Ramazani Ali, Khosravani Behnam, Taran Jafar, Ramazani Ali
Zanjan Pharmaceutical Biotechnology Research Center, Zanjan University of Medical Sciences, Zanjan, Iran.
Department of Chemistry, University of Zanjan, Zanjan, Iran.
Iran J Pharm Res. 2017 Summer;16(3):924-928.
Because of expanding resistance to efficient and affordable antimalarial drugs like chloroquine, the search is continuing for more effective drugs against this disease. antiplasmodial activity and cytotoxicity of α-(acyloxy)-α-(quinolin-4-yl) acetamides on and structure-activity relationships of this new class of Passerini adducts is described. The antiplasmodial activity of compounds was tested against chloroquine sensitive 3D7 strain. Toxicity of active compounds was investigated on HepG2 cell line. Compounds 1, 20 and 22 showed significant antiplasmodial activity with IC value of 1.511, 1.373 and 1.325 µM, respectively. The active compounds did not show noticeable toxicity when tested against HepG2 cell line. The present results bring essential elements which will be used for the synthesis of more active derivatives of α-(acyloxy)-α-(quinolin-4-yl) acetamides.
由于对氯喹等高效且价格合理的抗疟药物的耐药性不断增加，人们仍在继续寻找针对这种疾病的更有效药物。本文描述了α-(酰氧基)-α-(喹啉-4-基)乙酰胺类化合物的抗疟活性和细胞毒性，以及这类新型Passerini加合物的构效关系。化合物的抗疟活性针对氯喹敏感的3D7菌株进行了测试。对活性化合物在HepG2细胞系上的毒性进行了研究。化合物1、20和22表现出显著的抗疟活性，IC值分别为1.511、1.373和1.325μM。活性化合物在针对HepG2细胞系进行测试时未显示出明显的毒性。目前的结果为合成α-(酰氧基)-α-(喹啉-4-基)乙酰胺类更具活性的衍生物提供了重要元素。
