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https://www.readbyqxmd.com/read/27908928/development-and-validation-of-a-normal-phase-chiral-hplc-method-for-analysis-of-afoxolaner-using-a-chiralpak%C3%A2-ad-3-column
#1
Jinyou Zhuang, Satish Kumar, Abu Rustum
Afoxolaner is a new antiparasitic molecule from the isoxazoline family that acts on the insect acarine gamma-aminobutyric acid and glutamate receptors. Isoxazoline family of compounds has been employed as active pharmaceutical ingredient in drug products prescribed for control of fleas and ticks in dogs. Afoxolaner with a chiral center at isoxazoline ring exists as a racemic mixture. A normal phase chiral high performance liquid chromatography analytical method has been developed to verify that afoxolaner is a racemic mixture as demonstrated by specific rotation, as well as to determine enantiomeric purity of single enantiomer samples...
November 2016: Journal of Chromatographic Science
https://www.readbyqxmd.com/read/27899278/benznidazole-the-trypanocidal-drug-used-for-chagas-disease-induces-hepatic-nrf2-activation-and-attenuates-the-inflammatory-response-in-a-murine-model-of-sepsis
#2
Flavia Lambertucci, Omar Motiño, Silvina Villar, Juan Pablo Rigalli, María de Luján Alvarez, Viviana Catania, Paloma Martín-Sanz, Cristina Ester Carnovale, Ariel Darío Quiroga, Daniel Eleazar Francés, María Teresa Ronco
Molecular mechanisms on sepsis progression are linked to the imbalance between reactive oxygen species (ROS) production and cellular antioxidant capacity. Previous studies demonstrated that benznidazole (BZL), known for its antiparasitic action on Trypanosoma cruzi, has immunomodulatory effects, increasing survival in C57BL/6 mice in a model of polymicrobial sepsis induced by cecal ligation puncture (CLP). The mechanism by which BZL inhibits inflammatory response in sepsis is poorly understood. Also, our group recently reported that BZL is able to activate the nuclear erythroid 2-related factor 2 (NRF2) in vitro...
November 26, 2016: Toxicology and Applied Pharmacology
https://www.readbyqxmd.com/read/27882479/albendazole-microcrystal-formulations-based-on-chitosan-and-cellulose-derivatives-physicochemical-characterization-and-in-vitro-parasiticidal-activity-in-trichinella-spiralis-adult-worms
#3
Josefina Priotti, Ana V Codina, Darío Leonardi, María D Vasconi, Lucila I Hinrichsen, María C Lamas
The oral route has notable advantages to administering dosage forms. One of the most important questions to solve is the poor solubility of most drugs which produces low bioavailability and delivery problems, a major challenge for the pharmaceutical industry. Albendazole is a benzimidazole carbamate extensively used in oral chemotherapy against intestinal parasites, due to its extended spectrum activity and low cost. Nevertheless, the main disadvantage is the poor bioavailability due to its very low solubility in water...
November 23, 2016: AAPS PharmSciTech
https://www.readbyqxmd.com/read/27865740/sm-p80-based-schistosomiasis-vaccine-preparation-for-human-clinical-trials
#4
REVIEW
Afzal A Siddiqui, Sabrina Z Siddiqui
Mass antiparasitic drug administration programs and other control strategies have made important contributions in reducing the global prevalence of helminths. Schistosomiasis, however, continues to spread to new geographic areas. The advent of a viable vaccine and its deployment, coupled with existing control efforts, is expected to make significant headway towards sustained schistosomiasis control. In 2016, Science ranked the schistosomiasis vaccine as one of the top 10 vaccines that needs to be urgently developed...
November 16, 2016: Trends in Parasitology
https://www.readbyqxmd.com/read/27856406/efficacy-and-safety-of-high-dose-ivermectin-for-reducing-malaria-transmission-ivermal-protocol-for-a-double-blind-randomized-placebo-controlled-dose-finding-trial-in-western-kenya
#5
Menno R Smit, Eric Ochomo, Ghaith Aljayyoussi, Titus Kwambai, Bernard Abong'o, Nabie Bayoh, John Gimnig, Aaron Samuels, Meghna Desai, Penelope A Phillips-Howard, Simon Kariuki, Duolao Wang, Steve Ward, Feiko O Ter Kuile
BACKGROUND: Innovative approaches are needed to complement existing tools for malaria elimination. Ivermectin is a broad spectrum antiparasitic endectocide clinically used for onchocerciasis and lymphatic filariasis control at single doses of 150 to 200 mcg/kg. It also shortens the lifespan of mosquitoes that feed on individuals recently treated with ivermectin. However, the effect after a 150 to 200 mcg/kg oral dose is short-lived (6 to 11 days). Modeling suggests higher doses, which prolong the mosquitocidal effects, are needed to make a significant contribution to malaria elimination...
November 17, 2016: JMIR Research Protocols
https://www.readbyqxmd.com/read/27855177/benznidazole-use-among-patients-with-chronic-chagas-cardiomyopathy-in-an-endemic-region-of-brazil
#6
Ariela Mota Ferreira, Ester Cerdeira Sabino, Lea Campos de Oliveira, Cláudia Di Lorenzo Oliveira, Clareci Silva Cardoso, Antônio Luiz Pinho Ribeiro, Desirée Sant'Ana Haikal
Chagas disease (CD) is a neglected tropical disease that affects individuals in almost every country in Latin America. There are two available drugs with antiparasitic profiles; however, only benznidazole (BZN) has been approved for commercialization in Brazil. The usefulness of prescribing BZN for patients with chronic Chagas cardiomyopathy (CCC) is controversial. There are no studies in the literature describing the extent of BZN use at this stage or the profile of patients using this drug. The present study aimed to determine the prevalence and factors associated with previous BZN use among individuals with CCC...
2016: PloS One
https://www.readbyqxmd.com/read/27821451/phase-i-clinical-trial-results-of-auranofin-a-novel-antiparasitic-agent
#7
Edmund V Capparelli, Robin Bricker-Ford, M John Rogers, James H McKerrow, Sharon L Reed
Under an NIH priority to identify new drugs to treat Class B parasitic agents, we performed high throughput screens, which identified Auranofin's (Ridaura™) activity against Entamoeba histolytica and Giardia intestinalis, major causes of water- and food-borne outbreaks. Auranofin, an oral, gold-containing compound FDA approved in 1985 for rheumatoid arthritis, was effective in vitro and in vivo against E histolytica and both metronidazole-sensitive and resistant strains of Giardia We now report the results of an NIH sponsored Phase I trial to characterize the PK and safety of auranofin in healthy volunteers using modern techniques to measure gold levels...
November 7, 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27793563/targeting-protein-translation-in-organelles-of-the-apicomplexa
#8
REVIEW
Christopher D Goodman, Charisse Flerida A Pasaje, Kit Kennedy, Geoffrey I McFadden, Stuart A Ralph
Antibiotics inhibiting protein translation have long been used to treat and prevent infections by apicomplexan parasites. These compounds kill parasites by inhibiting organellar translation, and most act specifically against the apicoplast, a relict plastid in apicomplexans. Drug resistance in Plasmodium and other apicomplexans dictates a need for development of novel targets. Some apicoplast inhibitors have a delayed onset of action, so they cannot replace fast-acting drugs, although they still fulfil important roles in treating and preventing infections...
October 25, 2016: Trends in Parasitology
https://www.readbyqxmd.com/read/27785553/are-there-any-other-compounds-isolated-from-dermacoccus-spp-at-all
#9
REVIEW
Manaf AlMatar, Mohamed Eldeeb, Essam A Makky, Fatih Köksal, Işıl Var, Begüm Kayar
Microbial-derived natural products have functional and structural diversity and complexity. For several decades, they have provided the basic foundation for most drugs available to modern medicine. Microbial-derived natural products have wide-ranging applications, especially as chemotherapeutics for various diseases and disorders. By exploring distinct microorganisms in different environments, small novel bioactive molecules with unique functionalities and biological or biomedical significance can be identified...
October 26, 2016: Current Microbiology
https://www.readbyqxmd.com/read/27770751/effects-of-a-novel-%C3%AE-lapachone-derivative-on-trypanosoma-cruzi-parasite-death-involving-apoptosis-autophagy-and-necrosis
#10
Danielle Oliveira Dos Anjos, Eliomara Sousa Sobral Alves, Vinicius Tomaz Gonçalves, Sheila Suarez Fontes, Mateus Lima Nogueira, Ana Márcia Suarez-Fontes, João Batista Neves da Costa, Fabricio Rios-Santos, Marcos André Vannier-Santos
Natural products comprise valuable sources for new antiparasitic drugs. Here we tested the effects of a novel β-lapachone derivative on Trypanosoma cruzi parasite survival and proliferation and used microscopy and cytometry techniques to approach the mechanism(s) underlying parasite death. The selectivity index determination indicate that the compound trypanocidal activity was over ten-fold more cytotoxic to epimastigotes than to macrophages or splenocytes. Scanning electron microscopy analysis revealed that the R72 β-lapachone derivative affected the T...
October 12, 2016: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/27765649/consecutive-emamectin-benzoate-and-deltamethrin-treatments-affect-the-expressions-and-activities-of-detoxification-enzymes-in-the-rainbow-trout-oncorhynchus-mykiss
#11
Juan Guillermo Cárcamo, Marcelo N Aguilar, Constanza F Carreño, Tamara Vera, Luis Arias-Darraz, Jaime E Figueroa, Alex P Romero, Marco Alvarez, Alejandro J Yañez
Rainbow trout (Oncorhynchus mykiss) subjected to three consecutive, alternating treatments with emamectin benzoate (EMB) and deltamethrin (DM) during outbreaks of Caligus rogercresseyi in a farm located in southern Chile (Hornopiren, Chiloé), were studied to determine the effects of these treatments on the protein and enzymatic activity levels of cytochrome P450 1A (CYP1A), flavin-containing monooxygenase (FMO) and glutathione S-transferase (GST) in different tissues. Consecutive and alternating EMB/DM treatments resulted in a 10-fold increase and 3-fold decrease of CYP1A protein levels in the intestine and gills, respectively...
October 17, 2016: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/27719626/metabolic-inhibitors-as-antiparasitic-drugs-pharmacological-biochemical-and-molecular-perspectives
#12
Suprabhat Mukherjee, Niladri Mukherjee, Prajna Gayen, Priya Roy, Santi P Sinha Babu
Human diseases caused by the infectious parasites have been one of the major problems throughout the evolutionary journey. Protozoan and metazoan parasitic infections result in a large number of deaths, disabilities and socio-economic loss worldwide to date. Despite our best efforts of developing suitable antiparasitics, these infections take a massive toll on human health. The prevalence of emerging resistance to the existing drugs, lack of efficacy and toxic side effects came out as added complications. Being enlisted under 'neglected' category, serious diseases like leishmaniases, filariases, trypanosomiases etc...
October 4, 2016: Current Drug Metabolism
https://www.readbyqxmd.com/read/27716755/-frequency-and-in-vitro-susceptibility-antiparasitic-of-blastocystis-hominis-from-patients-admitted-to-the-hospital-regional-lambayeque-peru
#13
Heber Silva-Díaz, Lorena Flores-Esqueche, Dunalia Llatas-Cancino, Génesis Guevara Vásquez, Teresa Silva-García
OBJECTIVE: To describe the frequency and antiparasitic in vitro susceptibility of Blastocystis hominis in patients admitted to theHospital Regional Lambayeque, Peru. MATERIAL AND METHODS: A cross-sectional study was conducted from January to August 2015 at 313 patients of all ages. B. hominis detection was performed on serial fecal samples by direct microscopic examination and microculture in modified Locke solution. The in vitro susceptibility testing against the drug metronidazole, nitazoxanide, trimethoprim-sulfamethoxazole and erythromycin was performed in 24 strains of B...
July 2016: Revista de Gastroenterología del Perú: órgano Oficial de la Sociedad de Gastroenterología del Perú
https://www.readbyqxmd.com/read/27706843/organometallic-derivatization-of-the-nematocidal-drug-monepantel-leads-to-promising-antiparasitic-drug-candidates
#14
Jeannine Hess, Malay Patra, Loganathan Rangasamy, Sandro Konatschnig, Olivier Blacque, Abdul Jabbar, Patrick Mac, Erik M Jorgensen, Robin B Gasser, Gilles Gasser
The discovery of novel drugs against animal parasites is in high demand due to drug-resistance problems encountered around the world. Herein, the synthesis and characterization of 27 organic and organometallic derivatives of the recently launched nematocidal drug monepantel (Zolvix(®) ) are described. The compounds were isolated as racemates and were characterized by (1) H, (13) C, and (19) F NMR spectroscopy, mass spectrometry, and IR spectroscopy, and their purity was verified by microanalysis. The molecular structures of nine compounds were confirmed by X-ray crystallography...
October 5, 2016: Chemistry: a European Journal
https://www.readbyqxmd.com/read/27706395/in-vitro-susceptibility-of-nematophagous-fungi-to-antiparasitic-drugs-interactions-and-implications-for-biological-control
#15
J N Vieira, F S Maia, G F Ferreira, J F Mendes, C L Gonçalves, M M Villela, D I B Pereira, P S Nascente
The fast anthelmintic resistance development has shown a limited efficiency in the control of animal's endoparasitosis and has promoted research using alternative control methods. The use of chemicals in animal anthelmintic treatment, in association with nematophagous fungi used for biological control, is a strategy that has proven to be effective in reducing the nematode population density in farm animals. This study aims to verify the in vitro susceptibility of the nematophagous fungi Arthrobotrys oligospora, Duddingtonia flagrans and Paecilomyces lilacinus against the antiparasitic drugs albendazole, thiabendazole, ivermectin, levamisole and closantel by using the Minimum Inhibitory Concentration (MIC)...
October 3, 2016: Brazilian Journal of Biology, Revista Brasleira de Biologia
https://www.readbyqxmd.com/read/27688434/anti-inflammatory-and-immunomodulatory-effects-of-antibiotics-and-their-use-in-dermatology
#16
REVIEW
Swetalina Pradhan, Bhushan Madke, Poonam Kabra, Adarsh Lata Singh
Antibiotics (antibacterial, antiviral, and antiparasitic) are class of drugs which result in either killing or inhibiting growth and multiplication of infectious organisms. Antibiotics are commonly prescribed by all specialties for treatment of infections. However, antibiotics have hitherto immunomodulatory and anti-inflammatory properties and can be exploited for various noninfectious dermatoses. Dermatologists routinely prescribe antibiotics in treatment of various noninfectious disorders. This study will review anti-inflammatory and immunomodulatory effects of antibiotics and their use in dermatology...
September 2016: Indian Journal of Dermatology
https://www.readbyqxmd.com/read/27683627/cryptosporidium-infection-in-solid-organ-transplantation
#17
REVIEW
Diana F Florescu, Uriel Sandkovsky
Diarrhea is a common complication in solid organ transplant (SOT) recipients and may be attributed to immunosuppressive drugs or infectious organisms such as bacteria, viruses or parasites. Cryptosporidium usually causes self-limited diarrhea in immunocompetent hosts. Although it is estimated that cryptosporidium is involved in about 12% of cases of infectious diarrhea in developing countries and causes approximately 748000 cases each year in the United States, it is still an under recognized and important cause of infectious diarrhea in SOT recipients...
September 24, 2016: World Journal of Transplantation
https://www.readbyqxmd.com/read/27681791/antiparasitic-drugs-proteasome-inhibition-combats-kinetoplastid-infections
#18
Sarah Crunkhorn
No abstract text is available yet for this article.
September 29, 2016: Nature Reviews. Drug Discovery
https://www.readbyqxmd.com/read/27667552/conjugation-of-n-acylhydrazone-and-1-2-4-oxadiazole-leads-to-the-identification-of-active-antimalarial-agents
#19
José Maurício Dos Santos Filho, Diogo Manoel Alves de Queiroz E Silva, Taís Soares Macedo, Helena Mariana Pitangueira Teixeira, Diogo Rodrigo Magalhaes Moreira, Soura Challal, Jean-Luc Wolfender, Emerson Ferreira Queiroz, Milena Botelho Pereira Soares
Malaria, caused by several Plasmodium species, is the major life-threatening parasitic infection worldwide. Due to the parasite resistance to quinoline based drugs, the search for antimalarial agents is necessary. Here, we report the structural design, synthesis and antiparasitic evaluation of two novel series of 1,2,4-oxadiazoles in conjugation to N-acylhydrazones, both groups recognized as privileged structures, as well as the studies on the antimalarial activity of 16 previous described analogues. By varying substituents attached to the phenyl ring, it was possible to retain, enhance or increase the antiparasitic activity in comparison to the nonsubstituted derivatives...
September 9, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27649642/a-green-alternative-method-for-analysis-of-ivermectin-and-moxidectin-in-environmental-water-samples-using-automatized-preconcentration-previous-meekc
#20
Emiliano Felici, Cristian Casado, Chien C Wang, Julio Raba, María R Gomez
Antiparasitic drugs derived from macrocyclic lactones (MLs) are widely used in livestock activities around the world. An increasing concern for local authorities is the environmental pollution as a consequence of veterinary drugs widely used in rural areas. The purpose of environmental analysis is to monitor low levels of pollutant analytes in a large number of samples. Also, due to the lipophilic characteristic of these lactones, long-chain solvents are usually required for performing sample treatment before and during the analysis...
November 2016: Electrophoresis
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