Sharma Moni, Chauhan Kuldeep, Srivastava Rajeev K, Singh Shiv V, Srivastava Kumkum, Saxena Jitendra K, Puri Sunil K, Chauhan Prem M S
Medicinal and Process Chemistry Division, CSIR-Central Drug Research Institute, Lucknow, 226031, India.
Chem Biol Drug Des. 2014 Aug;84(2):175-81. doi: 10.1111/cbdd.12289. Epub 2014 Mar 13.
A series of novel 4-aminoquinolinyl and 9-anilinoacridinyl Schiff base hydrazones have been synthesized and evaluated for their antimalarial activity. All compounds were evaluated in vitro for their antimalarial activity against chloroquine-sensitive strain 3D7 and the chloroquine-resistant K1 strain of Plasmodium falciparum and for cytotoxicity toward Vero cells. Compounds 17, 20, and 21 displayed good activity against the 3D7 strain with IC50 values ranging from 19.69 to 25.38 nm. Moreover, compounds 16, 17, 21, 24, 32, and 33 exhibited excellent activities (21.64-54.26 nm) against K1 strain and several compounds displayed β-hematin inhibitory activity, suggesting that they act on the heme crystallization process such as CQ. Compounds were also found to be non-toxic with good selectivity index.
合成了一系列新型的4-氨基喹啉基和9-苯胺基吖啶基席夫碱腙，并对其抗疟活性进行了评估。所有化合物均在体外针对氯喹敏感株3D7和恶性疟原虫的氯喹抗性K1株进行了抗疟活性评估，并对Vero细胞进行了细胞毒性评估。化合物17、20和21对3D7株显示出良好的活性，IC50值范围为19.69至25.38纳米。此外，化合物16、17、21、24、32和33对K1株表现出优异的活性（21.64 - 54.26纳米），并且几种化合物表现出β-血红素抑制活性，表明它们作用于血红素结晶过程，如氯喹。还发现这些化合物无毒且具有良好的选择性指数。
