首页> 外文期刊>Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents >The synthesis, anti-inflammatory, and anti-microbial activity evaluation of new series of 4-(3-arylureido)phenyl-1,4-dihydropyridine urea derivatives
【24h】

The synthesis, anti-inflammatory, and anti-microbial activity evaluation of new series of 4-(3-arylureido)phenyl-1,4-dihydropyridine urea derivatives

机译:新系列4-(3-芳基脲基)苯基-1,4-二氢吡啶脲衍生物的合成,抗炎和抗菌活性评估

获取原文
获取原文并翻译 | 示例
           

摘要

A new series of 4-(3-arylureido)phenyl-l,4-dihydropyridine urea derivatives were synthesized using simple three component condensation, reduction, and nucle-ophilic addition sequence in moderate to good yields. All the synthesized compounds 6a-j were evaluated for their anti-inflammatory [against the pro-inflammatory cytokines (tumor necrosis factor-alpha, TNF-a and interleukin-6, IL-6)] and anti-microbial activity (anti-bacterial and anti-fungal). Among all the compound screened, the compound 6b, 6f, and 6} were found to have promising anti-inflammatory activity, 74-83 % TNF-a and 91-96 % IL-6 inhibitory activity, respectively as compared to the standard dexamethasone (71 and 86 % inhibition) but at the MIC of 10 uM/ml. The compounds 6d-e and 6h exhibited relatively lower TNF-a and IL-6 inhibitory activity and found to be moderately potent anti-inflammatory agents. The compounds 6c-e, 6g, and 6i were found to be promising anti-bacterial and anti-fungal agents and remarkably some of the new compounds, viz. 6d and 6i were found be more potent than the standard ciprofloxacin or miconazole. It is to be noted that this is the first report on the anti-inflammatory activity evaluation of novel 1,4-dihydropyridine urea derivatives against the important molecular target, TNF-a, and IL-6.
机译:使用简单的三组分缩合,还原和亲核加成顺序以中等至良好的收率合成了一系列新的4-(3-芳基脲基)苯基-1,4-二氢吡啶脲衍生物。评价所有合成的化合物6a-j的抗炎性[针对促炎性细胞因子(肿瘤坏死因子-α,TNF-α和白介素-6,IL-6)]和抗微生物活性(抗细菌和抗真菌剂)。在筛选的所有化合物中,与标准地塞米松相比,发现化合物6b,6f和6}具有良好的抗炎活性,分别具有74-83%TNF-a和91-96%IL-6抑制活性。 (抑制率为71%和86%),但MIC为10 uM / ml。化合物6d-e和6h表现出相对较低的TNF-α和IL-6抑制活性,并且被发现是中等有效的抗炎剂。发现化合物6c-e,6g和6i是有前途的抗菌剂和抗真菌剂,并且显然是一些新化合物,即。发现6d和6i比标准环丙沙星或咪康唑更有效。应当指出,这是关于新型1,4-二氢吡啶脲衍生物对重要分子靶标TNF-α和IL-6的抗炎活性评估的第一份报道。

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