Benzoxazine derivatives of phytophenols show anti-plasmodial activity via sodium homeostasis disruption
作者: Vijeta SharmaNagarjuna AmarnathSwapnil ShuklaR. AyanaNaveen KumarNisha YadavDeepika KannanSeema SehrawatSoumya PatiBimlesh LochabShailja Singh
作者单位: 1Department of Life Sciences, Shiv Nadar University, Gautam Buddha Nagar UP, 201314, India
2Department of Chemistry, Shiv Nadar University, Gautam Buddha Nagar UP, 201314, India
3Special Centre for Molecular Medicine, Jawaharlal Nehru University, New Delhi 110067, India
刊名: Bioorganic & Medicinal Chemistry Letters, 2018, Vol.28 (9), pp.1629-1637
来源数据库: Elsevier Journal
DOI: 10.1016/j.bmcl.2018.03.047
关键词: EugenolBenzoxazinePlasmodium falciparumSodium homeostasisP-type cation ATPase
英文摘要: Abstract(#br)Development of new class of anti-malarial drugs is an essential requirement for the elimination of malaria. Bioactive components present in medicinal plants and their chemically modified derivatives could be a way forward towards the discovery of effective anti-malarial drugs. Herein, we describe a new class of compounds, 1,3-benzoxazine derivatives of pharmacologically active phytophenols eugenol (compound 3 ) and isoeugenol (compound 4 ) synthesised on the principles of green chemistry, as anti-malarials. Compound 4 , showed highest anti-malarial activity with no cytotoxicity towards mammalian cells. Compound 4 induced alterations in the intracellular Na + levels and mitochondrial depolarisation in intraerythrocytic Plasmodium falciparum leading to cell death. Knowing...
全文获取路径: Elsevier  (合作)
影响因子:2.338 (2012)

  • homeostasis 体内平衡
  • disruption 破裂
  • plasmodial 合胞体的
  • sodium 
  • activity 活度
  • derivatives 派生物
  • cation 阳离子
  • ATPase ATP酶