keyword
MENU ▼
Read by QxMD icon Read
search

Antiparasitic drugs

keyword
https://www.readbyqxmd.com/read/28319176/insight-into-the-mechanism-of-action-of-temporin-sha-a-new-broad-spectrum-antiparasitic-and-antibacterial-agent
#1
Zahid Raja, Sonia André, Feten Abbassi, Vincent Humblot, Olivier Lequin, Tahar Bouceba, Isabelle Correia, Sandra Casale, Thierry Foulon, Denis Sereno, Bruno Oury, Ali Ladram
Antimicrobial peptides (AMPs) are promising drugs to kill resistant pathogens. In contrast to bacteria, protozoan parasites, such as Leishmania, were little studied. Therefore, the antiparasitic mechanism of AMPs is still unclear. In this study, we sought to get further insight into this mechanism by focusing our attention on temporin-SHa (SHa), a small broad-spectrum AMP previously shown to be active against Leishmania infantum. To improve activity, we designed analogs of SHa and compared the antibacterial and antiparasitic mechanisms...
2017: PloS One
https://www.readbyqxmd.com/read/28283781/gold-compounds-as-cysteine-protease-inhibitors-perspectives-for-pharmaceutical-application-as-antiparasitic-agents
#2
Lara Massai, Luigi Messori, Nicola Micale, Tanja Schirmeister, Louis Maes, Dolores Fregona, Maria Agostina Cinellu, Chiara Gabbiani
Gold compounds form a new class of promising metal-based drugs with a number of potential therapeutic applications, particularly in the fields of anticancer and antimicrobial treatments. Previous research revealed that a group of structurally diverse gold compounds cause conspicuous inhibition of the protease activities of the human proteasome. Given the pharmacological importance of protease inhibition, the present study further explored whether these gold compounds might inhibit a few other proteases that are accepted druggable targets for disease treatment...
March 10, 2017: Biometals: An International Journal on the Role of Metal Ions in Biology, Biochemistry, and Medicine
https://www.readbyqxmd.com/read/28282886/chroman-4-one-derivatives-targeting-pteridine-reductase-1-and-showing-anti-parasitic-activity
#3
Flavio Di Pisa, Giacomo Landi, Lucia Dello Iacono, Cecilia Pozzi, Chiara Borsari, Stefania Ferrari, Matteo Santucci, Nuno Santarem, Anabela Cordeiro-da-Silva, Carolina B Moraes, Laura M Alcantara, Vanessa Fontana, Lucio H Freitas-Junior, Sheraz Gul, Maria Kuzikov, Birte Behrens, Ina Pöhner, Rebecca C Wade, Maria Paola Costi, Stefano Mangani
Flavonoids have previously been identified as antiparasitic agents and pteridine reductase 1 (PTR1) inhibitors. Herein, we focus our attention on the chroman-4-one scaffold. Three chroman-4-one analogues (1-3) of previously published chromen-4-one derivatives were synthesized and biologically evaluated against parasitic enzymes (Trypanosoma brucei PTR1-TbPTR1 and Leishmania major-LmPTR1) and parasites (Trypanosoma brucei and Leishmania infantum). A crystal structure of TbPTR1 in complex with compound 1 and the first crystal structures of LmPTR1-flavanone complexes (compounds 1 and 3) were solved...
March 8, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28275906/molecular-modeling-and-infrared-and-raman-spectroscopy-of-the-crystal-structure-of-the-chiral-antiparasitic-drug-praziquantel
#4
Ana Borrego-Sánchez, Alfonso Hernández-Laguna, C Ignacio Sainz-Díaz
Anthelmintic praziquantel (PZQ) and its molecular and crystal lattice structures were studied by means of atomistic calculations based on empirical interatomic potentials and quantum mechanical methods (DFT). This chiral drug presents several crystal polymorphs due to the enantiomers (either R or S) or the racemic crystal, and different molecular conformations. The relative configurations of the carbonyl groups in PZQ define these conformations that produce different polymorphs. The polarity of these conformers is quite different and their relative population can vary in media with different polarity...
April 2017: Journal of Molecular Modeling
https://www.readbyqxmd.com/read/28274284/the-antimalarial-action-of-fk506-and-rapamycin-evidence-for-a-direct-effect-on-fk506-binding-protein-pffkbp35
#5
Paul Monaghan, Darren B Leneghan, Wesley Shaw, Angus Bell
FK506 and rapamycin (Rap) are immunosuppressive drugs that act principally on T-lymphocytes. The receptors for both drugs are FK506-binding proteins (FKBPs), but the molecular mechanisms of immunosuppression differ. An FK506-FKBP complex inhibits the protein phosphatase calcineurin, blocking a key step in T-cell activation, while the Rap -FKBP complex binds to the protein kinase target of rapamycin (TOR), which is involved in a subsequent signalling pathway. Both drugs, and certain non-immunosuppressive compounds related to FK506, have potent antimalarial activity...
March 9, 2017: Parasitology
https://www.readbyqxmd.com/read/28265521/genetic-and-structural-study-of-dna-directed-rna-polymerase-ii-of-trypanosoma-brucei-towards-the-designing-of-novel-antiparasitic-agents
#6
Louis Papageorgiou, Vasileios Megalooikonomou, Dimitrios Vlachakis
Trypanosoma brucei brucei (TBB) belongs to the unicellular parasitic protozoa organisms, specifically to the Trypanosoma genus of the Trypanosomatidae class. A variety of different vertebrate species can be infected by TBB, including humans and animals. Under particular conditions, the TBB can be hosted by wild and domestic animals; therefore, an important reservoir of infection always remains available to transmit through tsetse flies. Although the TBB parasite is one of the leading causes of death in the most underdeveloped countries, to date there is neither vaccination available nor any drug against TBB infection...
2017: PeerJ
https://www.readbyqxmd.com/read/28264505/antiprotozoal-activity-of-triazole-derivatives-of-dehydroabietic-acid-and-oleanolic-acid
#7
Mariano Walter Pertino, Celeste Vega, Miriam Rolón, Cathia Coronel, Antonieta Rojas de Arias, Guillermo Schmeda-Hirschmann
Tropical parasitic diseases such as Chagas disease and leishmaniasis are considered a major public health problem affecting hundreds of millions of people worldwide. As the drugs currently used to treat these diseases have several disadvantages and side effects, there is an urgent need for new drugs with better selectivity and less toxicity. Structural modifications of naturally occurring and synthetic compounds using click chemistry have enabled access to derivatives with promising antiparasitic activity. The antiprotozoal activity of the terpenes dehydroabietic acid, dehydroabietinol, oleanolic acid, and 34 synthetic derivatives were evaluated against epimastigote forms of Trypanosoma cruzi and promastigotes of Leishmaniabraziliensis and Leishmania infantum...
February 28, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28263719/mechanism-of-ascaridole-activation-in-leishmania
#8
Gerald Geroldinger, Matthias Tonner, Hubert Hettegger, Markus Bacher, Lianet Monzote, Martin Walter, Katrin Staniek, Thomas Rosenau, Lars Gille
Endoperoxides (EP) are an emerging class of drugs which have potential in antiparasitic therapy, but also in other fields. For malaria therapy the EP artemisinin (Art) and its derivatives are successfully used. We have shown in the past that the EP ascaridole (Asc) is useful for the treatment of cutaneous leishmaniasis in a mouse model. Biomimetic experiments suggested that these drugs need activation in the respective target pathogens to exert their function. In spite of this idea, direct activation of EP to radicals inside cells has never been demonstrated...
March 2, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28257952/in-vitro-immunomodulatory-effects-of-microemulsions-with-levamisole-delivery-systems-on-blood-phagocytes-interacting-with-giardia-lamblia
#9
Mara Rosa Gil Hernandes, Lucélia Campelo Albuquerque Moraes, Elton Brito Ribeiro, Danny Laura Gomes Fagundes, Adenilda Cristina Honorio-França, Eduardo Luzía França
BACKGROUND: Giardiasis is one of the main parasites that infect the gastrointestinal tract of humans, affecting hundreds of millions of people worldwide, particularly in developing countries. Antiparasitics administered to treat giardiasis are inefficient in 20% of the cases, usually because of parasite resistance and side effects. In this scenario, microemulsions are a promising pharmaceutical alternative as carriers of molecules with therapeutic action that stimulate the immune system...
February 28, 2017: Parasitology International
https://www.readbyqxmd.com/read/28245890/one-hundred-years-of-neglect-in-paediatric-schistosomiasis
#10
Amaya L Bustinduy, Stephen Wright, Elizabeth C Joekes, Narcis B Kabatereine, Jutta Reinhard-Rupp, Charles H King, J Russell Stothard
Early in the history of schistosomiasis research, children under 5 years of age were known to be infected. Although this problem was recognized over 100 years ago, insufficient action has been taken to address this issue. Under current policy, such infected children only receive their first antiparasitic treatment (praziquantel - PZQ) upon entry into primary school as current mass drug administration programmes typically target school-aged children. For many infected children, they will wait up to 6 years before receiving their first medication and significant schistosomiasis-related morbidity may have already established...
March 1, 2017: Parasitology
https://www.readbyqxmd.com/read/28245779/imidazole-an-essential-edifice-for-the-identification-of-new-lead-compounds-and-drug-development
#11
Nishtha Shalmali, Md Rahmat Ali, Sandhya Bawa
In recent years, a drastic rise has been observed in incidences of resistance, low efficacy rates and toxicities to various drugs used in therapeutic application. It has been observed that presence of imidazole nucleus in several categories of therapeutic agents such as antimicrobials, antivirals, antiparasites, anticancer, anti-inflammatory, antidiabetics etc. has made it a vital anchor for the development of new therapeutic agents. But, there is a need to couple the newest information with the already available knowledge to recognize the present standing of imidazole motif in medicinal chemistry research...
February 28, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28242550/desing-and-synthesis-of-potent-anti-trypanosoma-cruzi-agents-new-thiazoles-derivatives-which-induce-apoptotic-parasite-death
#12
Elany Barbosa da Silva, Dayane Albuquerque Oliveira E Silva, Arsênio Rodrigues Oliveira, Carlos Henrique da Silva Mendes, Thiago André Ramos Dos Santos, Aline Caroline da Silva, Maria Carolina Acioly de Castro, Rafaela Salgado Ferreira, Diogo Rodrigo Magalhães Moreira, Marcos Veríssimo de Oliveira Cardoso, Carlos Alberto de Simone, Valéria Rêgo Alves Pereira, Ana Cristina Lima Leite
Chagas disease, caused by the kinetoplastid protozoan parasite Trypanosoma cruzi, remains a relevant cause of illness and premature death and it is estimated that 6 million to 7 million people are infected worldwide. Although chemotherapy options are limited presenting serious problems, such as low efficacy and high toxicity. T. cruzi is susceptible to thiazoles, making this class of compounds appealing for drug development. Previously, thiazoles resulted in an increase in anti-T. cruzi activity in comparison to thiosemicarbazones...
April 21, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28238819/alkylphospholipids-an-update-on-molecular-mechanisms-and-clinical-relevance
#13
REVIEW
Pablo Ríos-Marco, Carmen Marco, Xiomara Gálvez, Jose M Jiménez-López, María P Carrasco
Alkylphospholipid (APL) represent a new class of drugs which do not interact directly with DNA but act on the cell membrane where they accumulate and interfere with lipid metabolism and signalling pathways. This review summarizes the mode of action at the molecular level of these compounds. In this sense, a diversity of mechanisms has been suggested to explain the actions of clinically-relevant APLs, in particular, in cancer treatment. One consistently reported finding is that APLs reduce the biosynthesis of phosphatidylcholine (PC) by inhibiting the rate-limiting enzyme CTP:phosphocholine cytidylyltransferase (CT)...
February 23, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28236702/antiparasitic-activity-of-1-3-dioxolanes-containing-tellurium-in-trichomonas-vaginalis
#14
Ângela Sena-Lopes, Raquel Nascimento das Neves, Francisco Silvestre Brilhante Bezerra, Mara Thais de Oliveira Silva, Patrick C Nobre, Gelson Perin, Diego Alves, Lucielli Savegnago, Karine Rech Begnini, Fabiana Kommling Seixas, Tiago Collares, Sibele Borsuk
The increased prevalence of metronidazole-resistant infections has resulted in a search for alternative drugs for the treatment of trichomoniasis. In the present study, we report the preparation and in vitro activity of three 1,3-dioxolanes that contain tellurium (PTeDOX 01, PTeDOX 02, and PTeDOX 03) against Trichomonas vaginalis. Six concentrations of these compounds were analyzed for in vitro activity against ATCC 30236 isolate of T. vaginalis. PTeDOX 01 reported a cytotoxic effect against 100% of T. vaginalis trophozoites at a final concentration of 90μM with an IC50 of 60μM...
February 22, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28231520/medicinal-plants-used-as-anthelmintics-ethnomedical-pharmacological-and-phytochemical-studies
#15
REVIEW
Juan Carlos Romero-Benavides, Ana Lucía Ruano, Ronal Silva-Rivas, Paola Castillo-Veintimilla, Sara Vivanco-Jaramillo, Natalia Bailon-Moscoso
Intestinal parasites delay mental and physical development in children. Infection with these parasites can result in complications during pregnancy and alter the health of newborns, which has long-term effects on educational attainment and economic productivity. The appearance of resistance against classical drug treatments generates interest in the development of new deworming alternatives. We think that research of new plants species may reveal potential antiparasitic compounds. This review is focused on the use of plants and secondary metabolites against intestinal parasites...
March 31, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28215185/nutritive-value-and-anthelmintic-effect-of-sainfoin-pellets-fed-to-experimentally-infected-growing-rabbits
#16
H Legendre, H Hoste, T Gidenne
Alternative strategies to synthetic chemical drugs are needed in livestock and are a key issue in organic farming today. This study aimed at examining the potentialities of sainfoin, a legume rich in condensed tannins, as a nutraceutical that combines nutritive and antiparasitic effects in rabbits. To test the effect of infection with a helminth (I: infected groups; NI: not infected groups) and the effect of substituting 40% of the alfalfa in a control diet (C) with sainfoin (diet S), four groups of 16 weaned rabbits were arranged according to a 2×2 bifactorial design...
February 20, 2017: Animal: An International Journal of Animal Bioscience
https://www.readbyqxmd.com/read/28187957/discovery-of-n-2-aminoethyl-n-benzyloxyphenyl-benzamides-new-potent-trypanosoma-brucei-inhibitors
#17
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...
March 1, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28167514/pediatric-exposures-to-veterinary-pharmaceuticals
#18
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
#19
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
#20
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
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"