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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/28139658/sc83288-is-a-clinical-development-candidate-for-the-treatment-of-severe-malaria
#3
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/28075589/water-soluble-ruthenium-ii-chiral-heteroleptic-complexes-with-amoebicidal-in-vitro-and-in-vivo-activity
#4
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
#5
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
#6
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/27979695/potential-of-marine-natural-products-against-drug-resistant-fungal-viral-and-parasitic-infections
#7
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
#8
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/27865740/sm-p80-based-schistosomiasis-vaccine-preparation-for-human-clinical-trials
#9
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/27719626/metabolic-inhibitors-as-antiparasitic-drugs-pharmacological-biochemical-and-molecular-perspectives
#10
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/27519462/discovery-and-antiparasitic-activity-of-az960-as-a-trypanosoma-brucei-erk8-inhibitor
#11
Ana L Valenciano, Aaron C Ramsey, Webster L Santos, Zachary B Mackey
Human African trypanosomiasis (HAT) is a lethal, vector-borne disease caused by the parasite Trypanosoma brucei. Therapeutic strategies for this neglected tropical disease suffer from disadvantages such as toxicity, high cost, and emerging resistance. Therefore, new drugs with novel modes of action are needed. We screened cultured T. brucei against a focused kinase inhibitor library to identify promising bioactive compounds. Among the ten hits identified from the phenotypic screen, AZ960 emerged as the most promising compound with potent antiparasitic activity (IC50=120nM) and was shown to be a selective inhibitor of an essential gene product, T...
October 1, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27431220/cryptosporidium-and-toxoplasma-parasites-are-inhibited-by-a-benzoxaborole-targeting-leucyl-trna-synthetase
#12
Andrés Palencia, Ru-Juan Liu, Maria Lukarska, Jiri Gut, Alexandre Bougdour, Bastien Touquet, En-Duo Wang, Xianfeng Li, M R K Alley, Yvonne R Freund, Philip J Rosenthal, Mohamed-Ali Hakimi, Stephen Cusack
The apicomplexan parasites Cryptosporidium and Toxoplasma are serious threats to human health. Cryptosporidiosis is a severe diarrheal disease in malnourished children and immunocompromised individuals, with the only FDA-approved drug treatment currently being nitazoxanide. The existing therapies for toxoplasmosis, an important pathology in immunocompromised individuals and pregnant women, also have serious limitations. With the aim of developing alternative therapeutic options to address these health problems, we tested a number of benzoxaboroles, boron-containing compounds shown to be active against various infectious agents, for inhibition of the growth of Cryptosporidium parasites in mammalian cells...
October 2016: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/27297108/pentamidine-blocks-the-interaction-between-mutant-s100a5-and-rage-v-domain-and-inhibits-the-rage-signaling-pathway
#13
Ching Chang Cho, Ruey Hwang Chou, Chin Yu
The human S100 protein family contains small, dimeric and acidic proteins that contain two EF-hand motifs and bind calcium. When S100A5 binds calcium, its conformation changes and promotes interaction with the target protein. The extracellular domain of RAGE (Receptor of Advanced Glycation End products) contain three domains: C1, C2 and V. The RAGE V domain is the target protein of S100A5 that promotes cell survival, growth and differentiation by activating several signaling pathways. Pentamidine is an apoptotic and antiparasitic drug that is used to treat or prevent pneumonia...
August 19, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27236016/nitroimidazole-carboxamides-as-antiparasitic-agents-targeting-giardia-lamblia-entamoeba-histolytica-and-trichomonas-vaginalis
#14
A M Jarrad, A Debnath, Y Miyamoto, K A Hansford, R Pelingon, M S Butler, T Bains, T Karoli, M A T Blaskovich, L Eckmann, M A Cooper
Diarrhoeal diseases caused by the intestinal parasites Giardia lamblia and Entamoeba histolytica constitute a major global health burden. Nitroimidazoles are first-line drugs for the treatment of giardiasis and amebiasis, with metronidazole 1 being the most commonly used drug worldwide. However, treatment failures in giardiasis occur in up to 20% of cases and development of resistance to metronidazole is of concern. We have re-examined 'old' nitroimidazoles as a foundation for the systematic development of next-generation derivatives...
September 14, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27139509/plant-extracts-from-encapsulation-to-application
#15
Brenda Armendáriz-Barragán, Nadiah Zafar, Waisudin Badri, Sergio Arturo Galindo-Rodríguez, Dounia Kabbaj, Hatem Fessi, Abdelhamid Elaissari
INTRODUCTION: Plants are a natural source of various products with diverse biological activities offering treatment for several diseases. Plant extract is a complex mixture of compounds, which can have antioxidant, antibiotic, antiviral, anticancer, antiparasitic, antifungal, hypoglycemic, anti-hypertensive and insecticide properties. The extraction of these extracts requires the use of organic solvents, which not only complicates the formulations but also makes it difficult to directly use the extracts for humans...
August 2016: Expert Opinion on Drug Delivery
https://www.readbyqxmd.com/read/27118499/antimicrobial-antiparasitic-and-anticancer-properties-of-hibiscus-sabdariffa-l-and-its-phytochemicals-in-vitro-and-in-vivo-studies
#16
Sherif T S Hassan, Kateřina Berchová, Miroslava Šudomová
UNLABELLED: In the last few decades, Hibiscus sabdariffa L. (Malvaceae; H. sabdariffa) has gained much attention in research field because of its potentially useful bioactivity as well as a great safety and tolerability. For decades, microbial, parasitic and cancer diseases remain a serious threat to human health and animals as well. To treat such diseases, a search for new sources such as plants that provide various bioactive compounds useful in the treatment of several physiological conditions is urgently needed, since most of the drugs currently used in the therapy have several undesirable side effects, toxicity, and drug resistance...
2016: Ceská a Slovenská Farmacie
https://www.readbyqxmd.com/read/27090120/toxicity-and-potential-utility-of-ivermectin-and-moxidectin-as-xenointoxicants-against-the-common-bed-bug-cimex-lectularius-l
#17
Johnathan M Sheele, Gale E Ridge
The recent resurgence of the common bed bug Cimex lectularius L. throughout western industrialized nations has been facilitated in part by the insect becoming pesticide-resistant. Novel control strategies, including xenointoxication, should be considered to combat C. lectularius. Ivermectin, a U.S. Food and Drug Administration (FDA)-approved treatment for several human parasites, and the antiparasitic drug moxidectin, currently being explored in human clinical trials, were evaluated for efficacy against C. lectularius...
August 2016: Parasitology Research
https://www.readbyqxmd.com/read/27070627/in-vitro-effect-of-the-synthetic-cal14-1a-conotoxin-derived-from-conus-californicus-on-the-human-parasite-toxoplasma-gondii
#18
Marco A De León-Nava, Eunice Romero-Núñez, Angélica Luna-Nophal, Johanna Bernáldez-Sarabia, Liliana N Sánchez-Campos, Alexei F Licea-Navarro, Jorge Morales-Montor, Saé Muñiz-Hernández
Toxins that are secreted by cone snails are small peptides that are used to treat several diseases. However, their effects on parasites with human and veterinary significance are unknown. Toxoplasma gondii is an opportunistic parasite that affects approximately 30% of the world's population and can be lethal in immunologically compromised individuals. The conventional treatment for this parasitic infection has remained the same since the 1950s, and its efficacy is limited to the acute phase of infection. These findings have necessitated the search for new drugs that specifically target T...
April 8, 2016: Marine Drugs
https://www.readbyqxmd.com/read/27045536/closantel-suppresses-angiogenesis-and-cancer-growth-in-zebrafish-models
#19
Xiao-Yu Zhu, Bo Xia, Hong-Cui Liu, Yi-Qiao Xu, Chang-Jiang Huang, Ji-Min Gao, Qiao-Xiang Dong, Chun-Qi Li
Angiogenesis has emerged as an important therapeutic target in several major diseases, including cancer and age-related macular degeneration. The zebrafish offer the potential for high-throughput drug discovery in a whole vertebrate system. In this study, we have taken advantage of the transgenic Tg (fli1a:EGFP) zebrafish line to screen the U.S. Drug Collection Library and identified 11 old drugs with antiangiogenic activity, including Closantel, an FDA-approved broad-spectrum salicylanilide antiparasitic drug for a variety of types of animals...
April 5, 2016: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/27003405/evaluation-of-medicated-feeds-with-antiparasitical-and-immune-enhanced-chinese-herbal-medicines-against-ichthyophthirius-multifiliis-in-grass-carp-ctenopharyngodon-idellus
#20
De-Jie Lin, Ya-Nan Hua, Qi-Zhong Zhang, De-Hai Xu, Yao-Wu Fu, Yan-Meng Liu, Sheng-Yu Zhou
Since malachite green was banned for using in food fish due to its carcinogenic and teratogenic effects on human, the search of alternative drug to treat Ichthyophthirius multifiliis becomes urgent. This study aimed to (1) evaluate the ethanol extracts of medicinal plants Cynanchum atratum, Zingiber officinale, Cynanchum paniculatum, immunostimulant (A), and immunostimulant (B) for their efficacy against I. multifiliis, and (2) determine effects of medicated feeds with C. atratum, Z. officinale, C. paniculatum, and immunostimulant (A) to treat I...
June 2016: Parasitology Research
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