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Synthesis of 9-anilinoacridine triazines as new class of hybrid antimalarial agents.

Author(s): 
Ashok Kumar, Kumkum Srivastava, S. Raja Kumar, S.K. Puri, Prem M.S. Chauhan
Reference: 
Bioorganic & Medicinal Chemistry Letters, Volume 19, Issue 24, 15 December 2009, Pages 6996-6999, doi:10.1016/j.bmcl.2009.10.010

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.