keyword
MENU ▼
Read by QxMD icon Read
search

Antiparasitic drugs

keyword
https://www.readbyqxmd.com/read/29031078/structural-design-synthesis-and-pharmacological-evaluation-of-thiazoles-against-trypanosoma-cruzi
#1
Gevanio Bezerra de Oliveira Filho, Marcos Veríssimo de Oliveira Cardoso, José Wanderlan Pontes Espíndola, Dayane Albuquerque Oliveira E Silva, Rafaela Salgado Ferreira, Pollyanne Lacerda Coelho, Pâmela Silva Dos Anjos, Emanuelle de Souza Santos, Cássio Santana Meira, Diogo Rodrigo Magalhaes Moreira, Milena Botelho Pereira Soares, Ana Cristina Lima Leite
Chagas disease is one of the most significant health problems in the American continent. benznidazole (BDZ) and nifurtimox (NFX) are the only drugs approved for treatment and exhibit strong side effects and ineffectiveness in the chronic stage, besides different susceptibility among T. cruzi DTUs (Discrete Typing Units). Therefore, new drugs to treat this disease are necessary. Thiazole compounds have been described as potent trypanocidal agents. Here we report the structural planning, synthesis and anti-T...
September 22, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29016295/ignoring-the-itch-the-global-health-problem-of-scabies
#2
Lola V Stamm, Lindsay C Strowd
Infestation with Sarcoptes scabiei var. hominis is a common human parasitic affliction endemic in tropical developing countries. Scabies is transmitted by close person-person contact, and outbreaks have been reported in reception centers for asylum seekers. Scabies presents clinically as extremely pruritic excoriated papules and linear burrows in the skin. This infestation predisposes to bacterial skin infections that can result in serious complications affecting the kidneys and possibly the heart. Treatment of individuals with scabies and their close contacts involves the use of antiparasitic agents...
October 2, 2017: American Journal of Tropical Medicine and Hygiene
https://www.readbyqxmd.com/read/28986531/experimental-testing-of-reciprocal-effects-of-nutrition-and-parasitism-in-wild-black-capuchin-monkeys
#3
Ilaria Agostini, Ezequiel Vanderhoeven, Mario S Di Bitetti, Pablo M Beldomenico
Nutritional stress may predispose individuals to infection, which in turn can have further detrimental effects on physical condition, thus creating an opportunity for reciprocal effects between nutrition and parasitism. Little experimental investigation has been conducted on this "vicious circle" hypothesis in wild animals, especially under natural conditions. We evaluated the reciprocal effects of nutritional status and parasitism using an experimental approach in two groups of wild black capuchin monkeys (Sapajus nigritus)...
October 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28983525/exploiting-the-2-amino-1-3-4-thiadiazole-scaffold-to-inhibit-trypanosoma-brucei-pteridine-reductase-in-support-of-early-stage-drug-discovery
#4
Pasquale Linciano, Alice Dawson, Ina Pöhner, David M Costa, Monica S Sá, Anabela Cordeiro-da-Silva, Rosaria Luciani, Sheraz Gul, Gesa Witt, Bernhard Ellinger, Maria Kuzikov, Philip Gribbon, Jeanette Reinshagen, Markus Wolf, Birte Behrens, Véronique Hannaert, Paul A M Michels, Erika Nerini, Cecilia Pozzi, Flavio di Pisa, Giacomo Landi, Nuno Santarem, Stefania Ferrari, Puneet Saxena, Sandra Lazzari, Giuseppe Cannazza, Lucio H Freitas-Junior, Carolina B Moraes, Bruno S Pascoalino, Laura M Alcântara, Claudia P Bertolacini, Vanessa Fontana, Ulrike Wittig, Wolfgang Müller, Rebecca C Wade, William N Hunter, Stefano Mangani, Luca Costantino, Maria P Costi
Pteridine reductase-1 (PTR1) is a promising drug target for the treatment of trypanosomiasis. We investigated the potential of a previously identified class of thiadiazole inhibitors of Leishmania major PTR1 for activity against Trypanosoma brucei (Tb). We solved crystal structures of several TbPTR1-inhibitor complexes to guide the structure-based design of new thiadiazole derivatives. Subsequent synthesis and enzyme- and cell-based assays confirm new, mid-micromolar inhibitors of TbPTR1 with low toxicity. In particular, compound 4m, a biphenyl-thiadiazole-2,5-diamine with IC50 = 16 μM, was able to potentiate the antitrypanosomal activity of the dihydrofolate reductase inhibitor methotrexate (MTX) with a 4...
September 30, 2017: ACS Omega
https://www.readbyqxmd.com/read/28983415/bilharzial-arthropathy-rare-cause-of-chronic-arthritis-in-tropical-areas
#5
Hoby N Rakotomalala, Maminirina V Ranaivoarison, Francia Andrianjafison, Dimby S Ralandison
Bilharziasis is a parasitic disease that affects the urinary tract and intestines. Finding bilharzia in joints is exceptional. We report two cases of Malagasy patients living in a highly endemic bilharziasis area and having chronic arthritis due to bilharziasis. The first case was a 32-year-old man presenting with a clinical picture of spondylitis with chronic oligoarthritis and paroxysmal asymmetric in his lower limbs, accompanied with sacroiliac pain and episodic dysentery. We retained the diagnosis of bilharziasis arthritis because of positive schistosomiasis serology in the joint fluid and the blood, poor response to therapy with nonsteroidal anti-inflammatory drugs (NSAIDs), and high efficacy of treatment with specific antiparasitic drugs...
September 2017: European Journal of Rheumatology
https://www.readbyqxmd.com/read/28979356/antiparasitic-activity-of-mirazid-myrrh-total-oil-and-nitazoxanide-compared-to-praziquantel-on-schistosoma-mansoni-scanning-electron-microscopic-study
#6
Mona El-Sayad, Sahar Abu Helw, Hend El-Taweel, Mohammad Aziz
BACKGROUND: The development of new antischistosomal drug remains a pressing need and a vital challenge in front of many researchers through screening the natural or chemical substances for their potential activity as antischistosomal agents. METHODS: Five groups of Schistosoma mansoni-infected mice (n=10) were enrolled in this study, the G1 was infected non-treated control group. G2 was infected treated with praziquantel 500 mg/kg for 2 consecutive days. G3 was given mirazid 500 mg/kg for 5 days...
July 2017: Iranian Journal of Parasitology
https://www.readbyqxmd.com/read/28973981/effect-of-moxidectin-on-bed-bug-feeding-development-fecundity-and-survivorship
#7
Chen Zha, Changlu Wang, Johnathan Michael Sheele
The common bed bug, Cimex lectularius L. (Hemiptera: Cimicidae), is a blood-feeding ectoparasite which experienced world-wide resurgence during recent decades. The control of bed bugs is often challenging, due to their cryptic nature and resistance to commonly used insecticides. In this study, we evaluated the effect of the antiparasitic drug moxidectin on bed bug survival, reproduction, and development. The LC50 (lethal concentration to kill half the members of a tested population) of moxidectin against bed bug male adults, female adults, and large nymphs were 52...
September 30, 2017: Insects
https://www.readbyqxmd.com/read/28954575/nanoformulations-of-albendazole-as-effective-anticancer-and-antiparasite-agents
#8
Fatemeh Movahedi, Li Li, Wenyi Gu, Zhi Ping Xu
Initially emerging as a widely used clinical antiparasitic drug, albendazole (ABZ) has been increasingly recognized as an effective anticancer agent due to its outstanding advantage, in other words, low toxicity to normal cells but high effectiveness against parasites and some tumors. The major challenge is its poor water solubility and subsequently low bioavailability. This article thus first reviews the brief achievements in using ABZ to treat parasites and cancers, and summarizes the basic mechanisms of action of ABZ...
September 28, 2017: Nanomedicine
https://www.readbyqxmd.com/read/28939506/impact-of-teflubenzuron-on-the-rockpool-shrimp-palaemon-elegans
#9
Pål A Olsvik, Bjørn T Lunestad, Ann-Lisbeth Agnalt, Ole B Samuelsen
Concerns have been raised over the environmental impacts of antiparasitic drugs used to delouse farmed salmon. Released into the marine environment, some of these drugs can have negative impact on non-targeted crustaceans in the vicinity of farming facilities. In this study, we examined the molecular effect of the insecticide teflubenzuron on a shrimp species inhabiting the littoral zone, the rockpool shrimp (Palaemon elegans). Rockpool shrimp was exposed for 98days to a dose representing 2% of a regular teflubenzuron medication applied to Atlantic salmon...
September 20, 2017: Comparative Biochemistry and Physiology. Toxicology & Pharmacology: CBP
https://www.readbyqxmd.com/read/28935948/novel-scaffolds-for-inhibition-of-cruzipain-identified-from-high-throughput-screening-of-anti-kinetoplastid-chemical-boxes
#10
Emir Salas-Sarduy, Lionel Urán Landaburu, Joel X Karpiak, Kevin P Madauss, Juan José Cazzulo, Fernán Agüero, Vanina Eder Alvarez
American Trypanosomiasis or Chagas disease is a prevalent, neglected and serious debilitating illness caused by the kinetoplastid protozoan parasite Trypanosoma cruzi. The current chemotherapy is limited only to nifurtimox and benznidazole, two drugs that have poor efficacy in the chronic phase and are rather toxic. In this scenario, more efficacious and safer drugs, preferentially acting through a different mechanism of action and directed against novel targets, are particularly welcome. Cruzipain, the main papain-like cysteine peptidase of T...
September 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28924201/discovery-semisynthesis-antiparasitic-and-cytotoxic-evaluation-of-14-membered-resorcylic-acid-lactones-and-their-derivatives
#11
Xue-Qing Zhang, Carmenza Spadafora, Laura M Pineda, Michelle G Ng, Ji-Hong Sun, Wei Wang, Chang-Yun Wang, Yu-Cheng Gu, Chang-Lun Shao
Ten antifouling 14-membered resorcylic acid lactones 1-10 were isolated previously with low or trace natural abundance from the zoanthid-derived Cochliobolus lunatus fungus. Further optimization of fermentation conditions led to the isolation of two major natural compounds 7 and 8 with multi-gram quantities. By one or two steps, we semisynthesized the six trace natural compounds 1-6 and a series of derivatives 11-27 of compounds 7 and 8 with high yields (65-95%). Compounds 11-13 showed strong antiplasmodial activity against Plasmodium falciparum with IC50 values of 1...
September 18, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28917450/a-novel-class-of-plasmodial-clpp-protease-inhibitors-as-potential-antimalarial-agents
#12
Sourabh Mundra, Vandana Thakur, Angelica M Bello, Sumit Rathore, Mohd Asad, Lianhu Wei, Jane Yang, Sai Kumar Chakka, Radhakrishnan Mahesh, Pawan Malhotra, Asif Mohmmed, Lakshmi P Kotra
The prokaryotic ATP-dependent ClpP protease, localized in the relict plastid of malaria parasite, represents a potential drug target. In the present study, we utilized in silico structure-based screening and medicinal chemistry approaches to identify a novel pyrimidine series of compounds inhibiting P. falciparum ClpP protease activity and evaluated their antiparasitic activities. Structure-activity relationship indicated that morpholine moiety at C2, an aromatic substitution at N3 and a 4-oxo moiety on the pyrimidine are important for potent inhibition of ClpP enzyme along with antiparasiticidal activity...
September 5, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28911671/albendazole-residues-in-goat-s-milk-interferences-in-microbial-inhibitor-tests-used-to-detect-antibiotics-in-milk
#13
Tamara Romero, Rafael Althaus, Vicente Javier Moya, María Del Carmen Beltrán, Wim Reybroeck, María Pilar Molina
Albendazole (ABZ) residues in goat's milk and their effect on the response of microbial inhibitor tests used for screening antibiotics were evaluated. A total of 18 Murciano-Granadina goats were treated with ABZ and individually milked once a day over a 7-day period. ABZ quantification was performed by high performance liquid chromatography. The ABZ parent drug was not detected. The maximum concentration of its metabolites (ABZ sulfoxide, ABZ sulfone, and ABZ 2-aminosulfone) was reached on the 1(st) day post treatment (260...
April 2017: Journal of Food and Drug Analysis
https://www.readbyqxmd.com/read/28910741/drug-susceptibility-testing-in-microaerophilic-parasites-cysteine-strongly-affects-the-effectivities-of-metronidazole-and-auranofin-a-novel-and-promising-antimicrobial
#14
David Leitsch
The microaerophilic parasites Entamoeba histolytica, Trichomonas vaginalis, and Giardia lamblia annually cause hundreds of millions of human infections which are treated with antiparasitic drugs. Metronidazole is the most often prescribed drug but also other drugs are in use, and novel drugs with improved characteristics are constantly being developed. One of these novel drugs is auranofin, originally an antirheumatic which has been relabelled for the treatment of parasitic infections. Drug effectivity is arguably the most important criterion for its applicability and is commonly assessed in susceptibility assays using in vitro cultures of a given pathogen...
September 5, 2017: International Journal for Parasitology, Drugs and Drug Resistance
https://www.readbyqxmd.com/read/28902434/biologically-active-quinoline-and-quinazoline-alkaloids-part-i
#15
REVIEW
Xiao-Fei Shang, Susan L Morris-Natschke, Ying-Qian Liu, Xiao Guo, Xiao-Shan Xu, Masuo Goto, Jun-Cai Li, Guan-Zhou Yang, Kuo-Hsiung Lee
Quinoline and quinazoline alkaloids, two important classes of N-based heterocyclic compounds, have attracted tremendous attention from researchers worldwide since the 19th century. Over the past 200 years, many compounds from these two classes were isolated from natural sources, and most of them and their modified analogs possess significant bioactivities. Quinine and camptothecin are two of the most famous and important quinoline alkaloids, and their discoveries opened new areas in antimalarial and anticancer drug development, respectively...
September 13, 2017: Medicinal Research Reviews
https://www.readbyqxmd.com/read/28881289/efficacy-of-a-series-of-alpha-pyrone-derivatives-against-leishmania-l-infantum-and-trypanosoma-cruzi
#16
Andre Gustavo Tempone, Daiane Dias Ferreira, Marta Lopes Lima, Thais Alves Costa Silva, Samanta E T Borborema, Juliana Quero Reimão, Mariana K Galuppo, Juliana Mariotti Guerra, Angelie J Russell, Graham M Wynne, Roy Y L Lai, Melissa M Cadelis, Brent R Copp
The neglected tropical diseases Chagas disease and leishmaniasis affect together more than 20 million people living mainly in developing countries. The mainstay of treatment is chemotherapy, however the drugs of choice, which include benznidazole and miltefosine, are toxic and have numerous side effects. Safe and effective therapies are urgently needed. Marine alpha-pyrones have been previously identified as scaffolds with potential antiprotozoan activities. In this work, using a phenotypic screen, twenty-seven examples of 3-substituted 4-hydroxy-6-methyl alpha-pyrones were synthesized and their antiparasitic efficacy evaluated against Leishmania (L...
October 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28876214/exposing-northern-shrimp-pandalus-borealis-to-fish-feed-containing-the-antiparasitic-drug-diflubenzuron-caused-high-mortality-during-molting
#17
Renée Katrin Bechmann, Emily Lyng, Mark Berry, Alfhild Kringstad, Stig Westerlund
Use of the chitin synthesis inhibitor diflubenzuron (DFB) as an antiparasitic drug in salmon aquaculture raises concern over its impact on marine ecosystems. Further, global drivers, such as ocean warming and acidification (OAW), may increase the toxicity of hazardous substances including DFB. The aim of the present study was to examine the combined effects of DFB-medicated salmon feed on ovigerous Northern shrimp (Pandalus borealis) under Control (pHNBS 8.0, 7.0ºC) and OAW conditions (pHNBS 7.6, 9.5ºC). DFB-exposed shrimp consumed on average 0...
September 6, 2017: Journal of Toxicology and Environmental Health. Part A
https://www.readbyqxmd.com/read/28869864/immunopegliposomes-for-the-targeted-delivery-of-novel-lipophilic-drugs-to-red-blood-cells-in-a-falciparum-malaria-murine-model
#18
Ernest Moles, Silvia Galiano, Ana Gomes, Miguel Quiliano, Cátia Teixeira, Ignacio Aldana, Paula Gomes, Xavier Fernàndez-Busquets
Most drugs currently entering the clinical pipeline for severe malaria therapeutics are of lipophilic nature, with a relatively poor solubility in plasma and large biodistribution volumes. Low amounts of these compounds do consequently accumulate in circulating Plasmodium-infected red blood cells, exhibiting limited antiparasitic activity. These drawbacks can in principle be satisfactorily dealt with by stably encapsulating drugs in targeted nanocarriers. Here this approach has been adapted for its use in immunocompetent mice infected by the Plasmodium yoelii 17XL lethal strain, selected as a model for human blood infections by Plasmodium falciparum...
August 15, 2017: Biomaterials
https://www.readbyqxmd.com/read/28868117/thiadiazoles-the-appropriate-pharmacological-scaffolds-with-leishmanicidal-and-antimalarial-activities-a-review
#19
REVIEW
Azar Tahghighi, Fateme Babalouei
Leishmaniasis and malaria are serious public health problems in tropical and sub-tropical regions worldwide. Development of drug-resistant strains has disrupted efforts to control the spread of these diseases in the world. The conventional antiparasitic chemotherapy still suffers from side effects and drug resistance. Therefore, the development of novel antimalarial and leishmanicidal drugs remains a critical topic to combat against these diseases. Five-membered heterocyclic systems have possessed antiparasitic activity such as thiadiazole scaffold which is a prevalent and an important heterocyclic ring...
June 2017: Iranian Journal of Basic Medical Sciences
https://www.readbyqxmd.com/read/28846817/the-usefulness-of-investigating-the-possible-underlying-conditions-in-rosacea
#20
G Ciccarese, A Parodi, A Rebora, F Drago
The paper entitled "Rosacea and demodicidosis with gain of function mutation in STAT1″ by Second et al.(1) is of indubitable interest and prompted us to make some observations. The Authors described a patient with cutaneous and ocular rosacea that they related to demodicidosis since oral ivermectin improved the cutaneous lesions(1) . However, the Authors did not demonstrate by skin scraping nor by standardized skin surface biopsy (SSSB) an excessive number of Demodex folliculorum (DF) mites in the pilosebaceous units to justify an oral antiparasitic treatment as a drug of first choice(1) ...
August 28, 2017: Journal of the European Academy of Dermatology and Venereology: JEADV
keyword
keyword
89731
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"