Antimalarial activity of new acridinone derivatives
Malaria is one of the major threats concerning world public health. Resistance to the current antimalarial drugs has led to searches for new antimalarial compounds. Acridinone derivatives have recently demonstrated to be active against malaria parasite. We focused our attention on synthesized new ac...
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2011
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| LEADER | 11635caa a22012857a 4500 | ||
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| 001 | PAPER-10591 | ||
| 003 | AR-BaUEN | ||
| 005 | 20230518204039.0 | ||
| 008 | 190411s2011 xx ||||fo|||| 00| 0 eng|d | ||
| 024 | 7 | |2 scopus |a 2-s2.0-79959676872 | |
| 024 | 7 | |2 cas |a atovaquone, 94015-53-9, 95233-18-4; chloroquine, 132-73-0, 3545-67-3, 50-63-5, 54-05-7; stigmatellin, 91682-96-1; Acridines; Antimalarials; Hemeproteins; hemozoin, 39404-00-7 | |
| 040 | |a Scopus |b spa |c AR-BaUEN |d AR-BaUEN | ||
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| 100 | 1 | |a Fernández-Calienes, A. | |
| 245 | 1 | 0 | |a Antimalarial activity of new acridinone derivatives |
| 260 | |c 2011 | ||
| 270 | 1 | 0 | |m Fernández-Calienes, A.; Departamento de Parasitología, Instituto de Medicina Tropical Pedro Kourí, Autopista Novia del Mediodía Km 6, Ciudad de La Habana, Marianao 13, Cuba; email: ayme@ipk.sld.cu |
| 506 | |2 openaire |e Política editorial | ||
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| 520 | 3 | |a Malaria is one of the major threats concerning world public health. Resistance to the current antimalarial drugs has led to searches for new antimalarial compounds. Acridinone derivatives have recently demonstrated to be active against malaria parasite. We focused our attention on synthesized new acridinone derivatives, some of them resulting with high antiviral and trypanocidal activity. In this study new derivatives of 10-alyl-, 10-(3-methyl-2-butenyl)- and 10-(1,2-propadienyl)-9(10H)-acridinone were evaluated for their antimalarial activity against Plasmodium falciparum. To assess the selectivity, cytotoxicity was assessed in parallel against human MRC-5 cells. Inhibition of β-hematin formation was determined using a spectrophotometric assay. Mitochondrial bc 1 complexes were isolated from yeast and bovine heart cells to test acridinone inhibitory activity. This study resulted in the identification of three compounds with submicromolar efficacy against P. falciparum and without cytotoxic effects on human cellular line. One compound, IIa (1-fluoro-10-(3-methyl-2-butenyl)-9(10H)-acridinone), can be classified as hit for antimalarial drug development exhibiting IC 50 less than 0.2μg/mL with SI greater than 100. In molecular tests, no relevant inhibitory activity was obtained for our compounds. The mechanism of acridinones antimalarial action remains unclear. © 2011 Elsevier Masson SAS. |l eng | |
| 593 | |a Departamento de Parasitología, Instituto de Medicina Tropical Pedro Kourí, Autopista Novia del Mediodía Km 6, Ciudad de La Habana, Marianao 13, Cuba | ||
| 593 | |a Laboratorio de Síntesis Orgánica, Facultad de Química, Ciudad de La Habana, Universidad de La Habana, Calle Zapata s/n entre G y Carlitos Aguirre. Plaza, CP 10 400, Cuba | ||
| 593 | |a CIHIDECAR (CONICET), Departamento de Química Orgánica, Facultad de Ciencias Exactas y Naturales, Universidad de Buenos Aires, Ciudad Universitaria, Pabellón 2, Piso 3, 1428 Buenos Aires, Argentina | ||
| 593 | |a Laboratory for microbiology, Parasitology and hygiene (LMPH), University of Antwerp, Groenenborgerlaan 171, 2020 Antwerp, Belgium | ||
| 593 | |a Molecular pharmacology and toxicology unit, Department of biomedical sciences, University of Veterinary Medicine, Veterinärpl. 1, 1210 Vienna, Austria | ||
| 690 | 1 | 0 | |a ACRIDINONE |
| 690 | 1 | 0 | |a ANTIMALARIAL ACTIVITY |
| 690 | 1 | 0 | |a PLASMODIUM FALCIPARUM |
| 690 | 1 | 0 | |a 10 (1,2 PROPADIENYL) 9 (10H) ACRIDINONE |
| 690 | 1 | 0 | |a 10 (3 METHYL 2 BUTENYL) 9 (10H) ACRIDINONE |
| 690 | 1 | 0 | |a 10 ALLYL 9 (10H) ACRIDINONE |
| 690 | 1 | 0 | |a ANTIMALARIAL AGENT |
| 690 | 1 | 0 | |a ATOVAQUONE |
| 690 | 1 | 0 | |a BETA HEMATIN |
| 690 | 1 | 0 | |a CHLOROQUINE |
| 690 | 1 | 0 | |a HEME DERIVATIVE |
| 690 | 1 | 0 | |a STIGMATELLIN |
| 690 | 1 | 0 | |a UNCLASSIFIED DRUG |
| 690 | 1 | 0 | |a ANIMAL CELL |
| 690 | 1 | 0 | |a ANTIMALARIAL ACTIVITY |
| 690 | 1 | 0 | |a ARTICLE |
| 690 | 1 | 0 | |a CONTROLLED STUDY |
| 690 | 1 | 0 | |a COW |
| 690 | 1 | 0 | |a CYTOTOXICITY |
| 690 | 1 | 0 | |a DRUG SELECTIVITY |
| 690 | 1 | 0 | |a HEART MUSCLE CELL |
| 690 | 1 | 0 | |a HUMAN |
| 690 | 1 | 0 | |a HUMAN CELL |
| 690 | 1 | 0 | |a IC 50 |
| 690 | 1 | 0 | |a NONHUMAN |
| 690 | 1 | 0 | |a PLASMODIUM FALCIPARUM |
| 690 | 1 | 0 | |a PRIORITY JOURNAL |
| 690 | 1 | 0 | |a SPECTROPHOTOMETRY |
| 690 | 1 | 0 | |a YEAST |
| 690 | 1 | 0 | |a ACRIDINES |
| 690 | 1 | 0 | |a ANIMALS |
| 690 | 1 | 0 | |a ANTIMALARIALS |
| 690 | 1 | 0 | |a CATTLE |
| 690 | 1 | 0 | |a CELL LINE |
| 690 | 1 | 0 | |a DRUG RESISTANCE, MICROBIAL |
| 690 | 1 | 0 | |a HEMEPROTEINS |
| 690 | 1 | 0 | |a HUMANS |
| 690 | 1 | 0 | |a PLASMODIUM FALCIPARUM |
| 690 | 1 | 0 | |a YEASTS |
| 650 | 1 | 7 | |2 spines |a MALARIA |
| 700 | 1 | |a Pellón, R. | |
| 700 | 1 | |a Docampo, M. | |
| 700 | 1 | |a Fascio, M. | |
| 700 | 1 | |a D'Accorso, N. | |
| 700 | 1 | |a Maes, L. | |
| 700 | 1 | |a Mendiola, J. | |
| 700 | 1 | |a Monzote, L. | |
| 700 | 1 | |a Gille, L. | |
| 700 | 1 | |a Rojas, L. | |
| 773 | 0 | |d 2011 |g v. 65 |h pp. 210-214 |k n. 3 |p Biomed. Pharmacother. |x 07533322 |t Biomedicine and Pharmacotherapy | |
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