，4H-3,1-苯并噻嗪，萘并[2,3-d] [1，制备了3]噻唑-4，9-二酮和其他含有2，4-二羟基苯基部分的相关化合物。它们是通过芳基修饰的亚磺酰基[双（2,4-二羟基苯基甲烷硫酮）] s与适当的工业化学试剂在环化过程中反应获得的。通过两次连续微量稀释肉汤法评估化合物对八种参考细菌菌株的MIC值。他们对与革兰氏阴性菌株相反的革兰氏阳性菌株表现出抑制作用。一些化合物比参考药物更有效。 4-（6-氯4H-3,1-苯并噻嗪-2-基）-6-甲基苯-1,3-二醇（5b）由于其非常好的活性（MIC从1.56至3.13μg/ mL）而低细胞毒性（IC 50> 50μg/ mL）可被视为开发新型抗菌剂的有希望的前体。一系列苯并噻唑，1,3-噻唑并[5,4-b]吡啶，4H-3,1-苯并噻嗪，萘并[2,3-d] [1,3]噻唑-4,9-二酮等制备了含有2,4-二羟基苯基部分的化合物，并确定了它们对八种参考细菌菌株的MIC值。 4-（6-氯-4H-3,1-苯并噻嗪-2-基）-6-甲基苯-1,3-二醇可被视为开发新型抗菌剂的有前途的前体。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号