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Volumn 19, Issue 24, 2009, Pages 6996-6999

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

Author keywords

9 Anilinoacridine triazine; Antimalarial; Plasmodium falciparum

Indexed keywords

6,9 DICHLORO 2 METHOXYACRIDINE; 9 ANILINOACRIDINE TRIAZINE DERIVATIVE; ACRIDINE DERIVATIVE; ANTIMALARIAL AGENT; CHLOROQUINE; CYANURIC ACID; UNCLASSIFIED DRUG;

EID: 71949092011     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.10.010     Document Type: Article
Times cited : (66)

References (41)
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    • note
    • 9O: C, 63.51; H, 5.01; N, 20.20. Found: C, 63.42; H, 5.13; N, 20.03.
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    • The compounds were dissolved in DMSO at 5 mg/ml. For the assays, fresh dilutions of all compounds in screening medium were prepared and 50 μl of highest starting concentration (500 ng/ml) was dispensed in duplicate wells in row B of 96-well tissue culture plate. The highest concentration for chloroquine was 25 ng/ml. Subsequently twofold serial dilutions were prepared up to row H (seven concentrations). Finally 50 μl of 2.5% parasitized cell suspension containing 0.5% parasitaemia was added to each well except four wells in row A which received non-infected cell suspension. These wells containing non-infected erythrocytes in the absence of drugs served as negative controls, while parasitized erythrocytes in the presence of CQ served as positive control. After 72 h of incubation, 100 μl of lysis buffer [20 mM tris (pH 7.5), 5 mM EDTA, 0.008% (wt/vol) saponin, and 0.08% (vol/vol) Triton X-100] containing 1× concentration of SYBER Green I (Invitrogen) was added to each cell
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    • 50) was determined using non-linear regression analysis dose-response curves and represented the concentration of compound required to kill 50% of the fibroblast cells.
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    • 6 parasitized RBC on day 0 and treatment was administered to a group of five mice from day 0 to 3, once daily. The aqueous suspensions of compounds were prepared with a few drops of Tween 80. The efficacy of test compounds was evaluated at 100 mg/kg/day and required daily dose was administered in 0.1 ml volume via oral route. Parasitaemia levels were recorded from thin blood smears between days 4 and 6. The mean value determined for a group of five mice was used to calculate the percent suppression of parasitaemia with respect to the untreated control group. Mice treated with CQ served as reference controls.
    • 6 parasitized RBC on day 0 and treatment was administered to a group of five mice from day 0 to 3, once daily. The aqueous suspensions of compounds were prepared with a few drops of Tween 80. The efficacy of test compounds was evaluated at 100 mg/kg/day and required daily dose was administered in 0.1 ml volume via oral route. Parasitaemia levels were recorded from thin blood smears between days 4 and 6. The mean value determined for a group of five mice was used to calculate the percent suppression of parasitaemia with respect to the untreated control group. Mice treated with CQ served as reference controls. Puri S.K., and Singh N. Expl. Parasitol. 94 (2000) 8
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* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.