Academic literature on the topic 'Antitrypanosomal'

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Journal articles on the topic "Antitrypanosomal"

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Dofuor, Aboagye Kwarteng, Temitayo Samson Ademolue, Cynthia Mmalebna Amisigo, Kwaku Kyeremeh, and Theresa Manful Gwira. "Chemical Derivatization and Characterization of Novel Antitrypanosomals for African Trypanosomiasis." Molecules 26, no. 15 (July 25, 2021): 4488. http://dx.doi.org/10.3390/molecules26154488.

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The search for novel antitrypanosomals and the investigation into their mode of action remain crucial due to the toxicity and resistance of commercially available antitrypanosomal drugs. In this study, two novel antitrypanosomals, tortodofuordioxamide (compound 2) and tortodofuorpyramide (compound 3), were chemically derived from the natural N-alkylamide tortozanthoxylamide (compound 1) through structural modification. The chemical structures of these compounds were confirmed through spectrometric and spectroscopic analysis, and their in vitro efficacy and possible mechanisms of action were, subsequently, investigated in Trypanosoma brucei (T. brucei), one of the causative species of African trypanosomiasis (AT). The novel compounds 2 and 3 displayed significant antitrypanosomal potencies in terms of half-maximal effective concentrations (EC50) and selectivity indices (SI) (compound 1, EC50 = 7.3 μM, SI = 29.5; compound 2, EC50 = 3.2 μM, SI = 91.3; compound 3, EC50 = 4.5 μM, SI = 69.9). Microscopic analysis indicated that at the EC50 values, the compounds resulted in the coiling and clumping of parasite subpopulations without significantly affecting the normal ratio of nuclei to kinetoplasts. In contrast to the animal antitrypanosomal drug diminazene, compounds 1, 2 and 3 exhibited antioxidant absorbance properties comparable to the standard antioxidant Trolox (Trolox, 0.11 A; diminazene, 0.50 A; compound 1, 0.10 A; compound 2, 0.09 A; compound 3, 0.11 A). The analysis of growth kinetics suggested that the compounds exhibited a relatively gradual but consistent growth inhibition of T. brucei at different concentrations. The results suggest that further pharmacological optimization of compounds 2 and 3 may facilitate their development into novel AT chemotherapy.
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Steverding, Dietmar, and Kevin M. Tyler. "Novel antitrypanosomal agents." Expert Opinion on Investigational Drugs 14, no. 8 (July 29, 2005): 939–55. http://dx.doi.org/10.1517/13543784.14.8.939.

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Sealey-Cardona, Marco, Simon Cammerer, Simon Jones, Luis M. Ruiz-Pérez, Reto Brun, Ian H. Gilbert, Julio A. Urbina, and Dolores González-Pacanowska. "Kinetic Characterization of Squalene Synthase from Trypanosoma cruzi: Selective Inhibition by Quinuclidine Derivatives." Antimicrobial Agents and Chemotherapy 51, no. 6 (March 19, 2007): 2123–29. http://dx.doi.org/10.1128/aac.01454-06.

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ABSTRACT The biosynthesis of sterols is a major route for the development of antitrypanosomals. Squalene synthase (SQS) catalyzes the first step committed to the biosynthesis of sterols within the isoprenoid pathway, and several inhibitors of the enzyme have selective antitrypanosomal activity both in vivo and in vitro. The enzyme from Trypanosoma cruzi is a 404-amino-acid protein with a clearly identifiable membrane-spanning region. In an effort to generate soluble recombinant enzyme, we have expressed in Escherichia coli several truncated versions of T. cruzi SQS with a His tag attached to the amino terminus. Deletions of both the amino- and carboxyl-terminal regions generated active and soluble forms of the enzyme. The highest levels of soluble protein were achieved when 24 and 36 amino acids were eliminated from the amino and carboxyl regions, respectively, yielding a protein of 41.67 kDa. The Michaelis-Menten constants of the purified enzyme for farnesyl diphosphate and NAD (NADPH) were 5.25 and 23.34 μM, respectively, whereas the V max was 1,428.56 nmol min−1mg−1. Several quinuclidine derivatives with antiprotozoal activity in vitro were found to be selective inhibitors of recombinant T. cruzi SQS in comparative assays with the human enzyme, with 50% inhibitory concentration values in the nanomolar range. These data suggest that selective inhibition of T. cruzi SQS may be an efficient strategy for the development of new antitrypanosomal agents.
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Kaminsky, R., E. Zweygarth, and E. De Clercq. "Antitrypanosomal Activity of Phosphonylmethoxyalkylpurines." Journal of Parasitology 80, no. 6 (December 1994): 1026. http://dx.doi.org/10.2307/3283453.

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Nenortas, Elizabeth, Christian Burri, and Theresa A. Shapiro. "Antitrypanosomal Activity of Fluoroquinolones." Antimicrobial Agents and Chemotherapy 43, no. 8 (August 1, 1999): 2066–68. http://dx.doi.org/10.1128/aac.43.8.2066.

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ABSTRACT Six fluoroquinolones presently in clinical use and four investigational tetracyclic fluoroquinolones were tested for in vitro activity against bloodstream-form Trypanosoma brucei brucei. All compounds had measurable activity, but the tetracyclic analogs were most potent, with 50% effective concentrations in the low micromolar range. In general, trypanosomes were more susceptible than L1210 leukemia cells. Consistent with the notion that they target type II topoisomerase in trypanosomes, the fluoroquinolones promote the formation of protein-DNA covalent complexes.
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Scovill, John, Elizabeth Blank, Michael Konnick, Elizabeth Nenortas, and Theresa Shapiro. "Antitrypanosomal Activities of Tryptanthrins." Antimicrobial Agents and Chemotherapy 46, no. 3 (March 2002): 882–83. http://dx.doi.org/10.1128/aac.46.3.882-883.2002.

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ABSTRACT New drugs and molecular targets are needed against Trypanosoma brucei, the protozoan that causes African sleeping sickness. Tryptanthrin (indolo[2,1-b]quinazoline-6,12-dione), a traditional antifungal agent, and 11 analogs were tested against T. brucei in vitro. The greatest activity was conferred by electron-withdrawing groups in the 8 position of the tryptanthrin ring system; the most potent compound had a 50% effective concentration of 0.40 μM.
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Abdeta, Debela, Nigatu Kebede, Mirutse Giday, Getachew Terefe, and Solomon Mequanente Abay. "In Vitro and In Vivo Antitrypanosomal Activities of Methanol Extract of Echinops kebericho Roots." Evidence-Based Complementary and Alternative Medicine 2020 (September 22, 2020): 1–6. http://dx.doi.org/10.1155/2020/8146756.

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Microbial resistance to the few conventional antitrypanosomal drugs, increasing resistance of vectors to insecticides, lack of effective vaccines, and adverse effects of the existing antitrypanosomal drugs justify the urgent need for effective, tolerable, and affordable drugs. We assessed antitrypanosomal effects of the hydromethanolic extract of Echinops kebericho Mesfin roots against Trypanosoma congolense field isolate using in vitro and in vivo techniques. Parasite load, packed cell volume (PCV), body weight, and rectal temperature in Swiss albino mice were assessed. This finding is part of the outcomes of drug discovery research for neglected tropical diseases. The extract arrested the motility of trypanosomes within 40 min at 4 and 2 mg/mL concentration, whereas in the untreated control, motility continued for more than 160 min. The extract also reduced parasitemia and prevented drop in PCV and body weight significantly (p<0.05), as compared to control. Phytochemical analysis showed the presence of flavonoids, triterpenes, steroids, saponins, glycosides, tannins, and alkaloids. It is observed that this extract has activity against the parasite. Isolation and purification of specific compounds are required to identify hit compounds responsible for the antitrypanosomal activity of the studied medicinal plant.
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Dofuor, Aboagye Kwarteng, Frederick Ayertey, Peter Bolah, Georgina Isabella Djameh, Kwaku Kyeremeh, Mitsuko Ohashi, Laud Kenneth Okine, and Theresa Manful Gwira. "Isolation and Antitrypanosomal Characterization of Furoquinoline and Oxylipin from Zanthoxylum zanthoxyloides." Biomolecules 10, no. 12 (December 13, 2020): 1670. http://dx.doi.org/10.3390/biom10121670.

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In the absence of vaccines, there is a need for alternative sources of effective chemotherapy for African trypanosomiasis (AT). The increasing rate of resistance and toxicity of commercially available antitrypanosomal drugs also necessitates an investigation into the mode of action of new antitrypanosomals for AT. In this study, furoquinoline 4, 7, 8-trimethoxyfuro (2, 3-b) quinoline (compound 1) and oxylipin 9-oxo-10, 12-octadecadienoic acid (compound 2) were isolated from the plant species Zanthoxylum zanthoxyloides (Lam) Zepern and Timler (root), and their in vitro efficacy and mechanisms of action investigated in Trypanosoma brucei (T. brucei), the species responsible for AT. Both compounds resulted in a selectively significant growth inhibition of T. brucei (compound 1, half-maximal effective concentration EC50 = 1.7 μM, selectivity indices SI = 74.9; compound 2, EC50 = 1.2 μM, SI = 107.3). With regards to effect on the cell cycle phases of T. brucei, only compound 1 significantly arrested the second growth-mitotic (G2-M) phase progression even though G2-M and DNA replication (S) phase arrest resulted in the overall reduction of T. brucei cells in G0-G1 for both compounds. Moreover, both compounds resulted in the aggregation and distortion of the elongated slender morphology of T. brucei. Analysis of antioxidant potential revealed that at their minimum and maximum concentrations, the compounds exhibited significant oxidative activities in T. brucei (compound 1, 22.7 μM Trolox equivalent (TE), 221.2 μM TE; compound 2, 15.0 μM TE, 297.7 μM TE). Analysis of growth kinetics also showed that compound 1 exhibited a relatively consistent growth inhibition of T. brucei at different concentrations as compared to compound 2. The results suggest that compounds 1 and 2 are promising antitrypanosomals with the potential for further development into novel AT chemotherapy.
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Croft, Simon L. "Pharmacological Approaches to Antitrypanosomal Chemotherapy." Memórias do Instituto Oswaldo Cruz 94, no. 2 (March 1999): 215–20. http://dx.doi.org/10.1590/s0074-02761999000200017.

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Nkemgu-Njinkeng, Joseph, Vera Rosenkranz, Michael Wink, and Dietmar Steverding. "Antitrypanosomal Activities of Proteasome Inhibitors." Antimicrobial Agents and Chemotherapy 46, no. 6 (June 2002): 2038–40. http://dx.doi.org/10.1128/aac.46.6.2038-2040.2002.

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ABSTRACT Seven peptidyl proteasome inhibitors were tested for in vitro activity against Trypanosoma brucei bloodstream forms. Two compounds showed activity in the low nanomolar range. In general, trypanosomes were more susceptible to the compounds than were human HL-60 cells. The data support the potential of proteasome inhibitors for rational antitrypanosomal drug development.
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Dissertations / Theses on the topic "Antitrypanosomal"

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Clark, Rachel L. "The development of new broad spectrum antitrypanosomal agents." Thesis, University of Strathclyde, 2005. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.415310.

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Golisade, Abolfasl. "Polymerunterstützte Synthese von antitrypanosomal und anti-Malaria-aktiven Adenosinderivaten." [S.l.] : [s.n.], 2001. http://deposit.ddb.de/cgi-bin/dokserv?idn=964083248.

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Mungongo, Singfrid Gasper. "The design, synthesis and biological evaluation of novel antitrypanosomal drugs." Thesis, University of Sunderland, 1994. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.284073.

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Skaf, Joseph [Verfasser], and Ulrike [Gutachter] Holzgrabe. "Antileishmanial and antitrypanosomal compounds from \(Achillea\) \(fragrantissima\) / Joseph Skaf ; Gutachter: Ulrike Holzgrabe." Würzburg : Universität Würzburg, 2018. http://d-nb.info/1166560244/34.

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Zulu, Ayanda Ignatia. "Synthesis and evaluation of arylpyrrole-chalcone hybrids as antiplasmodial and antitrypanosomal agents." Thesis, Rhodes University, 2017. http://hdl.handle.net/10962/65268.

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Rathnam, Rajendra Prasad. "Synthesis and biological evaluation of 1,4-benzodiazepin-2-one analogues with antitrypanosomal activity." Thesis, University of Greenwich, 2010. http://gala.gre.ac.uk/8110/.

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The 1,4-benzodiazepin-2-one motif has been taken as a privileged skeleton for making antitrypanosomal agents. A library of over sixty 1,4-benzodiazepin-2-one derivatives has been synthesised employing novel synthetic routes. These derivatives were characterised spectroscopically, by mass spectrometry, and by combustion analysis. Five derivatives were characterised, in the solid state, by single crystal X-ray crystallography. Biological assays of the library of compounds against Trypanosoma brucei brucei (T. b brucei) revealed a range of trypanocidal activities. A first generation library activity showed biological activity as low as 6.25 μM (minimum inhibitory concentration, MIC value). Structure activity relationships in this work revealed that an aromatic substituent at the C3 and N1 positions of the 1,4-benzodiazepin-2-one are important for improved bioactivity. In order to improve biological activity, putative P-2 transporter motifs were exploited in the 1,4-benzodiazepin-2-ones. Structural activity relationships indicate that the inclusion of a guanidine moiety, a putative P-2 transporter motif, can improve the biological activity of these molecules. In vitro screening of these compounds showed a range of antitrypanosomal activities against T. b.brucei, with a number in the low micromolar range (MIC ≥ 0.78 μm) including (S)-1-(4-((3-benzyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-1-yl)methyl)phenyl)guanidine, (S)-1-(3-((3-benzyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-1-yl)methyl)phenyl)guanidine, (S)-1-(4-((3-benzyl-5-cyclohexyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-1yl)methyl)phenyl)-guanidine and (S)-1-(1-benzyl-5-cyclohexyl-3-isopropyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-7-yl)guanidine)phenylquanidine.
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He, Shanshan. "Neglected Tropical Disease Chemotherapy: Mechanistic Characterization of Antitrypanosomal Dihydroquinolines and Development of a High Throughput Antileishmanial Screening Assay." The Ohio State University, 2012. http://rave.ohiolink.edu/etdc/view?acc_num=osu1337980540.

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Maiwald, Franziska [Verfasser], and Conrad [Akademischer Betreuer] Kunick. "Synthese neuer 4-Azapaullone als potenziell antitrypanosomale Wirkstoffe / Franziska Maiwald ; Betreuer: Conrad Kunick." Braunschweig : Technische Universität Braunschweig, 2013. http://d-nb.info/1175821853/34.

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Murebwayire, Sengabo. "Etudes des propriétés antiplasmodiales, antitrypanosomales et inhibitrices d'acétylcholinestérase de triclisia sacleuxii (Pierre) Diels "Menispermaceae"." Doctoral thesis, Universite Libre de Bruxelles, 2008. http://hdl.handle.net/2013/ULB-DIPOT:oai:dipot.ulb.ac.be:2013/210506.

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Le paludisme, la maladie la plus dévastatrice des régions tropicales fait l’objet de nombreuses recherches ayant pour but de trouver des médicaments préventifs, du matériel de protection, de nouveaux traitements, des vaccins, …

Notre travail s’est inscrit dans la recherche des composés naturels actifs sur l’agent pathogène, le Plasmodium. Nos investigations phytochimiques et pharmacologiques ont porté sur Triclisia sacleuxii, une plante utilisée en médecine traditionnelle pour traiter diverses maladies dont deux parasitaires: la schistosomiase et l’ascardiose. Elle est aussi employée dans la préparation du poison de flèche. De plus, T. sacleuxii appartient à la famille des Menispermaceae, une famille riche en alcaloïdes bisbenzylisoquinoléiques (BBIQ). Ces composés ont de nombreuses propriétés biologiques dont l’activité antipaludique et trypanocide. Plusieurs autres espèces appartenant au genre Triclisia sont utilisées en médecine traditionnelle pour traiter la fièvre, le paludisme et d’autres pathologies. Ces éléments ont motivé la recherche dans cette plante des composés à activité antiplasmodiale. En effet, la plupart des composés que nous en avons isolés (p 12) sont actifs aussi bien sur la souche chloroquino-sensible (3D7) que sur la souche chloroquino-résistante (W2) que nous avons testées.

Deux d’entre eux ont en plus une activité plus élevée vis-à-vis de la souche choroquino-résistante.

Les composés actifs sur Plasmodium falciparum ont également montré une toxicité à l’égard de Trypanosoma brucei brucei, une sous-espèce apparentée à celles qui sont à la base de la maladie du sommeil en Afrique Centrale et de l’Est.

A part les usages mentionnés précédemment, T. sacleuxii est en plus employée comme antidote contre les morsures de serpents. Ce qui voudrait dire qu’elle pourrait renfermer des inhibiteurs d’enzymes.

Aussi, des BBIQ ont déjà démontré une activité inhibitrice de l’acétylcholinéstérase (AChE) et des phospholipases A2. Sur base de ces informations, nous avons assigné un troisième objectif à notre investigation qui cible l’AChE en correlation avec la maladie d’Alzheimer (MA). La MA est une pathologie neurodégénérative qui affecte en général les personnes âgées de plus de 60 ans, caractérisée entre autres par une perte progressive de la mémoire, une détérioration de plusieurs fonctions cognitives, de troubles neurologiques et du comportement, … Les différents extraits alcaloïdiques ont montré un degré d’inhibition de l’AChE élevé ( 80 - 90%) à une concentration de 100 μg/ml. Avec les composés purs, l’inhibition est très variable (30 - 90 %) suivant la structure. Enfin, nous avons effectué des investigations pour déterminer le mode d’action antiplasmodiale des BBIQ majeurs isolés de T. sacleuxii. Il apparaît que non seulement toutes les BBIQ n’agissent pas par un même mode d’action, mais aussi un même composé pourrait agir simultanément suivant deux ou plusieurs mécanismes différents.

Malaria, the most devastating disease in tropical areas, is currently a target of numerous researches, aiming to find preventive medicines, protective tools, new treatments and vaccines. In a search for antiplasmodial natural compounds, we have undertaken phytochemical and pharmacological investigations on Triclisia sacleuxii, used in traditional medicine to treat various ailments including two parasitological diseases; schistosomiasis and ascariasis. It is also used as an arrow poison.

Triclisia sacleuxii belongs to the Menispermaceae family, which is known to contain bisbenzylisoquinolines. These components have shown various biological activities among which antimalarial and trypanocidal activity. Furthermore, many Triclisia species are used in traditional medicine for treating fever and malaria along with other disorders.

With this background the research was set out to investigate on possible antiparasitic compounds active against Plasmodium falciparum.

Most of the compounds isolated in this work were active towards both chloroquine sensitive strain (3D7) and chloroquine resistant Plasmodium strain (W2). Interestingly some of them demonstrated selectivity for the resistant strain.

The compounds which displayed antiplasmodial activity also showed toxicity against Trypanosoma brucei brucei, a parasite related to those which cause sleeping sickness.

Besides Triclisia sacleuxii traditional uses mentioned above, it is also used as a snakebites antidote. This suggests that it might contain enzymes inhibitors. Additionally, in previous works, bisbenzylisoquinolines which are believed to be present in T. sacleuxii, have displayed phospholipases A2 and acetylcholinesterase inhibitory activity. On the basis of these informations, the third aim of our investigation targeted acetylcholinesterase (AChE), an enzyme involved in Alzheimer’s disease (AD). AD is a neurodegenerative disease occurring mostly in people aged beyond 60 years, characterised by a progressive loss of memory, impairement of multiple cognitive functions, neurological and behavior disorders, Our results have demonstrated that leaves, stems and roots alkaloidal fractions have high anti-AChE activity. Pure compounds exhibited a structure-dependent activity ranging from 30 up to 90% at a concentration of 100μg/ml).

Finally, we have undertaken an investigation on the antiplasmodial mode of action of the major alkaloids. It appears that not only the BBIQ do not act by a same mechanism, but also a single compound may act by more than one mode of action.
Doctorat en Sciences biomédicales et pharmaceutiques
info:eu-repo/semantics/nonPublished

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Wendling, Ana Paula Barbosa. "Desempenho da pesquisa de anticorpos antiTrypanosoma cruzi, por citometria de fluxo, na monitoração precoce de cura pósterapêutica etiológica da doença de Chagas." Universidade Federal de Minas Gerais, 2006. http://hdl.handle.net/1843/ECJS-7GJN9A.

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Specific therapy of chronic Chagas disease aims mainly to reduce parasitemia, besides preventing and reducing symptoms. However, monitoring treatment efficacy still remains unclear due to the lack of laboratorial methods that could certify a complete parasitological cure. Currently, the cure criteria used by various researchers is based on repeated serological and parasitological negative tests. Several studies have shown that serology can remain positive for decades after specific therapeutics. The introduction of highly sensitive techniques such as specific antibodies detection by flow citometry brought new perspectives in Chagas disease cure monitoring. Herein, we developed two studies aiming to evaluate the performance of FC-AFEA and FC-ALTA techniques on post therapeutic evaluation. Our results showed that in a retrospective study using a population with 10 to 15 years of followup after specific therapeutics (n=60), FC-AFEA was capable to segregate cured chagasic patients from non cured ones. Since the method presents a very high sensitivity, some modifications on the original technique, like the utilization of higher dilutions and higher cutoffs, were shown to be necessary. In a prospective study along five years of post therapeutic follow-up (n=44), none of the serological methods used (FC-AFEA, FC-ALTA, IIF, IHA, ELISA, PaGIA) evidenced seronegativity. Nevertheless, we observed that the etiological treatment induced a decrease on FC-AFEA and FC-ALTA reactivity intensity. In addition, in patients presenting post therapy negative hemocultures (TEA), we could identify two subgroups of patients based on their magnitude of reactivity decrease. It is possible that patients with therapeutic success are included in the subgroup presenting higher reactivity decrease. Among the conventional serological tests applied in this study, IHA showed more titer variations, creating difficulties for its use on cure monitoring. IIF was capable to identify reactivity decrease in more than 2 titers in some patients of TEA group. ELISA and PaGIA, in the way they are standardized for diagnostic proposal, were not able to segregate treated and non-treated patients, indicating that modifications on the criterion have to be made for cure monitoring. Therefore, we conclude serology presents important limitations on early cure definition after etiological treatment of chronic Chagas disease. Seroreversion seems to be an inadequate approach for this purpose. Studies should be supported in order to investigate other markers associated to the presence of active infection other than searching for anti-T. cruzi antibodies.
O objetivo da terapeutica especifica da fase cronica da doenca de Chagas e a reducao da parasitemia, alem da prevencao e reducao dos sintomas. Entretanto, a monitoracao da eficacia do tratamento ainda e insatisfatoria, devido a ausencia de metodos laboratoriais que certifiquem a cura. Atualmente, o criterio de cura utilizado por diversos pesquisadores baseiase na negativacao de testes sorologicos e parasitologicos. Diversos estudos mostram que apos a terapia especifica, os testes sorologicos podem permanecer positivos por decadas. A introducao de tecnicas mais sensiveis como a pesquisa de anticorpos por citometria de fluxo trouxe novas perspectivas no monitoramento de cura da doenca de Chagas. Neste contexto, realizamos dois estudos que objetivaram avaliar o desempenho das tecnicas de FC-AFEA e FC-ALTA na avaliacao pos-terapeutica. Nossos resultados mostraram que, em um estudo retrospectivo em uma populacao com 10 a 15 anos de acompanhamento pos-terapeutico (n=60), a FC-AFEA foi capaz de discriminar pacientes chagasicos curados daqueles nao curados. Em virtude da alta sensibilidade do metodo, foram necessarias modificacoes do criterio de positividade da tecnica original utilizado para diagnostico, como o emprego de diluicoes mais altas e elevacao do ponto de corte. Em outro estudo, prospectivo, ao longo de cinco anos de acompanhamento pos-terapeutico (n=44), nenhum dos metodos sorologicos utilizados (FC-AFEA, FC-ALTA, IFI, HAI, ELISA, PaGIA) evidenciou soronegatividade. Entretanto, observou-se que o tratamento etiologico induziu queda na reatividade de FCAFEA e FC-ALTA. Ainda, no grupo de pacientes tratados que apresentavam hemoculturas pos-tratamento negativas (TEA), foi possivel identificar dois subgrupos de pacientes de acordo com a magnitude da queda na reatividade, sendo provavel que pacientes com sucesso terapeutico estejam compreendidos entre aqueles que evoluiram com maior queda de reatividade. Dentre os testes sorologicos convencionais empregados tambem nesta populacao, a HAI mostrou maior variacao dos titulos, dificultando seu emprego na monitoracao recente de cura e mostrando-se insatisfatorio no controle de cura. A IFI foi capaz de identificar queda na reatividade . 2 titulos em alguns pacientes do grupo TEA. A ELISA e o PaGIA, da forma como estao padronizados para uso no diagnostico, nao foram capazes de segregar pacientes tratados ou nao, indicando que para seu uso na monitoracao de cura, os criterios de positividade devam ser adequados. Conclui-se que o uso de testes sorologicos apresenta limitacoes na definicao de cura precoce apos tratamento etiologico da forma cronica da doenca de Chagas. A verificacao de ausencia de anticorpos anti-proteinas derivadas do agente infeccioso parece ser um criterio inadequado de cura. Devem-se incentivar estudos objetivando a procura de outros marcadores associados a presenca ativa da infeccao que nao a presenca de anticorpos anti-T. cruzi.
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Book chapters on the topic "Antitrypanosomal"

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Alberti, Andrés Sánchez, Natacha Cerny, Augusto Bivona, and Silvia I. Cazorla. "Antitrypanosomal and Antileishmanial Activities." In Sesquiterpene Lactones, 175–96. Cham: Springer International Publishing, 2018. http://dx.doi.org/10.1007/978-3-319-78274-4_8.

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Nardella, Flore, Jean-Baptiste Gallé, Mélanie Bourjot, Bernard Weniger, and Catherine Vonthron-Sénécheau. "Antileishmanial and Antitrypanosomal Activities of Flavonoids." In Sustainable Development and Biodiversity, 163–94. Cham: Springer International Publishing, 2018. http://dx.doi.org/10.1007/978-3-319-67045-4_7.

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Valente, María, Antonio E. Vidal, and Dolores González Pacanowska. "Potential of Pyrimidine Metabolism for Antitrypanosomal Drug Discovery." In Comprehensive Analysis of Parasite Biology: From Metabolism to Drug Discovery, 147–70. Weinheim, Germany: Wiley-VCH Verlag GmbH & Co. KGaA, 2016. http://dx.doi.org/10.1002/9783527694082.ch6.

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"Antitrypanosomal and Antileishmanial Targets." In Chemotherapeutic Targets in Parasites, 90–128. Cambridge University Press, 2002. http://dx.doi.org/10.1017/cbo9780511546440.006.

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Meneguetti, Dionatas Ulises de Oliveira, Adila Costa de Jesus, Fernanda Portela Madeira, and Romeu Paulo Martins Silva. "ANTITRYPANOSOMAL ETHNOPHARMACOLOGY IN THE BRAZILIAN AMAZON." In Patologias: Doenças Parasitárias, 55–72. Antonella Carvalho de Oliveira, 2019. http://dx.doi.org/10.22533/at.ed.9781918037.

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Kryshchyshyn, Anna, Danylo Kaminskyy, Philippe Grellier, and Roman Lesyk. "Thiazolidinone-Related Heterocyclic Compounds as Potential Antitrypanosomal Agents." In Azoles - Synthesis, Properties, Applications and Perspectives [Working Title]. IntechOpen, 2020. http://dx.doi.org/10.5772/intechopen.91861.

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Taber, Douglass. "Complex Cyclic Ethers: (+)-Conocarpan (Hashimoto), (-)-Brevisamide (Satake/ Tachibana), (+)-Bruguierol A (Fañanás/ Rodríguez), (-)-Berkelic Acid (Snider), and (-)-Aigialomycin D (Harvey)." In Organic Synthesis. Oxford University Press, 2011. http://dx.doi.org/10.1093/oso/9780199764549.003.0052.

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( + )-Conocarpan 3, isolated from the wood of Conocarpus erectus , exhibits insecticidal, antifungal and antitrypanosomal activity. Shunichi Hashimoto of Hokkaido University developed (J. Org. Chem. 2009, 74 , 4418) a chiral Rh (II) carboxylate that effected the cyclization of 1 to 2, setting the absolute configuration of 3. The dinoflagellate Karenia brevis produces the brevetoxins, a family of complex polyethers. Recently, the first N-containing cyclic ether, (-)-Brevisamide 6, was isolated from K. brevis . Masayuki Satake and Kazuo Tachibana of the University of Tokyo, in their synthesis of 6 (Organic Lett. 2009, 11, 217) found it convenient to set the relative configuration around the six-membered ring by double hydroboration/oxidation of the diene 4. ( + )-Bruguierol A 9, isolated from the mangrove Bruguiera gymmorrhiza, has an unusual bridged structure. Francisco J. Fañanás and Félix Rodríguez of the Universidad de Oviedo conceived (J. Org. Chem. 2009, 74, 932) an elegant approach to the construction of 9, based on the Pt-mediated addition of the alcohol of 7 to the alkyne to give a transient enol ether. It is not clear whether the subsequent intramolecular electrophilic addition to the aromatic ring is mediated by the Pt, or by a trace of adventitious acid. The overall transformation was remarkably efficient. The Berkeley Pit in Butte, Montana, is an abandoned open-pit copper mine filled with 30 billion gallons of pH = 2.5 water heavily contaminated with, inter alia , copper, cadmium, arsenic and zinc. Remarkably, microorganisms can be cultured from that water. (-)-Berkelic Acid 13 , isolated from a Penicillium fungus, showed selective activity against OVCAR-3 ovarian cancer. Barry B. Snider of Brandeis University set (Angew. Chem. Int. Ed. 2009, 48, 1283) the absolute configuration of the central five-membered ring ether of 13 by conjugate addition of the enantiomerically-pure reagent 11 to the prochiral lactone 10. (-)-Aigialomycin D 17, isolated from the mangrove fungus Aigialus parvus , was found to be a selective inhibitor of the kinases CDK1, CDK5 and GSK3.
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Conference papers on the topic "Antitrypanosomal"

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VazquezRodriguez, Saleta, Maria João Matos, Roberto Figueroa Guíñez, Juan Diego Maya, Michel Lapier, Claudio Olea-Azar, Fernanda Pérez-Cruz, Eugenio Uriarte, and Lourdes Santana. "Coumarin-chalcone Derivatives as Potential Antitrypanosomal and Antioxidant Compounds." In The 16th International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2012. http://dx.doi.org/10.3390/ecsoc-16-01037.

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Adefolaju, Oluwaferanmi, and Abdulkadir Abubakar. "ANTITRYPANOSOMAL POTENTIAL OF BUCHHOLZIA CORIACEA SEED EXTRACTS IN MICE." In MOL2NET 2019, International Conference on Multidisciplinary Sciences, 5th edition. Basel, Switzerland: MDPI, 2019. http://dx.doi.org/10.3390/mol2net-05-06242.

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Kimani, Njogu, Josphat Matasyoh, Marcel Kaiser, Mauro Nogueira, Gustavo Trossini, and Thomas Schmidt. "An extended study on quantitative structure-antitrypanosomal activity relationships of sesquiterpene lactones." In 4th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2018. http://dx.doi.org/10.3390/ecmc-4-05591.

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Suckling, Colin J., Fraser Scott, Abedawn Khalaf, Kirsten Gillingwater, Liam Morrison, Harry de Koning, Michael Barrett, and Federica Giordani. "Minor Groove Binders for DNA as Antitrypanosomal Agents: the Veterinary Context." In 3rd International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2017. http://dx.doi.org/10.3390/ecmc-3-04647.

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Soares, Ozildéia, Gabriela R. Hurtado, Luiz H. Viana, Sérgio de Albuquerque, and Adriano C. M. Baroni. "Synthesis of Isoxazolic analogues derivatives of Grandisin and Veraguensin neolignans with anti-leishmania and antitrypanosomal activities." In 15th Brazilian Meeting on Organic Synthesis. São Paulo: Editora Edgard Blücher, 2013. http://dx.doi.org/10.5151/chempro-15bmos-bmos2013_20139410384.

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Montero-Torres, Alina, María Vega, Yovani Marrero-Ponce, Miriam Rolón, Alicia Gómez-Barrio, José Escario, Vicente Arán, Antonio Martínez-Fernández, and Alfredo Meneses-Marcel. "A Novel Non-Stochastic Quadratic Fingerprints-Based Approach for the “in silico” Discovery of New Antitrypanosomal Compounds." In The 9th International Electronic Conference on Synthetic Organic Chemistry. Basel, Switzerland: MDPI, 2005. http://dx.doi.org/10.3390/ecsoc-9-01663.

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Lago, J., S. Grecco, T. Costa-Silva, F. Sousa, C. Tcacenco, C. Andrade, P. Sartorelli, and A. Tempone. "Neolignans from leaves of Nectandra leucantha (Lauraceae) display in vitro antitrypanosomal activity via plasma membrane and mitochondrial damages." In GA 2017 – Book of Abstracts. Georg Thieme Verlag KG, 2017. http://dx.doi.org/10.1055/s-0037-1608157.

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Kimani, M., J. Matasyoh, M. Kaiser, R. Brun, and TJ Schmidt. "Antitrypanosomale Sesquiterpenlactone aus Vernonia cinerascens." In Phytotherapie 2017 „Von der Innovation zur Evidenz“. Georg Thieme Verlag KG, 2017. http://dx.doi.org/10.1055/s-0037-1607128.

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Reports on the topic "Antitrypanosomal"

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Markovac, A., D. J. Dagli, R. L. Kalamas, G. S. Wu, A. B. Ash, and C. L. Stevens. Synthesis of Improved Antileishmanial and Antitrypanosomal Drugs Treatment and Prophylaxis. Fort Belvoir, VA: Defense Technical Information Center, November 1986. http://dx.doi.org/10.21236/adb110976.

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Markovac, A., D. J. Dagli, A. B. Ash, and C. L. Stevens. Synthesis of Improved Antileishmanial and Antitrypanosomal Drugs, Treatment and Prophylaxis. Fort Belvoir, VA: Defense Technical Information Center, February 1988. http://dx.doi.org/10.21236/adb121621.

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Markovac, A., D. J. Dagli, A. B. Ash, and C. L. Stevens. Synthesis of Improved Antileishmanial and Antitrypanosomal Drugs, Treatment and Prophylaxis. Fort Belvoir, VA: Defense Technical Information Center, April 1989. http://dx.doi.org/10.21236/adb145101.

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