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[摘要]：There is challenge and urgency to synthesize cost-effective chemotherapeutic agents for treatment of malaria after the widespread development of resistance to CQ. In the present study, we synthesized a new series of hybrid 9-anilinoacridine triazines using the cheap chemicals 6,9-dichloro-2-methoxy acridine and cyanuric chloride. The series of new hybrid 9-anilinoacridine triazines were evaluated in vitro for their antimalarial activity against CQ-sensitive 3D7 strain of Plasmodium falciparum and their cytotoxicity were determined on VERO cell line. Of the evaluated compounds, two compounds 17 (IC50 = 4.21 nM) and 22 (IC50 = 4.27 nM) displayed two times higher potency than CQ (IC50 = 8.15 nM). Most of the compounds showed fairly high selectivity index. The compounds 13 and 29 displayed > 96.59% and 98.73% suppression, respectively, orally against N-67 strain of Plasmodium yoelii in swiss mice at dose 100 mg/kg for four days. (C) 2009 Elsevier Ltd. All rights reserved. |
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