• 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Open Chemistry Journal >Synthesis and Biological Evaluation of Novel Antihypertensive Compounds
【24h】

Synthesis and Biological Evaluation of Novel Antihypertensive Compounds

机译：新型抗高血压化合物的合成及生物学评价

获取原文
           
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Hypertension has been associated as a pathogenesis involved in the renin angiotensin system. The most commonly used drug to block the AT1R, is Losartan which has specific pharmacophore groups such as imidazole and biphenyl. However the development of new selective antagonists would be advantagous to improving the treatment of hypertension. We investigated innovative antihypertensive candidates 1-3 using in vitro and in vivo assays. Although only Compound 2 showed low affinity to the AT1R, it had no effect on blood pressure. Compound 1 produced a reduction in blood pressure and this effect seems to be mediated through ACE inhibition and not the blockage of the AT1R. Compound 1 was able to inhibit the ACE activity in a similar way to captopril, while Compounds 2 and 3 showed no effect on the enzyme activity.Further studies need to be conducted to understand the mechanisms involved as well as signaling pathways.
机译：高血压已被认为与肾素血管紧张素系统有关。阻断AT1R最常用的药物是Losartan，它具有特定的药效团，例如咪唑和联苯。然而，新的选择性拮抗剂的开发将有利于改善高血压的治疗。我们使用体外和体内试验研究了创新的降压候选药物1-3。尽管仅化合物2对AT1R表现出低亲和力，但对血压没有影响。化合物1降低了血压，这种作用似乎是通过ACE抑制而不是AT1R的阻断来介导的。化合物1能够以类似于卡托普利的方式抑制ACE活性，而化合物2和3则对酶的活性没有影响。还需要进行进一步的研究以了解涉及的机制以及信号传导途径。

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