Synthesis of new chalcone derivatives containing acridinyl moiety with potential antimalarial activity
作者:V. Tomar、G. Bhattacharjee、Kamaluddin、S. Rajakumar、Kumkum Srivastava、S.K. Puri
DOI:10.1016/j.ejmech.2009.11.022
日期:2010.2
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
通过各种3'-氨基查耳酮或4'-氨基查耳酮与9-氯chloro啶之间的非催化亲核芳族取代反应,合成了一系列新颖的查耳酮,查耳酮在其环A的氨基上带有连接有a啶基的部分。已经表征了合成的查耳酮衍生物,并针对恶性疟原虫NF-54的体外抗疟活性进行了筛选。所有的查耳酮在10μg/ mL及以上的浓度下均显示出完全的抑制作用,而三种化合物在2μg/ mL的浓度下均显示出明显的抑制作用。还筛选了三种活性最高的查尔酮衍生物的体内活性,但腹膜内给予时,未观察到对寄生虫血症的显着抑制作用。约氏疟原虫感染的小鼠模型。