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Volumn 19, Issue 9, 2009, Pages 2570-2573

Synthesis of novel thiourea, thiazolidinedione and thioparabanic acid derivatives of 4-aminoquinoline as potent antimalarials

Author keywords

4 Aminoquinoline; Antimalarial; Plasmodium falciparum; Thiazolidinedione; Thioparabanic acid; Thiourea

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; 4 AMINOQUINOLINE; ANTIMALARIAL AGENT; CHLOROQUINE; HEMATIN; THIOPARABANIC ACID; THIOUREA DERIVATIVE; UNCLASSIFIED DRUG;

EID: 64349106120     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.03.026     Document Type: Article
Times cited : (93)

References (21)
  • 1
    • 57049140232 scopus 로고    scopus 로고
    • Twentieth Report, World Health Organization
    • WHO Expert Committee on Malaria. Technical Report Series, Geneva
    • WHO Expert Committee on Malaria. Technical Report Series. Twentieth Report, World Health Organization, Geneva 2000.
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  • 17
    • 64349122256 scopus 로고    scopus 로고
    • note
    • 2S: C, 55.31; H, 4.90; N, 14.33. Found: C, 55.35; H, 4.83; N, 14.31.
  • 18
    • 64349107432 scopus 로고    scopus 로고
    • note
    • 50) was determined using non-linear regression analysis dose-response curves.
  • 19
    • 0033007803 scopus 로고    scopus 로고
    • 5 P. yoelii infected RBCs. Blood of infected animal at ∼50% parasitemia was collected by cardiac puncture in 2.0% citrate buffer and centrifuged at 5000 rpm for 10 min at 4 °C. The plasma was used in assay of β-hematin formation. The assay mixture contained 100 mM sodium acetate buffer pH (5.1), 50 μL plasma, 100 μM hemin as the substrate and 1-20 μg compound/drug in a total volume of 1.0 mL. The control tube contained all reagents except compound. The reaction mixture in triplicate was incubated at 37 °C for 16 h in a rotary shaker. The reaction was stopped by centrifugation at 10,000 rpm for 10 min at 30 °C. The pellet was suspended in 100 mM Tris-HCl buffer pH (7.4) containing 2.5% SDS. The pellet obtained after centrifugation was washed thrice with distilled water (TDW) to remove free hemin attached to β-hematin.
    • 5 P. yoelii infected RBCs. Blood of infected animal at ∼50% parasitemia was collected by cardiac puncture in 2.0% citrate buffer and centrifuged at 5000 rpm for 10 min at 4 °C. The plasma was used in assay of β-hematin formation. The assay mixture contained 100 mM sodium acetate buffer pH (5.1), 50 μL plasma, 100 μM hemin as the substrate and 1-20 μg compound/drug in a total volume of 1.0 mL. The control tube contained all reagents except compound. The reaction mixture in triplicate was incubated at 37 °C for 16 h in a rotary shaker. The reaction was stopped by centrifugation at 10,000 rpm for 10 min at 30 °C. The pellet was suspended in 100 mM Tris-HCl buffer pH (7.4) containing 2.5% SDS. The pellet obtained after centrifugation was washed thrice with distilled water (TDW) to remove free hemin attached to β-hematin. The pellet was solubilized in 50 μL of 2 N NaOH and volume was made up to 1.0 mL with TDW. Absorbance was measured at 400 nm. Pandey A.V., Singh N., Tekwani B.L., Puri S.K., and Chauhan V.S. J.Pharm. Biomed. Anal. 20 (1999) 203
    • (1999) J.Pharm. Biomed. Anal. , vol.20 , pp. 203
    • Pandey, A.V.1    Singh, N.2    Tekwani, B.L.3    Puri, S.K.4    Chauhan, V.S.5
  • 20
    • 0021061819 scopus 로고
    • 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.
    • 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. Mosmann T. J. Immunol. Methods 65 (1983) 55
    • (1983) J. Immunol. Methods , vol.65 , pp. 55
    • Mosmann, T.1
  • 21
    • 0033973112 scopus 로고    scopus 로고
    • 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 50 mg/kg/day and required daily dose was administered in 0.2 mL volume via intraperitoneal route. Parasitaemia levels were recorded from thin blood smears on days 4. 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 50 mg/kg/day and required daily dose was administered in 0.2 mL volume via intraperitoneal route. Parasitaemia levels were recorded from thin blood smears on days 4. 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. Parasit. 94 (2000) 8
    • (2000) Expl. Parasit. , vol.94 , pp. 8
    • Puri, S.K.1    Singh, N.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.