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Antiparasitic drugs

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https://www.readbyqxmd.com/read/28077462/bromodomains-in-protozoan-parasites-evolution-function-and-opportunities-for-drug-development
#1
REVIEW
Victoria Jeffers, Chunlin Yang, Sherri Huang, William J Sullivan
Parasitic infections remain one of the most pressing global health concerns of our day, affecting billions of people and producing unsustainable economic burdens. The rise of drug-resistant parasites has created an urgent need to study their biology in hopes of uncovering new potential drug targets. It has been established that disrupting gene expression by interfering with lysine acetylation is detrimental to survival of apicomplexan (Toxoplasma gondii and Plasmodium spp.) and kinetoplastid (Leishmania spp...
March 2017: Microbiology and Molecular Biology Reviews: MMBR
https://www.readbyqxmd.com/read/28075589/water-soluble-ruthenium-ii-chiral-heteroleptic-complexes-with-amoebicidal-in-vitro-and-in-vivo-activity
#2
Yanis Toledano-Magaña, Juan Carlos García-Ramos, Carolina Torres-Gutiérrez, Cristina Vázquez-Gasser, José Manuel Esquivel-Sánchez, Marcos Flores-Alamo, Luis Ortiz-Frade, Rodrigo Galindo-Murillo, Mario Nequiz, Marco Gudiño-Zayas, Juan Pedro Laclette, Julio César Carrero, Lena Ruiz-Azuara
Three novel water soluble Ru(II) chiral heteroleptic coordination compounds [Ru(en)(pdto)]Cl2 (1), [Ru(gly)(pdto)]Cl (2) and [Ru(acac)(pdto)]Cl (3) where pdto= 1,8-bis-(2-pyridyl)-3,6-dithioctane, en= ethylendiamine, gly= glycinate and acac= acetylacetonate have been synthesised and have shown remarkable amoebicidal activity in vitro and in vivo. The crystal structures of compounds 1-3 are described. The in vitro IC50 values found are within nanomolar range (0.14, 0.12 and 0.06 µM for compounds 1, 2 and 3, respectively)...
January 11, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28018295/combined-whole-cell-high-throughput-functional-screening-for-identification-of-new-nicotinamidases-pyrazinamidases-in-metagenomic-polygenomic-libraries
#3
Rubén Zapata-Pérez, Antonio G García-Saura, Mohamed Jebbar, Peter N Golyshin, Álvaro Sánchez-Ferrer
Nicotinamidases catalyze the hydrolysis of the amide bond in nicotinamide (NAM) to produce ammonia and nicotinic acid (NA). These enzymes are an essential component of the NAD(+) salvage pathway and are implicated in the viability of several pathogenic organisms. Its absence in humans makes them a promising drug target. In addition, although they are key analytical biocatalysts for screening modulators in relevant biomedical enzymes, such as sirtuins and poly-ADP-ribosyltransferases, no commercial sources are available...
2016: Frontiers in Microbiology
https://www.readbyqxmd.com/read/28017859/antiparasitic-activity-of-menadione-vitamin-k3-against-schistosoma-mansoni-in-babl-c-mice
#4
Govind J Kapadia, Ingrid A O Soares, G Subba Rao, Fernanda R Badoco, Ricardo A Furtado, Mariana B Correa, Denise C Tavares, Wilson R Cunha, Lizandra G Magalhães
Schistosomiasis is one of the neglected tropical diseases affecting nearly quarter of a billion people in economically challenged tropical and subtropical countries of the world. Praziquantel (PZQ) is the only drug currently available to treat this parasitic disease in spite being ineffective against juvenile worms and concerns about developing resistance to treat reinfections. Our earlier in vitro viability studies demonstrated significant antiparasitic activity of menadione (MEN) (vitamin K3) against Schistosoma mansoni adult worms...
December 23, 2016: Acta Tropica
https://www.readbyqxmd.com/read/28017125/review-of-theoretical-models-to-study-natural-products-with-antiprotozoal-activity
#5
Miguel A Herrera-Rueda, Gabriel Navarrete-Vázquez, Francisco Aguirre-Crespo, María Guadalupe Maldonado-Velazquez, Jorge Vergara-Galicia, Hilario Chi Canul, Xerardo García-Mera, Francisco J Prado-Prado
There exists many pathogen parasite species with different susceptibility profiles of antiparasitic drugs. Unfortunately, almost QSAR models predict the biological activity of drugs against only one parasite species. Consequently, predicting the probability with which a drug is active against different species with a single unified model is a goal of major importance. In doing so, we use Markov Chains theory to calculate new multi-target spectral moments to fit a QSAR model that for the first time, can predicta meet-QSAR model for more than 40,000 cases obtained from databases CHEMBL against more than 35 proteins of 4 parasite species obtained from the Protein Data Bases (PDB)...
December 22, 2016: Current Drug Targets
https://www.readbyqxmd.com/read/28011170/antiprotozoal-drug-nitazoxanide-enhances-parasitemia-tissue-lesions-and-mortality-caused-by-trypanosoma-cruzi-in-murine-model
#6
Juan Salvador Valle-Reyes, Valery Melnikov, Oxana Dobrovinskaya, Alejandrina Rodriguez-Hernández, Cristina Wookee-Zea, Víctor Pimientel-Rodrigez, Gabriela Rueda-Valdovinos, Iván Delgado-Enciso, Uriel A López-Lemus, Francisco Espinoza-Gómez
Chagas' disease is caused by unicellular parasite Trypanosoma cruzi (T. cruzi). It is endemic throughout Latin America, but nowadays has become a global challenge due to tourism and migration. Non-treated infection may result in health-threatening complications and lead to death. Current medications for this infection are nifurtimox (NFT) and benznidazol. Both drugs may cause side effects and are ineffective in the chronic phase. Therefore, new antichagasic compounds are urgently required. Nitazoxanide (NTZ) is a broad spectrum antiparasitic drug, proposed recently as a potential candidate to be added to the list of essential medicines for integrated neglected tropical disease control and elimination...
December 21, 2016: Experimental Parasitology
https://www.readbyqxmd.com/read/28010902/evaluating-the-effect-of-synchronized-sea-lice-treatments-in-chile
#7
G Arriagada, H Stryhn, J Sanchez, R Vanderstichel, J L Campistó, E E Rees, R Ibarra, S St-Hilaire
The sea louse is considered an important ectoparasite that affects farmed salmonids around the world. Sea lice control relies heavily on pharmacological treatments in several salmon-producing countries, including Chile. Among options for drug administration, immersion treatments represent the majority of antiparasitic control strategies used in Chile. As a topical procedure, immersion treatments do not induce a long lasting effect; therefore, re-infestation from neighbouring farms may undermine their efficacy...
January 1, 2017: Preventive Veterinary Medicine
https://www.readbyqxmd.com/read/28008252/nanoscaled-hydrated-antimony-v-oxide-as-a-new-approach-to-first-line-antileishmanial-drugs
#8
Antonia Mr Franco, Iryna Grafova, Fabiane V Soares, Gennaro Gentile, Claudia Dc Wyrepkowski, Marcos A Bolson, Ézio Sargentini, Cosimo Carfagna, Markku Leskelä, Andriy Grafov
BACKGROUND: Coordination compounds of pentavalent antimony have been, and remain, the first-line drugs in leishmaniasis treatment for >70 years. Molecular forms of Sb (V) complexes are commercialized as sodium stibogluconate (Pentostam(®)) and meglumine antimoniate (MA) (Glucantime(®)). Ever-increasing drug resistance in the parasites limits the use of antimonials, due to the low drug concentrations being administered against high parasitic counts. Sb(5+) toxicity provokes severe side effects during treatment...
2016: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28002965/in-vitro-and-in-vivo-anti-trypanosoma-cruzi-activity-of-new-arylamine-mannich-base-type-derivatives
#9
Elsa Moreno-Viguri, Carmen Jiménez-Montes, Rubén Martín-Escolano, Mery Santivañez-Veliz, Alvaro Martin-Montes, Amaya Azqueta, Marina Jimenez-Lopez, Salvador Zamora Ledesma, Nuria Cirauqui, Adela López de Ceráin, Clotilde Marín, Manuel Sánchez-Moreno, Silvia Pérez-Silanes
Chagas disease is a neglected tropical disease with 6-7 million people infected worldwide, and there is no effective treatment. Therefore, there is an urgent need to continue researching in order to discover novel therapeutic alternatives. We present a series of arylaminoketone derivatives as means of identifying new drugs to treat Chagas disease in the acute phase with greater activity, less toxicity, and a larger spectrum of action than that corresponding to the reference drug benznidazole. Indexes of high selectivity found in vitro formed the basis for later in vivo assays in BALB/c mice...
December 22, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27994215/antimicrobial-activity-of-basil-oregano-and-thyme-essential-oils
#10
REVIEW
Hercules Sakkas, Chrissanthy Papadopoulou
For centuries plants have been used for a wide variety of purposes, from treating infectious diseases to food preservation and perfume production. Presently, the increasing resistance of microorganisms to currently used antimicrobials in combination with the appearance of emerging diseases requires urgently the development of new, more effective drugs. Plants, due to the large biological and structural diversity of their components, constitute a unique and renewable source for the discovery of new antibacterial, antifungal and antiparasitic treatments...
December 20, 2016: Journal of Microbiology and Biotechnology
https://www.readbyqxmd.com/read/27979695/potential-of-marine-natural-products-against-drug-resistant-fungal-viral-and-parasitic-infections
#11
REVIEW
Usama Ramadan Abdelmohsen, Srikkanth Balasubramanian, Tobias A Oelschlaeger, Tanja Grkovic, Ngoc B Pham, Ronald J Quinn, Ute Hentschel
Antibiotics have revolutionised medicine in many aspects, and their discovery is considered a turning point in human history. However, the most serious consequence of the use of antibiotics is the concomitant development of resistance against them. The marine environment has proven to be a very rich source of diverse natural products with significant antibacterial, antifungal, antiviral, antiparasitic, antitumour, anti-inflammatory, antioxidant, and immunomodulatory activities. Many marine natural products (MNPs)-for example, neoechinulin B-have been found to be promising drug candidates to alleviate the mortality and morbidity rates caused by drug-resistant infections, and several MNP-based anti-infectives have already entered phase 1, 2, and 3 clinical trials, with six approved for usage by the US Food and Drug Administration and one by the EU...
December 12, 2016: Lancet Infectious Diseases
https://www.readbyqxmd.com/read/27978783/in-silico-design-of-new-inhibitors-of-guanine-phosphoribosyltransferase-gprt-from-giardia-lamblia-as-antiparasitic-drug-candidates
#12
Gustavo Machado das Neves, Luciano Porto Kagami, Ricardo Pereira Rodrigues, Vinicius Barreto da Silva, Vera Lucia Eifler-Lima, Daniel Fábio Kawano
BACKGROUND: Guanine phosphoribosyltransferase (GPRT) is a very attractive target for the development of new drugs against G. lamblia because of its critical role in the syntheses of DNA and RNA. Herein we report the use of in silico approaches to identify potential G. lamblia GPRT inhibitors. METHODS: Analyses of the binding site of the enzyme accomplished through the use of several methods allowed the construction of a pharmacophore model, which was screened against a database of commercial substances...
December 13, 2016: Current Drug Discovery Technologies
https://www.readbyqxmd.com/read/27940092/crystal-structures-of-an-archaeal-thymidylate-kinase-from-sulfolobus-tokodaii-provide-insights-into-the-role-of-a-conserved-active-site-arginine-residue
#13
Ansuman Biswas, Arpit Shukla, R S K Vijayan, Jeyaraman Jeyakanthan, Kanagaraj Sekar
Thymidylate kinase (TMK) is a key enzyme that plays an important role in DNA synthesis. Therefore, it serves as an attractive therapeutic target for the development of antibacterial, antiparasitic and anticancer drugs. Herein, we report the biochemical characterization and crystal structure determination of thymidylate kinase from a hyperthermophilic organism Sulfolobus tokodaii (StTMK) in its apo and ADP-bound forms. Our study describes the first three-dimensional structure of an archaeal TMK. StTMK is a thermostable enzyme with optimum activity at 80°C...
December 9, 2016: Journal of Structural Biology
https://www.readbyqxmd.com/read/27928976/activity-of-two-extracts-of-cynanchum-paniculatum-against-ichthyophthirius-multifiliis-theronts-and-tomonts
#14
Wen Ji-Hong, Wang Yan-Li, Liu Yu-Hua, Zhang Ji-Yuan, L I Ze-Hong
The present study aims to evaluate the antiparasitic activity of active components from Cynanchum paniculatum against Ichthyophthirius multifiliis. The antiparasitic activities of two bioassay-guided fractionationated compounds from C. paniculatum identified as Cynatratoside-A and Cynanversicoside C, by comparing spectral data (NMR and ESI-MS) with literature values, were evaluated by in vitro assay. These showed that both could kill theronts of I. multifiliis at a concentration of 10·0 mg L-1, with the median effective concentration (EC50) values of 4·6 mg L-1 and 5·2 mg L-1 for Cynatratoside-A and Cynanversicoside C, respectively...
December 8, 2016: Parasitology
https://www.readbyqxmd.com/read/27914754/antiparasitic-and-disease-modifying-activity-of-nyctanthes-arbor-tristis-linn-in-malaria-an-exploratory-clinical-study
#15
Chhaya S Godse, Prakash S Tathed, Sameer S Talwalkar, Rama A Vaidya, Ashok J Amonkar, Akhil B Vaidya, Ashok D B Vaidya
BACKGROUND: An unceasing threat of drug resistance continuously poses demand for new antimalarial drugs. A scientific assessment of traditionally used antimalarial plants through reverse pharmacology is crucial for a fast track drug discovery. An Ayurvedic plant Nyctanthes arbor-tristis Linn. - (Parijat) is being used in clinical practice and had shown antimalarial activity, with a parasite clearance in 76.6% of 120 patients, in an earlier clinical study. OBJECTIVE: To further explore antimalarial potential of the plant through additional objective markers...
October 2016: Journal of Ayurveda and Integrative Medicine
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
#16
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
#17
Flavia Lambertucci, Omar Motiño, Silvina Villar, Juan Pablo Rigalli, María de Luján Alvarez, Viviana A 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 and 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 factor erytroide-derived 2-Like 2 (NRF2) in vitro...
November 27, 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
#18
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
#19
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
#20
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
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