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Antimalarial Activity (antimalarial + activity)
Kinds of Antimalarial Activity Selected AbstractsSynthesis and Antimalarial Activities of Some Furoxan Sulfones and Related Furazans.CHEMINFORM, Issue 18 2006Ubaldina Galli Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF. [source] Synthesis of Ring-Substituted 4-Aminoquinolines and Evaluation of Their Antimalarial Activities.CHEMINFORM, Issue 25 2005Peter B. Madrid Abstract For Abstract see ChemInform Abstract in Full Text. [source] Artemisinin Derivatives with Antimalarial Activity against Plasmodium falciparum Designed with the Aid of Quantum Chemical and Partial Least Squares MethodsMOLECULAR INFORMATICS, Issue 8 2003Abstract Artemisinin derivatives with antimalarial activity against Plasmodium falciparum resistant to mefloquine are designed with the aid of Quantum Chemical and Partial Least Squares Methods. The PLS model with three principal components explaining 89.55% of total variance, Q2=0.83 and R2=0.92 was obtained for 14/5 molecules in the training/external validation set. The most important descriptors for the design of the model were one level above the lowest unoccupied molecular orbital energy (LUMO+1), atomic charges in atoms C9 and C11 (Q9) and (Q11) respectively, the maximum number of hydrogen atoms that might make contact with heme (NH) and RDF030,m (a radial distribution function centered at 3.0,Å interatomic distance and weighted by atomic masses). From a set of ten proposed artemisinin derivatives, a new compound (26), was predicted with antimalarial activity higher than the compounds reported in literature. Molecular graphics and modeling supported the PLS results and revealed heme-ligand and protein-ligand stereoelectronic relationships as important for antimalarial activity. The most active 26 and 29 in the prediction set possess substituents at C9 able to extend to hemoglobin exterior, what determines the high activity of these compounds. [source] ChemInform Abstract: Synthesis and Antimalarial Activity of New Analogues of Amodiaquine.CHEMINFORM, Issue 28 2008Sandrine Delarue-Cochin Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Non-Thiol Farnesyltransferase Inhibitors: N-(4-Aminoacylamino-3-benzoylphenyl)-3- [5-(4-nitrophenyl)-2-furyl]acrylic Acid Amides and Their Antimalarial Activity.CHEMINFORM, Issue 22 2005Katja Kettler Abstract For Abstract see ChemInform Abstract in Full Text. [source] Antimalarial Activity of Phenazines from Lapachol, ,-Lapachone and Its Derivatives Against Plasmodium falciparum in vitro and Plasmodium berghei in vivo.CHEMINFORM, Issue 26 2004Valter F. de Andrade-Neto Abstract For Abstract see ChemInform Abstract in Full Text. [source] Design, Synthesis and Antimalarial Activity of Novel, Quinoline-Based, Zinc Metallo-Aminopeptidase Inhibitors.CHEMINFORM, Issue 50 2003Marian Flipo Abstract For Abstract see ChemInform Abstract in Full Text. [source] ChemInform Abstract: Diaryl Ester Prodrugs of FR900098 with Improved in vivo Antimalarial Activity.CHEMINFORM, Issue 28 2001Armin Reichenberg Abstract ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a "Full Text" option. The original article is trackable via the "References" option. [source] Study of Antimalarial Activity of Chemical Constituents from Diospyros quaesitaCHEMISTRY & BIODIVERSITY, Issue 11 2008Cui-Ying Ma Abstract Bioassay-directed fractionation led to the isolation of seven compounds from a sample of the dried leaves, twigs, and branches of Diospyros quaesitaThw. (Ebenaceae). One of the isolates, betulinic acid 3-caffeate (1), showed in vitro antimalarial activity against Plasmodium falciparum clones D6 (chloroquine-sensitive) and W2 (chloroquine-resistant) with IC50 values of 1.40 and 0.98,,M, respectively. Evaluation of compound 1 in the human oral epidermoid (KB) cancer cell line revealed cytotoxicity at ED50 of 4.0,,M. In an attempt to reduce the cytotoxicity of 1, the acetylated derivative 1a and betulinic acid (1b) were prepared. Of the seven isolates, diospyrosin (2) was determined to be a new neolignan. In addition to 1, other known compounds isolated in this study were pinoresinol, lariciresinol, N -benzoyl- L -phenylalaninol, scopoletin, and poriferast-5-en-3,,7, -diol. The structure of 2 was elucidated based on spectroscopic data analysis including 1D- and 2D-NMR, and HR-ESI-MS. [source] Docking Studies of Structurally Diverse Antimalarial Drugs Targeting PfATP6: No Correlation between in,silico Binding Affinity and in,vitro Antimalarial Activity.CHEMMEDCHEM, Issue 9 2009Fatima Bousejra-El Garah Abstract PfATP6, a calcium-dependent ATPase of Plasmodium falciparum, is considered the putative target of the antimalarial drug artemisinin and its derivatives. Herein, the 3D structure of PfATP6 was modeled on the basis of the crystal structure of SERCA,1a, the mammalian homologue. Model validation was achieved using protein structure checking tools. AutoDock4 was used to predict the binding affinities of artemisinin (and analogues) and various other antimalarial agents for PfATP6, for which in,vitro activity is also reported. No correlation was found between the affinity of the compounds for PfATP6 predicted by AutoDock4 and their antimalarial activity. [source] A Combinatorial Approach to 2,4,6-Trisubstituted Triazines with Potent Antimalarial Activity: Combining Conventional Synthesis and Microwave-AssistanceCHEMMEDCHEM, Issue 6 2008Sergio Melato Dr. Managing malaria. Malaria is responsible for two million deaths per year particularly in developing countries, therefore there is great need for the development of cost effective treatment. The synthesis of a library of trisubstituted triazines with potent antimalarial in,vitro activity is reported. Among them, five products may be developed as potential leads in the search for new drugs against plasmodial chloroquine-resistant strains. [source] Synthesis and in vitro Antimalarial Activity of Several Simple Analogues of Peroxyplakoric AcidCHINESE JOURNAL OF CHEMISTRY, Issue 11 2005He-Hua Liu Abstract Several simple analogues of peroxyplakoric acid were synthesized by using Kobayashi's method to construct the key 1,2-dioxane core and tested in vitro for antimalarial activity. The scope and limitation of the method was also briefly examined. [source] Synthesis of new arylaminoquinoxalines and their antimalarial activity in miceJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 10 2001J. B. Rangisetty 2-Arylaminoquinoxalines were prepared by the condensation of 2-chloroquinoxaline with the appropriate Mannich bases in the presence of HCl. To synthesize the Mannich bases, 4-acetamidophenol was reacted with formaldehyde and dialkylamine to yield 3-[(dialkylamino) methyl]-4-hydroxyacetanilide, followed by hydrolysis. Antimalarial activities of the new arylaminoquinoxalines were evaluated against the rodent malaria parasite Plasmodium yoelii at a dose of 75 mg kg,1. Three compounds synthesized (2-[3-[(diethylamino) methyl]-4-hydroxy-anilino]-quinoxaline dihydrochloride (2b), 2-[3-[(pyrrolidinyl) methyl]-4-hydroxyanilino]-quinoxaline dihydrochloride (2f), and 2-[3-[(piperidinyl) methyl]-4-hydroxyanilino]-quinoxaline dihydrochloride (2g)) showed moderate antimalarial activity. [source] Antimalarial activities of gedunin and 7-methoxygedunin and synergistic activity with dillapiolANNALS OF APPLIED BIOLOGY, Issue 2 2003S OMAR Summary Gedunin from Cedrela odorata (Meliaceae), a potent in vitro antimalarial agent, was investigated for its in vivo efficacy in CD-1 mice infected with Plasmodium berghei. When orally administered at 50 mg kg-1 day-1 for 4 days, gedunin was able to suppress the parasitaemia level by 44%. However, no clear dose-response effects were observed in the 0,100 mg kg-1 day-1 dose range. Preliminary pharmacokinetics in Sprague-Dawley rats showed poor absorption. However, a binary treatment of 50 mg kg-1 day-1 gedunin with 25 mg kg-1 day-1 dillapiol, a cytochrome P450 inhibitor, increased parasitaemia clearance in mice to 75%. A clear dose-response was observed in the 0,50 mg kg-1 day-1 gedunin dose range when administration was combined with 25 mg kg-1 day-1 dillapiol. In addition, 7-methoxygedunin, a semi-synthetic derivative which is more stable to degradation than gedunin, suppressed the level in mice by 67% at 50 mg kg-1 day-1. When administered at this dose in combination with 25 mg kg-1 day-1 dillapiol, clearance increased to 80%. These results demonstrate the potentialefficacy of antimalarial drugs and phytomedicines based on gedunin and the value of the combination therapy. [source] Synthesis and Biological Evaluation of Novel 4-Substituted 1-{[4-(10,15,20-Triphenylporphyrin-5-yl)phenyl]methylidene}thiosemicarbazides as New Class of Potential Antiprotozoal AgentsCHEMISTRY & BIODIVERSITY, Issue 5 2008Abdul Abstract A novel series of 4-substituted 1-{[4-(10,15,20-triphenylporphyrin-5-yl)phenyl]methylidene}thiosemicarbazide, 4a,4n, was synthesized in 9,21% yield by the condensation of 4-(10,15,20-triphenylporphyrin-5-yl)benzaldehyde (3) with various substituted thiosemicarbazides in presence of catalytic amount of AcOH. These compounds were assayed for in vitro antiamoebic activity, and the results showed that out of 14 compounds 9 were found with IC50 values lower than metronidazole corresponding to 1.05- to 4.7-fold increase in activity. MTT Assay showed that all the compounds are nontoxic to human kidney epithelial cell line. 4-(m -Toluidinyl)-1-{[4-(10,15,20-triphenylporphyrin-5-yl)phenyl]methylidene}thiosemicarbazide (4h) showed the highest antiamoebic activity with least cytotoxicity. Some of the compounds were screened for their antimalarial activities and ability to inhibit , -haematin formation, but none of them showed an activity better than chloroquine and quinine. Only one compound out of six showed an activity comparable to standard drug. [source] Quinolone analogues 10: Synthesis of antimalarial quinolones having pyridyl moiety in N1-side chainJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 3 2010Yoshihisa Kurasawa Novel 4-quinolone-3-carboxylates 6,7 and 4-quinolone-3-carboxylic acids 8,11 were synthesized from 4-hydroxyquinoline-3-carboxylates. Ethyl 1-[1-ethoxycarbonyl-2-(4-pyridyl)vinyl]-6-fluoro-4-oxoquinoline-3-carboxylate 7a was found to show antimalarial activity from the screening data. J. Heterocyclic Chem., (2010). [source] Cyclopeptides of Linum usitatissimumJOURNAL OF PEPTIDE SCIENCE, Issue 9 2006Boles, aw Picur Abstract Cyclolinopeptide A (CLA), a cyclic nonapeptide from linseed, possesses strong immunosuppressive and antimalarial activity along with the ability to inhibit cholate uptake into hepatocytes. The structure of the peptide was studied extensively in solution as well as in the solid state. It is postulated that both the Pro,Pro cis -amide bond and an ,edge-to-face' interaction between the aromatic rings of two adjacent Phe residues are important for biological activity. Structure,activity relationship studies of many linear and cyclic analogues of CLA suggest that the Pro-Xxx-Phe sequence and the flexibility of the peptide are important for the immunosuppressive activity. Copyright © 2006 European Peptide Society and John Wiley & Sons, Ltd. [source] Synthesis of new arylaminoquinoxalines and their antimalarial activity in miceJOURNAL OF PHARMACY AND PHARMACOLOGY: AN INTERNATI ONAL JOURNAL OF PHARMACEUTICAL SCIENCE, Issue 10 2001J. B. Rangisetty 2-Arylaminoquinoxalines were prepared by the condensation of 2-chloroquinoxaline with the appropriate Mannich bases in the presence of HCl. To synthesize the Mannich bases, 4-acetamidophenol was reacted with formaldehyde and dialkylamine to yield 3-[(dialkylamino) methyl]-4-hydroxyacetanilide, followed by hydrolysis. Antimalarial activities of the new arylaminoquinoxalines were evaluated against the rodent malaria parasite Plasmodium yoelii at a dose of 75 mg kg,1. Three compounds synthesized (2-[3-[(diethylamino) methyl]-4-hydroxy-anilino]-quinoxaline dihydrochloride (2b), 2-[3-[(pyrrolidinyl) methyl]-4-hydroxyanilino]-quinoxaline dihydrochloride (2f), and 2-[3-[(piperidinyl) methyl]-4-hydroxyanilino]-quinoxaline dihydrochloride (2g)) showed moderate antimalarial activity. [source] Artemisinin Derivatives with Antimalarial Activity against Plasmodium falciparum Designed with the Aid of Quantum Chemical and Partial Least Squares MethodsMOLECULAR INFORMATICS, Issue 8 2003Abstract Artemisinin derivatives with antimalarial activity against Plasmodium falciparum resistant to mefloquine are designed with the aid of Quantum Chemical and Partial Least Squares Methods. The PLS model with three principal components explaining 89.55% of total variance, Q2=0.83 and R2=0.92 was obtained for 14/5 molecules in the training/external validation set. The most important descriptors for the design of the model were one level above the lowest unoccupied molecular orbital energy (LUMO+1), atomic charges in atoms C9 and C11 (Q9) and (Q11) respectively, the maximum number of hydrogen atoms that might make contact with heme (NH) and RDF030,m (a radial distribution function centered at 3.0,Å interatomic distance and weighted by atomic masses). From a set of ten proposed artemisinin derivatives, a new compound (26), was predicted with antimalarial activity higher than the compounds reported in literature. Molecular graphics and modeling supported the PLS results and revealed heme-ligand and protein-ligand stereoelectronic relationships as important for antimalarial activity. The most active 26 and 29 in the prediction set possess substituents at C9 able to extend to hemoglobin exterior, what determines the high activity of these compounds. [source] Antiparasitic, nematicidal and antifouling constituents from Juniperus berriesPHYTOTHERAPY RESEARCH, Issue 12 2008Volodymyr Samoylenko Abstract A bioassay-guided fractionation of Juniperus procera berries yielded antiparasitic, nematicidal and antifouling constituents, including a wide range of known abietane, pimarane and labdane diterpenes. Among these, abieta-7,13-diene (1) demonstrated in vitro antimalarial activity against Plasmodium falciparum D6 and W2 strains (IC50 = 1.9 and 2.0 µg/mL, respectively), while totarol (6), ferruginol (7) and 7, -hydroxyabieta-8,13-diene-11,12-dione (8) inhibited Leishmania donovani promastigotes with IC50 values of 3.5,4.6 µg/mL. In addition, totarol demonstrated nematicidal and antifouling activities against Caenorhabditis elegans and Artemia salina at a concentration of 80 µg/mL and 1 µg/mL, respectively. The resinous exudate of J. virginiana afforded known antibacterial E -communic acid (4) and 4- epi -abietic acid (5), while the volatile oil from its trunk wood revealed large quantities of cedrol (9). Using GC/MS, the two known abietanes totarol (6) and ferruginol (7) were identified from the berries of J. procera, J. excelsa and J. phoenicea. Copyright © 2008 John Wiley & Sons, Ltd. [source] Antimalarial compounds from Kniphofia foliosa rootsPHYTOTHERAPY RESEARCH, Issue 6 2005Abraham Abebe Wube Abstract During the course of screening Ethiopian medicinal plants for their antimalarial properties, it was found that the dichloromethane extract of the roots of Kniphofia foliosa Hochst. (Asphodelaceae), which have long been used in the traditional medicine of Ethiopia for the treatment of abdominal cramps and wound healing, displayed strong in vitro antiplasmodial activity against the chloroquine-sensitive 3D7 strain of Plasmodium falciparum with an ED50 value of 3.8 µg/mL and weak cytotoxic activity against KB cells with an ED50 value of 35.2 µg/mL. Five compounds were isolated from the roots and evaluated for their invitro antimalarial activity. Among the compounds tested, 10-(chrysophanol-7,-yl)-10-(,)-hydroxychrysopanol-9-anthrone and chryslandicin, showed a high inhibition of the growth of the malaria parasite, P. falciparum with ED50 values of 0.260 and 0.537 µg/mL, respectively, while the naphthalene derivative, 2-acetyl-1-hydroxy-8-methoxy-3-methylnaphthalene, exhibited a less significant antimalarial activity with an ED50 value of 15.4 µg/mL. To compare the effect on the parasite with toxicity to mammalian cells, the cytotoxic activities of the isolated compounds against the KB cell line were evaluated and 10-(chrysophanol-7,-yl)-10-(,)-hydroxychrysopanol-9-anthrone and chryslandicin displayed very low toxicity with ED50 values of 104 and 90 µg/mL, respectively. This is the first report of the inhibition of the growth of P. falciparum by anthraquinone-anthrone dimers and establishes them as a new class of potential antimalarial compounds with very little host cell toxicity. Copyright © 2005 John Wiley & Sons, Ltd. [source] Evaluation of antiprotozoal and plasmodial enoyl-ACP reductase inhibition potential of turkish medicinal plantsPHYTOTHERAPY RESEARCH, Issue 2 2005D. Tasdemir Abstract A total of 58 extracts of different polarity were prepared from various organs of 16 species of Turkish plants and screened for their antitrypanosomal, antileishmanial and antiplasmodial activities. No significant activity was observed against Trypanosoma cruzi, whereas many extracts showed appreciable trypanocidal potential against T. brucei rhodesiense, with the CHCl3 -soluble portion of Phlomis kurdica being the most active (IC50 2.7 µg[sol ]mL). Almost all extracts, particularly the CHCl3 phases, exhibited growth inhibition activity against Leishmania donovani amastigotes. The CHCl3 -solubles of Putoria calabrica roots (IC50 1.9 µg[sol ]mL), Wendlandia ligustroides leaves (IC50 2.1 µg[sol ]mL) and Rhododendronluteum leaves (IC50 2.3 µg[sol ]mL) displayed the highest leishmanicidal potential. The majority of the extracts also possessed antiplasmodial activity against the multi-drug resistant K1 Plasmodium falciparum strain. The most potent antiplasmodial activity was observed with the CHCl3 extracts of Phlomis kurdica (IC50 1.5 µg[sol ]mL), P. leucophracta (IC50 1.6 µg[sol ]mL), Scrophularia cryptophila (IC50 1.8 µg[sol ]mL), Morina persica (IC50 1.9 µg[sol ]mL) and the aqueous root extract of Asperula nitida subsp. subcapitellata (IC50 1.6 µg[sol ]mL). Twenty-one extracts with significant antimalarial activity (IC50 < 5 µg[sol ]mL) were also tested for their ability to inhibit the purified enoyl-ACP reductase (FabI), a crucial enzyme in the fatty acid biosynthesis of P. falciparum. The CHCl3 extract of Rhododendronungernii leaves (IC50 10 µg[sol ]mL) and the H2O-soluble portion of Rhododendronsmirnovii leaves (IC50 0.4 µg[sol ]mL) strongly inhibited the FabI enzyme. The preliminary data indicate that some (poly)phenolic compounds are responsible for the FabI inhibition potential of these extracts. The presented work reports for the first time the antiprotozoal activity of nine different genera as well as a target specific antimalarial screening for the identification of P. falciparum FabI inhibitors from medicinal plant extracts. Copyright © 2005 John Wiley & Sons, Ltd. [source] Study of Antimalarial Activity of Chemical Constituents from Diospyros quaesitaCHEMISTRY & BIODIVERSITY, Issue 11 2008Cui-Ying Ma Abstract Bioassay-directed fractionation led to the isolation of seven compounds from a sample of the dried leaves, twigs, and branches of Diospyros quaesitaThw. (Ebenaceae). One of the isolates, betulinic acid 3-caffeate (1), showed in vitro antimalarial activity against Plasmodium falciparum clones D6 (chloroquine-sensitive) and W2 (chloroquine-resistant) with IC50 values of 1.40 and 0.98,,M, respectively. Evaluation of compound 1 in the human oral epidermoid (KB) cancer cell line revealed cytotoxicity at ED50 of 4.0,,M. In an attempt to reduce the cytotoxicity of 1, the acetylated derivative 1a and betulinic acid (1b) were prepared. Of the seven isolates, diospyrosin (2) was determined to be a new neolignan. In addition to 1, other known compounds isolated in this study were pinoresinol, lariciresinol, N -benzoyl- L -phenylalaninol, scopoletin, and poriferast-5-en-3,,7, -diol. The structure of 2 was elucidated based on spectroscopic data analysis including 1D- and 2D-NMR, and HR-ESI-MS. [source] Docking Studies of Structurally Diverse Antimalarial Drugs Targeting PfATP6: No Correlation between in,silico Binding Affinity and in,vitro Antimalarial Activity.CHEMMEDCHEM, Issue 9 2009Fatima Bousejra-El Garah Abstract PfATP6, a calcium-dependent ATPase of Plasmodium falciparum, is considered the putative target of the antimalarial drug artemisinin and its derivatives. Herein, the 3D structure of PfATP6 was modeled on the basis of the crystal structure of SERCA,1a, the mammalian homologue. Model validation was achieved using protein structure checking tools. AutoDock4 was used to predict the binding affinities of artemisinin (and analogues) and various other antimalarial agents for PfATP6, for which in,vitro activity is also reported. No correlation was found between the affinity of the compounds for PfATP6 predicted by AutoDock4 and their antimalarial activity. [source] Synthesis and in vitro Antimalarial Activity of Several Simple Analogues of Peroxyplakoric AcidCHINESE JOURNAL OF CHEMISTRY, Issue 11 2005He-Hua Liu Abstract Several simple analogues of peroxyplakoric acid were synthesized by using Kobayashi's method to construct the key 1,2-dioxane core and tested in vitro for antimalarial activity. The scope and limitation of the method was also briefly examined. [source] | |||||||||||||||||||||||||