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Antiparasitic drugs

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https://www.readbyqxmd.com/read/29908440/organometallic-compounds-in-the-discovery-of-new-agents-against-kinetoplastid-caused-diseases
#1
REVIEW
Mauro Ravera, Elsa Moreno-Viguri, Rocio Paucar, Silvia Pérez-Silanes, Elisabetta Gabano
The development of safe and affordable antiparasitic agents effective against neglected tropical diseases is a big challenge of the drug discovery. The drugs currently employed have limitations such as poor efficacy, drug resistance or side effects. Thus, the search for new promising drugs is more and more crucial. Metal complexes and, in particular, organometallic compounds may expand the list of the drug candidates due to the peculiar attributes that the presence of the metal core add to the organic fragment (e...
June 1, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29887026/efficacy-of-afoxolaner-in-the-treatment-of-otodectic-mange-in-naturally-infested-cats
#2
Marília Alves Machado, Diefrey Ribeiro Campos, Natália Lôres Lopes, Isabela Pessôa Barbieri Bastos, Cristiane Bazaga Botelho, Thais Ribeiro Correia, Fábio Barbour Scott, Julio Israel Fernandes
Afoxolaner is a drug belonging to the isoxazolines' family, and it is recommended for ectoparasite control in dogs. The objective of this study was to evaluate the efficacy of afoxolaner in the treatment of otodectic mange in naturally infested cats. Sixteen cats were divided into two groups (treated and control). The treated group (n = 8) underwent a single oral presentation of afoxolaner at a dose of 2.5 mg/kg. The control group (n = 8) received no antiparasitic treatment. The detection of mite infestations were performed by video otoscopy before the medication, 48 h after the medication and at weekly intervals up to 35 days after treatment (+7, +14, +21, +28, +35)...
May 30, 2018: Veterinary Parasitology
https://www.readbyqxmd.com/read/29862213/synthesis-and-in-vitro-leishmanicidal-activities-of-six-quercetin-derivatives
#3
Maryam Mohajeri, Lotfollah Saghaei, Mustafa Ghanadian, Sedighe Saberi, Nader Pestechian, Ehsan Ostadhusseini
Background: Today, leishmaniasis is a widespread, infectious parasitic disease caused by Leishmania spp. Natural-derived compounds are likely to provide a valuable source of new pharmaceuticals, and among them, quercetin derivatives may have antileishmanial effects. The antileishmanial activity of 3,5,7,3',4'-pentahydroxyflavonol (quercetin) derivatives is partly attributed to the position and pKa of phenolic or catechol hydroxyl groups. Therefore, to optimize their leishmanicidal effect, the structural features of quercetin and its derivatives were improved by acylation or alkylation of hydroxyl groups and changing their pKa and consequently their activities...
2018: Advanced Biomedical Research
https://www.readbyqxmd.com/read/29846763/effects-of-the-antiparasitic-drug-moxidectin-in-cattle-dung-on-zooplankton-and-benthic-invertebrates-and-its-accumulation-in-a-water-sediment-system
#4
Leticia M Mesa, J Hörler, I Lindt, M F Gutiérrez, L Negro, G Mayora, L Montalto, M Ballent, A Lifschitz
Two anthelmintic macrocyclic lactones-ivermectin and moxidectin-have revolutionized parasite control in cattle. These drugs are only partly metabolized by livestock, and the main route of excretion is via feces. In seasonally inundated floodplains, cattle feces come into direct contact with surface water. Important differences in pharmacokinetics and pharmacodynamics between these drugs may bear on their ecotoxicology in aquatic ecosystems. Moxidectin strongly binds to organic matter and thereby may be consumed in aquatic food webs, but there is a scarcity of data on toxicity to freshwater invertebrates...
May 30, 2018: Archives of Environmental Contamination and Toxicology
https://www.readbyqxmd.com/read/29784074/effects-of-fenbendazole-impregnated-feed-and-topical-moxidectin-during-quarantine-on-the-gut-microbiota-of-c57bl-6-mice
#5
Scott W Korte, Craig L Franklin, Rebecca A Dorfmeyer, Aaron C Ericsson
To protect the biosecurity of research rodent colonies, research institutions frequently require a quarantine period for live animals transferred into their facilities. Quarantine practices often include antibiotic and antiparasitic treatment with drugs such as fenbendazole and macrolide lactones. The influence of these compounds on the resident gut microbiota of mice is unknown, and any effects might subsequently affect model reproducibility. To test the influence of standard quarantine procedures on the composition of the microbiota, C57BL/6 mice, purchased from 2 different commercial suppliers, were randomly assigned to treatment groups (n = 12) by vendor and treated with fenbendazole-supplemented feed, topical moxidectin, both treatments, or no treatment (control), according to our institution's standard treatment regimen and duration...
May 1, 2018: Journal of the American Association for Laboratory Animal Science: JAALAS
https://www.readbyqxmd.com/read/29784064/effects-of-eprinomectin-on-the-survival-reproduction-and-feeding-activity-of-the-dung-beetles-onthophagus-lenzii-harold-and-rare-species-copris-ochus-motschulsky-coleoptera-scarabaeidae
#6
I Ishikawa, M Iwasa
Effects of the antiparasitic drug eprinomectin were studied on the dung beetles, Onthophagus lenzii Harold and the rare species, Copris ochus Motschulsky by pour-on administrations (500 µg kg-1) in Japan. Eprinomectin was detected in cattle dung from 1 to 7 or 14 days after treatment, with a peak at 1 day after treatment in two experiments. In O. lenzii, adult survivals and numbers of brood balls constructed were significantly reduced in dung from eprinomectin-treated cattle at 1 and 3 days post-treatment in experiment 1, and adult emergence rates were extremely reduced in dung at 1, 3, and 7 days post-treatment...
May 22, 2018: Bulletin of Entomological Research
https://www.readbyqxmd.com/read/29774351/diversity-of-biologically-active-secondary-metabolites-from-endophytic-and-saprotrophic-fungi-of-the-ascomycete-order-xylariales
#7
REVIEW
Soleiman E Helaly, Benjarong Thongbai, Marc Stadler
Covering: up to December 2017The diversity of secondary metabolites in the fungal order Xylariales is reviewed with special emphasis on correlations between chemical diversity and biodiversity as inferred from recent taxonomic and phylogenetic studies. The Xylariales are arguably among the predominant fungal endophytes, which are the producer organisms of pharmaceutical lead compounds including the antimycotic sordarins and the antiparasitic nodulisporic acids, as well as the marketed drug, emodepside. Many Xylariales are "macromycetes", which form conspicuous fruiting bodies (stromata), and the metabolite profiles that are predominant in the stromata are often complementary to those encountered in corresponding mycelial cultures of a given species...
May 18, 2018: Natural Product Reports
https://www.readbyqxmd.com/read/29772747/involvement-of-cyp4f2-in-the-metabolism-of-a-novel-monophosphate-ester-prodrug-of-gemcitabine-and-its-interaction-potential-in-vitro
#8
Yedong Wang, Yuan Li, Jia Lu, Huixin Qi, Isabel Cheng, Hongjian Zhang
Compound- 3 is an oral monophosphate prodrug of gemcitabine. Previous data showed that Compound- 3 was more potent than gemcitabine and it was orally active in a tumor xenograft model. In the present study, the metabolism of Compound- 3 was investigated in several well-known in vitro matrices. While relatively stable in human and rat plasma, Compound- 3 demonstrated noticeable metabolism in liver and intestinal microsomes in the presence of NADPH and human hepatocytes. Compound- 3 could also be hydrolyzed by alkaline phosphatase, leading to gemcitabine formation...
May 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29762040/orally-bioavailable-and-effective-buparvaquone-lipid-based-nanomedicines-for-visceral-leishmaniasis
#9
Lindsay A Smith, Dolores Remedios Serrano, Marion Mauger, Francisco Bolás-Fernández, Maria Auxiliadora Dea-Ayuela, Aikaterini Lalatsa
Nano-enabled lipid based drug delivery systems offer a platform to overcome challenges encountered with current failed leads in the treatment of parasitic and infectious diseases. When prepared with FDA or EMA approved excipients, they can be readily translated without the need for further toxicological studies, while they remain affordable and amenable to scale-up. Buparvaquone (BPQ), a hydroxynapthoquinone with in vitro activity in the nanomolar range, failed to clinically translate as a viable treatment for visceral leishmaniasis due to its poor oral bioavailability limited by its poor aqueous solubility (BCS Class II drug)...
May 15, 2018: Molecular Pharmaceutics
https://www.readbyqxmd.com/read/29727200/tamoxifen-never-ceases-to-amaze-new-findings-on-non-estrogen-receptor-molecular-targets-and-mediated-effects
#10
Tatiana Anatolievna Bogush, Boris Borisovich Polezhaev, Ivan Andreevich Mamichev, Elena Alexandrovna Bogush, Boris Evseevich Polotsky, Sergei Alexeevich Tjulandin, Andrey Borisovich Ryabov
Tamoxifen is a first targeted drug that continues to be the gold standard in treatment of estrogen receptor positive breast cancer for almost 50 years. The current review is an update of the paper published in 2012. We provide the new data on the tamoxifen targets that are the key points of signaling cascades activating cellular proliferation, which determines aggressiveness of disease and chemotherapy resistance or sensitivity. Some inspiring clinical cases dealing with tamoxifen efficiency in treatment of different tumors are discussed...
May 4, 2018: Cancer Investigation
https://www.readbyqxmd.com/read/29716880/report-an-ex-vivo-up-take-of-levamisole-molecules-by-cestode-monezia-expensa-of-goat-capra-hirsa-and-its-detection-through-rp-hplc
#11
Muhammad Mazhar Ayaz, Muhammad Sajid, Sanjota Nirmal Das, Muhammad Hanif
Detection of various molecules of drugs remained a prime issue especially in tissues of animals, humans and in their target parasites. The cestode/tapeworms pose a dilemma because of their weird body composition and uptake pattern of nutrients and medicines especially through absorption by tegument. We selected levamisole; thought to be potent antiparasitic/ani-cestodal drug. The uptake of levamisole (LEV) through cestodeal tissues is studied through HPCL in this paper. High performance liquid chromatography technique has been utilized to know the uptake of levamisole in tissues of cestodes of Goat (Monezia expensa) in small ruminants...
May 2018: Pakistan Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/29701142/polyamines-and-related-nitrogen-compounds-in-the-chemotherapy-of-neglected-diseases-caused-by-kinetoplastids
#12
Juan A Bisceglia, Maria C Mollo, Nadia Gruber, Liliana R Orelli
Neglected diseases due to the parasitic protozoa Leishmania and Trypanosoma (kinetoplastids) affect millions of people worldwide, and the lack of suitable treatments has promoted an ongoing drug discovery effort to identify novel nontoxic and cost-effective chemotherapies. Polyamines are ubiquitous small organic molecules that play key roles in kinetoplastid parasites metabolism, redox homeostasis and in the normal progression of cell cycles, which differ from those found in the mammalian host. These features make polyamines attractive in terms of antiparasitic drug development...
April 27, 2018: Current Topics in Medicinal Chemistry
https://www.readbyqxmd.com/read/29686657/naphthoquinone-derivatives-as-scaffold-to-develop-new-drugs-for-tuberculosis-treatment
#13
Priscila C B Halicki, Laís A Ferreira, Kelly C G De Moura, Paula F Carneiro, Karina P Del Rio, Tatiane Dos S C Carvalho, Maria do C F R Pinto, Pedro E A da Silva, Daniela F Ramos
Despite being a curable disease, tuberculosis (TB) remains a public health problem worldwide mainly due to lengthy treatment, as well as its toxic effects, TB/HIV co-infection and the emergence of resistant Mycobacterium tuberculosis strains. These barriers reinforcing the need for development of new antimicrobial agents, that ideally should reduce the time of treatment and be active against susceptible and resistant strains. Quinones are compounds found in natural sources and among them, the naphthoquinones show antifungal, antiparasitic, and antimycobacterial activity...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29684665/anti-trypanosoma-cruzi-action-of-a-new-benzofuran-derivative-based-on-amiodarone-structure
#14
Andrea Pinto-Martinez, Vanessa Hernández-Rodríguez, Jessica Rodríguez-Durán, Elżbieta Hejchman, Gustavo Benaim
Chagas disease is a neglected tropical affection caused by the protozoan parasite Trypanosoma cruzi. There is no current effective treatment since the only two available drugs have a limited efficacy and produce side effects. Thus, investigation efforts have been directed to the identification of new drug leads. In this context, Ca2+ regulating mechanisms have been postulated as targets for antiparasitic compounds, since they present paramount differences when compared to host cells. Amiodarone is an antiarrhythmic with demonstrated trypanocidal activity acting through the disruption of the parasite intracellular Ca2+ homeostasis...
June 2018: Experimental Parasitology
https://www.readbyqxmd.com/read/29679042/effect-of-antimicrobial-peptides-from-galleria-mellonella-on-molecular-models-of-leishmania-membrane-thermotropic-and-fluorescence-anisotropy-study
#15
Isabel Andrea Patiño-Márquez, Marcela Manrique-Moreno, Edwin Patiño-González, Małgorzata Jemioła-Rzemińska, Kazimierz Strzałka
Antimicrobial peptides are molecules of natural origin, produced by organisms such as insects, which have focused attention as potential antiparasitic agents. They can cause the death of parasites such Leishmania by interacting with their membrane. In this study, additional information was obtained on how the anionic peptide 2 and cecropin D-like peptide derived from Galleria mellonella interact with liposomes that mimic the composition of the Leishmania membrane. In order to do this, lipid bilayers consisting of dipalmitoylphosphatidylcholine, dipalmitoylphosphatidylethanolamine, dimyristoylphosphatidylserine, and dimyristoylphosphatidylglycerol were constructed...
April 20, 2018: Journal of Antibiotics
https://www.readbyqxmd.com/read/29673959/a-200k-snp-chip-reveals-a-novel-pacific-salmon-louse-genotype-linked-to-differential-efficacy-of-emamectin-benzoate
#16
Amber M Messmer, Jong S Leong, Eric B Rondeau, Anita Mueller, Cody A Despins, David R Minkley, Matthew P Kent, Sigbjørn Lien, Brad Boyce, Diane Morrison, Mark D Fast, Joseph D Norman, Roy G Danzmann, Ben F Koop
Antiparasitic drugs such as emamectin benzoate (EMB) are relied upon to reduce the parasite load, particularly of the sea louse Lepeophtheirus salmonis, on farmed salmon. The decline in EMB treatment efficacy for this purpose is an important issue for salmon producers around the world, and particularly for those in the Atlantic Ocean where widespread EMB tolerance in sea lice is recognized as a significant problem. Salmon farms in the Northeast Pacific Ocean have not historically experienced the same issues with treatment efficacy, possibly due to the relatively large population of endemic salmonid hosts that serve to both redistribute surviving lice and dilute populations potentially under selection by introducing naïve lice to farms...
April 16, 2018: Marine Genomics
https://www.readbyqxmd.com/read/29672908/molecular-insights-into-trypanothione-reductase-inhibitor-interaction-a-structure-based-review
#17
REVIEW
Neha Tiwari, Neetu Tanwar, Manoj Munde
Information on how small molecules bind to the target enzyme has the potential to impact immensely on how medicinal chemists go about antiparasitic drug discovery. In this review, for the first time, we intend to make an assessment of the structural aspects of trypanothione reductase as drug target, and its complexes with several reversible drugs from the Protein Data Bank (PDB). We attempt to reveal the mechanism of these interactions by careful accounting of the X-ray structures and their possible roles in biological activity to treat Trypanosomatidae diseases...
June 2018: Archiv der Pharmazie
https://www.readbyqxmd.com/read/29655377/schistosomicidal-antifibrotic-and-antioxidant-effects-of-cucurbita-pepo-l-seed-oil-and-praziquantel-combined-treatment-for-schistosoma-mansoni-infection-in-a-mouse-model
#18
E V N Beshay, A A Rady, A F Afifi, A H Mohamed
Despite the seriousness of schistosomiasis, its treatment depends only on praziquantel (PZQ), which has begun to lose its efficacy against the emergent Schistosoma mansoni-resistant strains. Therefore, the discovery of a novel schistosomicidal drug is an urgent priority. This study was designed to evaluate treatment with Cucurbita pepo L. (pumpkin) seed oil (PSO) alone and combined with PZQ against S. mansoni in experimentally infected mice. The study involved five groups: GI was the normal control; GII was the infected control; GIII was treated with an oral dose of PZQ of 500 mg/kg/day for two successive days, starting in the sixth week post infection; GIV was treated with an oral dose of PSO of 50 mg/kg/day for four weeks, starting in the fourth week post infection; and GV was treated with combined PSO-PZQ...
April 15, 2018: Journal of Helminthology
https://www.readbyqxmd.com/read/29642881/antiplasmodial-and-trypanocidal-activity-of-violacein-and-deoxyviolacein-produced-from-synthetic-operons
#19
Elizabeth Bilsland, Tatyana A Tavella, Renata Krogh, Jamie E Stokes, Annabelle Roberts, James Ajioka, David R Spring, Adriano D Andricopulo, Fabio T M Costa, Stephen G Oliver
BACKGROUND: Violacein is a deep violet compound that is produced by a number of bacterial species. It is synthesized from tryptophan by a pathway that involves the sequential action of 5 different enzymes (encoded by genes vioA to vioE). Violacein has antibacterial, antiparasitic, and antiviral activities, and also has the potential of inducing apoptosis in certain cancer cells. RESULTS: Here, we describe the construction of a series of plasmids harboring the complete or partial violacein biosynthesis operon and their use to enable production of violacein and deoxyviolacein in E...
April 11, 2018: BMC Biotechnology
https://www.readbyqxmd.com/read/29642830/-a-new-strategy-for-enhancing-acanthamoebicidal-activity-with-synthesis-of-nanoflower-of-laurocerausus-officinalis-roemer-cherry-laurel-fruit-extracts
#20
Ayşe Baldemir, Ülkü Karaman, Sadi Yusufbeyoğlu, Ayşe Eken, Nilay Ildız, Selen İlgün, Cemil Çolak, Gamze Kaçmaz, İsmail Öçsoy, Soner Çankaya
Pathogenic Acanthamoeba species often cause infection known as Acanthamoeba keratitis among people who use contact lenses. It is a type of infection that can result in corneal ulceration, visual loss or even blindness, if not treated. There are various therapeutic options available in the treatment of Acanthamoeba infections but they are usually tough treatments with limited efficacy. For instance, hydrogen peroxide (H2 O2 ) is a commonly used contact lens disinfectant which is effective against Acanthamoeba but it is toxic to the cornea...
January 2018: Mikrobiyoloji Bülteni
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