Department of Chemistry, Indian Institute of Technology Roorkee, Roorkee-247667, Uttarakhand, India.
Eur J Med Chem. 2010 Feb;45(2):745-51. doi: 10.1016/j.ejmech.2009.11.022. Epub 2009 Nov 20.
A series of novel chalcones bearing acridine moiety attached to the amino group in their ring A have been synthesized through noncatalyzed nucleophilic aromatic substitution reaction between various 3'-aminochalcone or 4'-aminochalcones and 9-chloroacridine. The synthesized chalcone derivatives have been characterized and screened for in vitro antimalarial activity against Plasmodium falciparum NF-54. All the chalcones showed complete inhibition at concentration of 10 microg/mL and above while three compounds showed significant inhibition at concentration of 2 microg/mL. The three most active chalcone derivatives were screened for in vivo activity as well, but no significant inhibition in parasitaemia was observed when given intraperitoneally to Plasmodium yoelii infected mice model.
一系列新型查耳酮通过各种 3'-氨基查尔酮或 4'-氨基查尔酮与 9-氯吖啶在环 A 的氨基上的非催化亲核芳香取代反应合成。合成的查尔酮衍生物已被表征并筛选对体外抗疟原虫活性对恶性疟原虫 NF-54。所有查尔酮在浓度为 10 μg/mL 及以上时表现出完全抑制，而三种化合物在浓度为 2 μg/mL 时表现出显著抑制。对三种最活跃的查尔酮衍生物进行了体内活性筛选，但在给感染疟原虫耶氏疟原虫的小鼠模型腹腔内给药时，没有观察到寄生虫血症的显著抑制。
