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Antiparasitic drugs

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https://www.readbyqxmd.com/read/28421410/antiparasitic-sesquiterpenes-from-the-cameroonian-spice-scleria-striatinux-and-preliminary-in-vitro-and-in-silico-dmpk-assessment
#1
Kennedy D Nyongbela, Fidele Ntie-Kang, Thomas R Hoye, Simon M N Efange
The antiparasitic activity and preliminary in vitro and in silico drug metabolism and pharmacokinetic (DMPK) assessment of six isomeric sesquiterpenes (1-6), isolated from the Cameroonian spice Scleria striatinux De Wild (Cyperaceae) is reported. The study was prompted by the observation that two of the compounds (1 and 2) exhibited varying levels of antiparasitic activity on Plasmodium falciparum, Trypanosoma brucei rhodesiense, Trypanosoma cruzi and Leishmania donovani. The in silico method employed a total of 46 descriptors, calculated using Schrödinger QikProp software...
April 18, 2017: Natural Products and Bioprospecting
https://www.readbyqxmd.com/read/28405061/emergency-department-discharge-prescription-errors-in-an-academic-medical-center
#2
Kelly A Murray, April Belanger, Lauren T Devine, Aaron Lane, Michelle E Condren
This study described discharge prescription medication errors written for emergency department patients. This study used content analysis in a cross-sectional design to systematically categorize prescription errors found in a report of 1000 discharge prescriptions submitted in the electronic medical record in February 2015. Two pharmacy team members reviewed the discharge prescription list for errors. Open-ended data were coded by an additional rater for agreement on coding categories. Coding was based upon majority rule...
April 2017: Proceedings of the Baylor University Medical Center
https://www.readbyqxmd.com/read/28386903/long-term-broiler-litter-amendments-can-alter-the-soil-s-capacity-to-sorb-monensin
#3
Sarah A Doydora, Peizhe Sun, Miguel Cabrera, Nehru Mantripragada, John Rema, Spyros G Pavlostathis, Ching-Hua Huang, Aaron Thompson
Monensin is a common antiparasitic drug given to poultry that contaminates poultry manure and bedding material (broiler litter). As broiler litter is commonly applied to agricultural fields as fertilizer, monensin could be released beyond the farm if it is not retained or degraded in the soil. This study aimed to assess the impact of long-term surface application of broiler litter (i.e., 17 years) on the capacity of pasture soil to sorb monensin. The soils were exposed to a range of monensin concentrations (0...
April 7, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28375176/design-synthesis-and-biological-evaluation-of-2-2-amino-5-6-nitro-1h-benzimidazol-1-yl-n-arylacetamides-as-antiprotozoal-agents
#4
Emanuel Hernández-Núñez, Hugo Tlahuext, Rosa Moo-Puc, Diego Moreno, María Ortencia González-Díaz, Gabriel Navarrete Vázquez
Parasitic diseases are a public health problem affecting millions of people worldwide. One of the scaffolds used in several drugs for the treatment of parasitic diseases is the benzimidazole moiety, a heterocyclic aromatic compound. This compound is a crucial pharmacophore group and is considered a privileged structure in medicinal chemistry. In this study, the benzimidazole core served as a model for the synthesis of a series of 2-(2-amino-5(6)-nitro-1H-benzimidazol-1-yl)-N-arylacetamides 1-8 as benznidazole analogues...
April 4, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28337329/antiparasitic-lead-discovery-toward-optimization-of-a-chemotype-with-activity-against-multiple-protozoan-parasites
#5
William Devine, Sarah M Thomas, Jessey Erath, Kelly A Bachovchin, Patricia J Lee, Susan E Leed, Ana Rodriguez, Richard J Sciotti, Kojo Mensa-Wilmot, Michael P Pollastri
Human African trypanosomiasis (HAT), Chagas disease, and leishmaniasis present a significant burden across the developing world. Existing therapeutics for these protozoal neglected tropical diseases suffer from severe side effects and toxicity. Previously, NEU-1045 (3) was identified as a promising lead with cross-pathogen activity, though it possessed poor physicochemical properties. We have designed a library of analogues with improved calculated physicochemical properties built on the quinoline scaffold of 3 incorporating small, polar aminoheterocycles in place of the 4-(3-fluorobenzyloxy)aniline substituent...
March 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28319176/insight-into-the-mechanism-of-action-of-temporin-sha-a-new-broad-spectrum-antiparasitic-and-antibacterial-agent
#6
Zahid Raja, Sonia André, Feten Abbassi, Vincent Humblot, Olivier Lequin, Tahar Bouceba, Isabelle Correia, Sandra Casale, Thierry Foulon, Denis Sereno, Bruno Oury, Ali Ladram
Antimicrobial peptides (AMPs) are promising drugs to kill resistant pathogens. In contrast to bacteria, protozoan parasites, such as Leishmania, were little studied. Therefore, the antiparasitic mechanism of AMPs is still unclear. In this study, we sought to get further insight into this mechanism by focusing our attention on temporin-SHa (SHa), a small broad-spectrum AMP previously shown to be active against Leishmania infantum. To improve activity, we designed analogs of SHa and compared the antibacterial and antiparasitic mechanisms...
2017: PloS One
https://www.readbyqxmd.com/read/28283781/gold-compounds-as-cysteine-protease-inhibitors-perspectives-for-pharmaceutical-application-as-antiparasitic-agents
#7
Lara Massai, Luigi Messori, Nicola Micale, Tanja Schirmeister, Louis Maes, Dolores Fregona, Maria Agostina Cinellu, Chiara Gabbiani
Gold compounds form a new class of promising metal-based drugs with a number of potential therapeutic applications, particularly in the fields of anticancer and antimicrobial treatments. Previous research revealed that a group of structurally diverse gold compounds cause conspicuous inhibition of the protease activities of the human proteasome. Given the pharmacological importance of protease inhibition, the present study further explored whether these gold compounds might inhibit a few other proteases that are accepted druggable targets for disease treatment...
March 10, 2017: Biometals: An International Journal on the Role of Metal Ions in Biology, Biochemistry, and Medicine
https://www.readbyqxmd.com/read/28282886/chroman-4-one-derivatives-targeting-pteridine-reductase-1-and-showing-anti-parasitic-activity
#8
Flavio Di Pisa, Giacomo Landi, Lucia Dello Iacono, Cecilia Pozzi, Chiara Borsari, Stefania Ferrari, Matteo Santucci, Nuno Santarem, Anabela Cordeiro-da-Silva, Carolina B Moraes, Laura M Alcantara, Vanessa Fontana, Lucio H Freitas-Junior, Sheraz Gul, Maria Kuzikov, Birte Behrens, Ina Pöhner, Rebecca C Wade, Maria Paola Costi, Stefano Mangani
Flavonoids have previously been identified as antiparasitic agents and pteridine reductase 1 (PTR1) inhibitors. Herein, we focus our attention on the chroman-4-one scaffold. Three chroman-4-one analogues (1-3) of previously published chromen-4-one derivatives were synthesized and biologically evaluated against parasitic enzymes (Trypanosoma brucei PTR1-TbPTR1 and Leishmania major-LmPTR1) and parasites (Trypanosoma brucei and Leishmania infantum). A crystal structure of TbPTR1 in complex with compound 1 and the first crystal structures of LmPTR1-flavanone complexes (compounds 1 and 3) were solved...
March 8, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28275906/molecular-modeling-and-infrared-and-raman-spectroscopy-of-the-crystal-structure-of-the-chiral-antiparasitic-drug-praziquantel
#9
Ana Borrego-Sánchez, Alfonso Hernández-Laguna, C Ignacio Sainz-Díaz
Anthelmintic praziquantel (PZQ) and its molecular and crystal lattice structures were studied by means of atomistic calculations based on empirical interatomic potentials and quantum mechanical methods (DFT). This chiral drug presents several crystal polymorphs due to the enantiomers (either R or S) or the racemic crystal, and different molecular conformations. The relative configurations of the carbonyl groups in PZQ define these conformations that produce different polymorphs. The polarity of these conformers is quite different and their relative population can vary in media with different polarity...
April 2017: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/28274284/the-antimalarial-action-of-fk506-and-rapamycin-evidence-for-a-direct-effect-on-fk506-binding-protein-pffkbp35
#10
Paul Monaghan, Darren B Leneghan, Wesley Shaw, Angus Bell
FK506 and rapamycin (Rap) are immunosuppressive drugs that act principally on T-lymphocytes. The receptors for both drugs are FK506-binding proteins (FKBPs), but the molecular mechanisms of immunosuppression differ. An FK506-FKBP complex inhibits the protein phosphatase calcineurin, blocking a key step in T-cell activation, while the Rap -FKBP complex binds to the protein kinase target of rapamycin (TOR), which is involved in a subsequent signalling pathway. Both drugs, and certain non-immunosuppressive compounds related to FK506, have potent antimalarial activity...
March 9, 2017: Parasitology
https://www.readbyqxmd.com/read/28265521/genetic-and-structural-study-of-dna-directed-rna-polymerase-ii-of-trypanosoma-brucei-towards-the-designing-of-novel-antiparasitic-agents
#11
Louis Papageorgiou, Vasileios Megalooikonomou, Dimitrios Vlachakis
Trypanosoma brucei brucei (TBB) belongs to the unicellular parasitic protozoa organisms, specifically to the Trypanosoma genus of the Trypanosomatidae class. A variety of different vertebrate species can be infected by TBB, including humans and animals. Under particular conditions, the TBB can be hosted by wild and domestic animals; therefore, an important reservoir of infection always remains available to transmit through tsetse flies. Although the TBB parasite is one of the leading causes of death in the most underdeveloped countries, to date there is neither vaccination available nor any drug against TBB infection...
2017: PeerJ
https://www.readbyqxmd.com/read/28264505/antiprotozoal-activity-of-triazole-derivatives-of-dehydroabietic-acid-and-oleanolic-acid
#12
Mariano Walter Pertino, Celeste Vega, Miriam Rolón, Cathia Coronel, Antonieta Rojas de Arias, Guillermo Schmeda-Hirschmann
Tropical parasitic diseases such as Chagas disease and leishmaniasis are considered a major public health problem affecting hundreds of millions of people worldwide. As the drugs currently used to treat these diseases have several disadvantages and side effects, there is an urgent need for new drugs with better selectivity and less toxicity. Structural modifications of naturally occurring and synthetic compounds using click chemistry have enabled access to derivatives with promising antiparasitic activity. The antiprotozoal activity of the terpenes dehydroabietic acid, dehydroabietinol, oleanolic acid, and 34 synthetic derivatives were evaluated against epimastigote forms of Trypanosoma cruzi and promastigotes of Leishmaniabraziliensis and Leishmania infantum...
February 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28263719/mechanism-of-ascaridole-activation-in-leishmania
#13
Gerald Geroldinger, Matthias Tonner, Hubert Hettegger, Markus Bacher, Lianet Monzote, Martin Walter, Katrin Staniek, Thomas Rosenau, Lars Gille
Endoperoxides (EP) are an emerging class of drugs which have potential in antiparasitic therapy, but also in other fields. For malaria therapy the EP artemisinin (Art) and its derivatives are successfully used. We have shown in the past that the EP ascaridole (Asc) is useful for the treatment of cutaneous leishmaniasis in a mouse model. Biomimetic experiments suggested that these drugs need activation in the respective target pathogens to exert their function. In spite of this idea, direct activation of EP to radicals inside cells has never been demonstrated...
March 2, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28257952/in-vitro-immunomodulatory-effects-of-microemulsions-with-levamisole-delivery-systems-on-blood-phagocytes-interacting-with-giardia-lamblia
#14
Mara Rosa Gil Hernandes, Lucélia Campelo Albuquerque Moraes, Elton Brito Ribeiro, Danny Laura Gomes Fagundes, Adenilda Cristina Honorio-França, Eduardo Luzía França
BACKGROUND: Giardiasis is one of the main parasites that infect the gastrointestinal tract of humans, affecting hundreds of millions of people worldwide, particularly in developing countries. Antiparasitics administered to treat giardiasis are inefficient in 20% of the cases, usually because of parasite resistance and side effects. In this scenario, microemulsions are a promising pharmaceutical alternative as carriers of molecules with therapeutic action that stimulate the immune system...
February 28, 2017: Parasitology International
https://www.readbyqxmd.com/read/28245890/one-hundred-years-of-neglect-in-paediatric-schistosomiasis
#15
Amaya L Bustinduy, Stephen Wright, Elizabeth C Joekes, Narcis B Kabatereine, Jutta Reinhard-Rupp, Charles H King, J Russell Stothard
Early in the history of schistosomiasis research, children under 5 years of age were known to be infected. Although this problem was recognized over 100 years ago, insufficient action has been taken to address this issue. Under current policy, such infected children only receive their first antiparasitic treatment (praziquantel - PZQ) upon entry into primary school as current mass drug administration programmes typically target school-aged children. For many infected children, they will wait up to 6 years before receiving their first medication and significant schistosomiasis-related morbidity may have already established...
March 1, 2017: Parasitology
https://www.readbyqxmd.com/read/28245779/imidazole-an-essential-edifice-for-the-identification-of-new-lead-compounds-and-drug-development
#16
Nishtha Shalmali, Md Rahmat Ali, Sandhya Bawa
In recent years, a drastic rise has been observed in incidences of resistance, low efficacy rates and toxicities to various drugs used in therapeutic application. It has been observed that presence of imidazole nucleus in several categories of therapeutic agents such as antimicrobials, antivirals, antiparasites, anticancer, anti-inflammatory, antidiabetics etc. has made it a vital anchor for the development of new therapeutic agents. But, there is a need to couple the newest information with the already available knowledge to recognize the present standing of imidazole motif in medicinal chemistry research...
February 28, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28242550/desing-and-synthesis-of-potent-anti-trypanosoma-cruzi-agents-new-thiazoles-derivatives-which-induce-apoptotic-parasite-death
#17
Elany Barbosa da Silva, Dayane Albuquerque Oliveira E Silva, Arsênio Rodrigues Oliveira, Carlos Henrique da Silva Mendes, Thiago André Ramos Dos Santos, Aline Caroline da Silva, Maria Carolina Acioly de Castro, Rafaela Salgado Ferreira, Diogo Rodrigo Magalhães Moreira, Marcos Veríssimo de Oliveira Cardoso, Carlos Alberto de Simone, Valéria Rêgo Alves Pereira, Ana Cristina Lima Leite
Chagas disease, caused by the kinetoplastid protozoan parasite Trypanosoma cruzi, remains a relevant cause of illness and premature death and it is estimated that 6 million to 7 million people are infected worldwide. Although chemotherapy options are limited presenting serious problems, such as low efficacy and high toxicity. T. cruzi is susceptible to thiazoles, making this class of compounds appealing for drug development. Previously, thiazoles resulted in an increase in anti-T. cruzi activity in comparison to thiosemicarbazones...
April 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28238819/alkylphospholipids-an-update-on-molecular-mechanisms-and-clinical-relevance
#18
REVIEW
Pablo Ríos-Marco, Carmen Marco, Xiomara Gálvez, Jose M Jiménez-López, María P Carrasco
Alkylphospholipid (APL) represent a new class of drugs which do not interact directly with DNA but act on the cell membrane where they accumulate and interfere with lipid metabolism and signalling pathways. This review summarizes the mode of action at the molecular level of these compounds. In this sense, a diversity of mechanisms has been suggested to explain the actions of clinically-relevant APLs, in particular, in cancer treatment. One consistently reported finding is that APLs reduce the biosynthesis of phosphatidylcholine (PC) by inhibiting the rate-limiting enzyme CTP:phosphocholine cytidylyltransferase (CT)...
February 23, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28236702/antiparasitic-activity-of-1-3-dioxolanes-containing-tellurium-in-trichomonas-vaginalis
#19
Ângela Sena-Lopes, Raquel Nascimento das Neves, Francisco Silvestre Brilhante Bezerra, Mara Thais de Oliveira Silva, Patrick C Nobre, Gelson Perin, Diego Alves, Lucielli Savegnago, Karine Rech Begnini, Fabiana Kommling Seixas, Tiago Collares, Sibele Borsuk
The increased prevalence of metronidazole-resistant infections has resulted in a search for alternative drugs for the treatment of trichomoniasis. In the present study, we report the preparation and in vitro activity of three 1,3-dioxolanes that contain tellurium (PTeDOX 01, PTeDOX 02, and PTeDOX 03) against Trichomonas vaginalis. Six concentrations of these compounds were analyzed for in vitro activity against ATCC 30236 isolate of T. vaginalis. PTeDOX 01 reported a cytotoxic effect against 100% of T. vaginalis trophozoites at a final concentration of 90μM with an IC50 of 60μM...
February 22, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28231520/medicinal-plants-used-as-anthelmintics-ethnomedical-pharmacological-and-phytochemical-studies
#20
REVIEW
Juan Carlos Romero-Benavides, Ana Lucía Ruano, Ronal Silva-Rivas, Paola Castillo-Veintimilla, Sara Vivanco-Jaramillo, Natalia Bailon-Moscoso
Intestinal parasites delay mental and physical development in children. Infection with these parasites can result in complications during pregnancy and alter the health of newborns, which has long-term effects on educational attainment and economic productivity. The appearance of resistance against classical drug treatments generates interest in the development of new deworming alternatives. We think that research of new plants species may reveal potential antiparasitic compounds. This review is focused on the use of plants and secondary metabolites against intestinal parasites...
March 31, 2017: European Journal of Medicinal Chemistry
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