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Human antiparasitic drugs

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https://www.readbyqxmd.com/read/28502250/antiplasmodial-dihetarylthioethers-target-the-coenzyme-a-synthesis-pathway-in-plasmodium-falciparum-erythrocytic-stages
#1
Thomas Weidner, Leonardo Lucantoni, Abed Nasereddin, Lutz Preu, Peter G Jones, Ron Dzikowski, Vicky M Avery, Conrad Kunick
BACKGROUND: Malaria is a widespread infectious disease that threatens a large proportion of the population in tropical and subtropical areas. Given the emerging resistance against the current standard anti-malaria chemotherapeutics, the development of alternative drugs is urgently needed. New anti-malarials representing chemotypes unrelated to currently used drugs have an increased potential for displaying novel mechanisms of action and thus exhibit low risk of cross-resistance against established drugs...
May 15, 2017: Malaria Journal
https://www.readbyqxmd.com/read/28446445/susceptibility-testing-of-medically-important-parasites
#2
REVIEW
Abebe Genetu Bayih, Anjan Debnath, Edward Mitre, Christopher D Huston, Benoît Laleu, Didier Leroy, Benjamin Blasco, Brice Campo, Timothy N C Wells, Paul A Willis, Peter Sjö, Wesley C Van Voorhis, Dylan R Pillai
In the last 2 decades, renewed attention to neglected tropical diseases (NTDs) has spurred the development of antiparasitic agents, especially in light of emerging drug resistance. The need for new drugs has required in vitro screening methods using parasite culture. Furthermore, clinical laboratories sought to correlate in vitro susceptibility methods with treatment outcomes, most notably with malaria. Parasites with their various life cycles present greater complexity than bacteria, for which standardized susceptibility methods exist...
July 2017: Clinical Microbiology Reviews
https://www.readbyqxmd.com/read/28433563/aryl-thiosemicarbazones-in%C3%A2-vitro-and-immunomodulatory-activities-against-l-%C3%A2-amazonensis
#3
Aline Caroline da Silva, Thiago André Ramos Dos Santos, Isis Viviane Bezerra da Silva, Marcos Victor Gregório de Oliveira, Diogo Rodrigo Magalhães Moreira, Ana Cristina Lima Leite, Valéria Rêgo Alves Pereira
Leishmaniasis is an infection caused by different species of Leishmania genus. Currently, there is no vaccine available for Leishmania infections in humans and conventional treatments are limited due to side effects. Therefore, the development of new antileishmanial drugs is an urgent need. In present study, we evaluated the cytotoxicity in host cells, leishmanicidal activity and immunomodulatory potential of seven aryl thiosemicarbazones. Host cell cytotoxicity was determined in peritoneal macrophages of BALB/c mouse, antiparasitic activity was determined against promastigotes and amastigotes of WHOM/00LTB 0016 strain of L...
April 19, 2017: Experimental Parasitology
https://www.readbyqxmd.com/read/28421410/antiparasitic-sesquiterpenes-from-the-cameroonian-spice-scleria-striatinux-and-preliminary-in-vitro-and-in-silico-dmpk-assessment
#4
Kennedy D Nyongbela, Fidele Ntie-Kang, Thomas R Hoye, Simon M N Efange
The antiparasitic activity and preliminary in vitro and in silico drug metabolism and pharmacokinetic (DMPK) assessment of six isomeric sesquiterpenes (1-6), isolated from the Cameroonian spice Scleria striatinux De Wild (Cyperaceae) is reported. The study was prompted by the observation that two of the compounds (1 and 2) exhibited varying levels of antiparasitic activity on Plasmodium falciparum, Trypanosoma brucei rhodesiense, Trypanosoma cruzi and Leishmania donovani. The in silico method employed a total of 46 descriptors, calculated using Schrödinger QikProp software...
April 18, 2017: Natural Products and Bioprospecting
https://www.readbyqxmd.com/read/28337329/antiparasitic-lead-discovery-toward-optimization-of-a-chemotype-with-activity-against-multiple-protozoan-parasites
#5
William Devine, Sarah M Thomas, Jessey Erath, Kelly A Bachovchin, Patricia J Lee, Susan E Leed, Ana Rodriguez, Richard J Sciotti, Kojo Mensa-Wilmot, Michael P Pollastri
Human African trypanosomiasis (HAT), Chagas disease, and leishmaniasis present a significant burden across the developing world. Existing therapeutics for these protozoal neglected tropical diseases suffer from severe side effects and toxicity. Previously, NEU-1045 (3) was identified as a promising lead with cross-pathogen activity, though it possessed poor physicochemical properties. We have designed a library of analogues with improved calculated physicochemical properties built on the quinoline scaffold of 3 incorporating small, polar aminoheterocycles in place of the 4-(3-fluorobenzyloxy)aniline substituent...
March 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28283781/gold-compounds-as-cysteine-protease-inhibitors-perspectives-for-pharmaceutical-application-as-antiparasitic-agents
#6
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/28265521/genetic-and-structural-study-of-dna-directed-rna-polymerase-ii-of-trypanosoma-brucei-towards-the-designing-of-novel-antiparasitic-agents
#7
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/28257952/in-vitro-immunomodulatory-effects-of-microemulsions-with-levamisole-delivery-systems-on-blood-phagocytes-interacting-with-giardia-lamblia
#8
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...
June 2017: Parasitology International
https://www.readbyqxmd.com/read/28238819/alkylphospholipids-an-update-on-molecular-mechanisms-and-clinical-relevance
#9
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/28187957/discovery-of-n-2-aminoethyl-n-benzyloxyphenyl-benzamides-new-potent-trypanosoma-brucei-inhibitors
#10
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
#11
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
#12
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
#13
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
#14
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
#15
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
#16
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
#17
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
#18
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...
March 2017: Trends in Parasitology
https://www.readbyqxmd.com/read/27719626/metabolic-inhibitors-as-antiparasitic-drugs-pharmacological-biochemical-and-molecular-perspectives
#19
REVIEW
Suprabhat Mukherjee, Niladri Mukherjee, Prajna Gayen, Priya Roy, Santi P Sinha Babu
BACKGROUND: 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 the best efforts for 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 are as added complications...
2016: Current Drug Metabolism
https://www.readbyqxmd.com/read/27519462/discovery-and-antiparasitic-activity-of-az960-as-a-trypanosoma-brucei-erk8-inhibitor
#20
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
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