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Antiparasitic drugs

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https://www.readbyqxmd.com/read/28187957/discovery-of-n-2-aminoethyl-n-benzyloxyphenyl-benzamides-new-potent-trypanosoma-brucei-inhibitors
#1
Andriy Buchynskyy, J Robert Gillespie, Matthew A Hulverson, Joshua McQueen, Sharon A Creason, Ranae M Ranade, Nicole A Duster, Michael H Gelb, Frederick S Buckner
A phenotypic screen of a compound library for antiparasitic activity on Trypanosoma brucei, the causative agent of Human African Trypanosomiasis (HAT), led to the identification of N-(2-aminoethyl)-N-phenyl benzamides as a starting point for hit-to-lead medicinal chemistry. Eighty two analogues were prepared, which led to the identification of a set of highly potent N-(2-aminoethyl)-N-benzyloxyphenyl benzamides with the most potent compound 73 having an in vitro EC50=0.001μM. The compounds displayed drug-like properties when tested in a number of in vitro assays...
November 12, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28167514/pediatric-exposures-to-veterinary-pharmaceuticals
#2
Suzanne Tomasi, Kristin J Roberts, Jason Stull, Henry A Spiller, Lara B McKenzie
OBJECTIVE: To describe the epidemiology of veterinary pharmaceutical-related exposures to children based on calls to a regional poison control center. METHODS: A retrospective analysis of pediatric (≤19 years of age) exposures to pharmaceutical products intended for animal use, managed by a regional poison control center from 1999 through 2013, was conducted. Case narratives were reviewed and coded for exposure-related circumstances and intended species. Descriptive statistics were generated...
February 6, 2017: Pediatrics
https://www.readbyqxmd.com/read/28166232/repositioning-approved-drugs-for-the-treatment-of-problematic-cancers-using-a-screening-approach
#3
Hristo P Varbanov, Fabien Kuttler, Damiano Banfi, Gerardo Turcatti, Paul J Dyson
Advances in treatment strategies together with an earlier diagnosis have considerably increased the average survival of cancer patients over the last four decades. Nevertheless, despite the growing number of new antineoplastic agents introduced each year, there is still no adequate therapy for problematic malignancies such as pancreatic, lung and stomach cancers. Consequently, it is important to ensure that existing drugs used to treat other types of cancers, and potentially other diseases, are not overlooked when searching for new chemotherapy regimens for these problematic cancer types...
2017: PloS One
https://www.readbyqxmd.com/read/28158900/biochemical-proximates-of-pumpkin-cucurbitaeae-spp-and-their-beneficial-effects-on-the-general-well-being-of-poultry-species
#4
REVIEW
M C Achilonu, I C Nwafor, D O Umesiobi, M M Sedibe
There is a growing need to increase productivity in poultry. Growth hormones and antibiotics have the ability to improve health, weight gain and feed efficiency in meat-producing animals. The growth-promoting antibiotics are administered to poultry to improve the general performance of the chicken. However, the use of the xenobiotic drugs in food-producing animals has been a concern and a sensitive issue of debate for several decades in the EU and many other regional blocks of the world. Consequently, the use of hormones in animal production has been banned in Italy, Denmark and Germany for over 4-5 decades, while Belgium and Greece had never permitted its use for livestock fattening purposes...
February 3, 2017: Journal of Animal Physiology and Animal Nutrition
https://www.readbyqxmd.com/read/28154849/organometallic-gold-iii-complexes-with-hybrid-sns-donating-thiosemicarbazone-ligands-cytotoxicity-and-anti-trypanosoma-cruzi-activity
#5
P I da S Maia, Z A Carneiro, C D Lopes, C G Oliveira, J S Silva, S de Albuquerque, A Hagenbach, R Gust, V M Deflon, U Abram
Stable organogold(iii) compounds of the composition [Au(III)(Hdamp)(L1)]Cl are formed from reactions of [AuCl2(damp)] with H2L1 (damp(-) = dimethylaminomethylphenyl; H2L1 = N'-(diethylcarbamothioyl)benzimidothiosemicarbazides). The cationic complexes can be neutralized by reactions with weak bases under the formation of [Au(III)(damp)(L1)] compounds. The structures of the products show interesting features like relatively short AuH contacts between the methylene protons of the Hdamp ligand and the gold(iii) ions...
February 3, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28139658/sc83288-is-a-clinical-development-candidate-for-the-treatment-of-severe-malaria
#6
Stefano Pegoraro, Maëlle Duffey, Thomas D Otto, Yulin Wang, Roman Rösemann, Roland Baumgartner, Stefanie K Fehler, Leonardo Lucantoni, Vicky M Avery, Alicia Moreno-Sabater, Dominique Mazier, Henri J Vial, Stefan Strobl, Cecilia P Sanchez, Michael Lanzer
Severe malaria is a life-threatening complication of an infection with the protozoan parasite Plasmodium falciparum, which requires immediate treatment. Safety and efficacy concerns with currently used drugs accentuate the need for new chemotherapeutic options against severe malaria. Here we describe a medicinal chemistry program starting from amicarbalide that led to two compounds with optimized pharmacological and antiparasitic properties. SC81458 and the clinical development candidate, SC83288, are fast-acting compounds that can cure a P...
January 31, 2017: Nature Communications
https://www.readbyqxmd.com/read/28131660/light-and-scanning-electron-microscopy-study-of-in%C3%A2-vitro-effects-of-artesunate-in-newly-excysted-metacercariae-of-echinostoma-paraensei-trematoda-digenea
#7
Joyce G R Souza, Eduardo J Lopes Torres, Juberlan S Garcia, Ana Paula N Gomes, Rosangela Rodrigues-Silva, Arnaldo Maldonado, José Roberto Machado-Silva
Chemotherapy of food-borne trematodes relies on two drugs, praziquantel and tricabendazole, and there is growing interest in finding alternative therapies. Plant oil extracts have long been used in traditional Chinese medicine as sources of bioactive compounds with antiparasitic activity. Species of the genus Echinostoma are used as good models to test effective compounds against food-borne trematodes. This study evaluated the anthelmintic activity of crude artesunate extracts in vitro on newly excysted metacercariae of Echinostoma paraensei by light and scanning electron microscopy (SEM)...
January 25, 2017: Experimental Parasitology
https://www.readbyqxmd.com/read/28119024/antiparasitic-lethality-of-sulfonamidebenzamides-in-kinetoplastids
#8
Amber Hackler, Stephen L Patrick, Elizabeth W Kahney, Daniel P Flaherty, Elizabeth R Sharlow, James C Morris, Jennifer E Golden
A sulfonamidebenzamide series was assessed for anti-kinetoplastid parasite activity based on structural similarity to the antiparasitic drug, nifurtimox. Through structure-activity optimization, derivatives with limited mammalian cell toxicity and increased potency toward African trypanosomes and Leishmania promastigotes were developed. Compound 22 had the best potency against the trypanosome (EC50=0.010μM) while several compounds showed ∼10-fold less potency against Leishmania promastigotes without impacting mammalian cells (EC50>25μM)...
February 15, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28077462/bromodomains-in-protozoan-parasites-evolution-function-and-opportunities-for-drug-development
#9
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
#10
Yanis Toledano-Magaña, Juan C García-Ramos, Carolina Torres-Gutiérrez, Cristina Vázquez-Gasser, José M Esquivel-Sánchez, Marcos Flores-Alamo, Luis Ortiz-Frade, Rodrigo Galindo-Murillo, Mario Nequiz, Marco Gudiño-Zayas, Juan P Laclette, Julio C Carrero, Lena Ruiz-Azuara
Three 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 = 2,2'-[1,2-ethanediylbis-(sulfanediyl-2,1-ethanediyl)]dipyridine, en = ethylendiamine, gly = glycinate, and acac = acetylacetonate, have been synthezised and fully characterized. The crystal structures of compounds 1-3 are described. The IC50 values for compounds 1-3 are within nanomolar range (14, 12, and 6 nM, respectively). The cytotoxicity for human peripheral blood lymphocytes is extremely low (>100 μM)...
February 9, 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
#11
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
#12
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...
March 2017: Acta Tropica
https://www.readbyqxmd.com/read/28017125/review-of-theoretical-models-to-study-natural-products-with-antiprotozoal-activity
#13
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
#14
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...
January 2017: Experimental Parasitology
https://www.readbyqxmd.com/read/28010902/evaluating-the-effect-of-synchronized-sea-lice-treatments-in-chile
#15
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
#16
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
#17
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
#18
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
#19
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...
February 2017: 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
#20
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
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