Search results for "Antiparasitic"

showing 3 items of 23 documents

Synthesis and biological evaluation of papain-family cathepsin L-like cysteine protease inhibitors containing a 1,4-benzodiazepine scaffold as antipr…

2014

Novel papain-family cathepsin L-like cysteine protease inhibitors endowed with antitrypanosomal and antimalarial activity were developed, through an optimization study of previously developed inhibitors. In the present work, we studied the structure-activity relationships of these derivatives, with the aim to develop new analogues with a simplified and more synthetically accessible structure and with improved antiparasitic activity. The structure of the model compounds was significantly simplified by modifying or even eliminating the side chain appended at the C3 atom of the benzodiazepine scaffold. In addition, a simple methylene spacer of appropriate length was inserted between the benzod…

Trypanosomamedicine.drug_classPeptidomimeticStereochemistryAntiparasiticCell SurvivalCathepsin LAntiprotozoal AgentsCysteine Proteinase InhibitorsBiochemistryCathepsin BCell LineCathepsin Lchemistry.chemical_compoundBenzodiazepinesMiceStructure-Activity RelationshipDrug DiscoverymedicineMoietyAnimalsGeneral Pharmacology Toxicology and PharmaceuticsPharmacologyCathepsinbiologyOrganic ChemistryCombinatorial chemistryCysteine proteasePapainantiprotozoal agents; inhibitors; Malaria; Peptidomimetics; structure-activity relationshipsCysteine EndopeptidaseschemistryAntiprotozoalbiology.proteinMolecular MedicineProtein BindingChemMedChem
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Efficacy and safety assessment of azithromycin 1.5% eye drops (azyter) in peri-operative antibio-prophylaxis for cataract surgery

2009

International audience; Introduction: Background: Endophthalmitis is still one of the most fearsome complications of cataract surgery. The most important pathogens causing post-operative phacoemulsification endophthalmitis are staphylococci. Methods: 85 patients were included in a phase II pilot study. Patients were divided in three groups, group 1 and 3 received either azithromycin 1.5% eye drops or placebo eye drops one day before surgery and for 2 days after surgery and group 2 received azithromycin 1.5% eye drops for 3 days after surgery. Treatments were administered twice a day: one drop in the morning and one in the evening. Bacterial samples were collected three times from the conjun…

[SDV.MHEP] Life Sciences [q-bio]/Human health and pathology[SDV.MHEP.OS] Life Sciences [q-bio]/Human health and pathology/Sensory Organscataractclinical (human) or epidemiologic studies: treatment/prevention assessment/controlled clinical trials[SDV.MHEP.OS]Life Sciences [q-bio]/Human health and pathology/Sensory Organsantibiotics/antifungals/antiparasitics[SDV.MHEP]Life Sciences [q-bio]/Human health and pathology
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Salmon lice in the Pacific Ocean show evidence of evolved resistance to parasiticide treatment

2022

AbstractParasitic salmon lice (Lepeophtheirus salmonis) threaten the economic and ecological sustainability of salmon farming, and their evolved resistance to treatment with emamectin benzoate (EMB) has been a major problem for salmon farming in the Atlantic Ocean. In contrast, the Pacific Ocean, where wild salmon are far more abundant, has not seen widespread evolution of EMB-resistant lice. Here, we use EMB bioassays and counts of lice on farms from the Broughton Archipelago, Canada—a core region of salmon farming in the Pacific—to show that EMB sensitivity has dramatically decreased since 2010, concurrent with marked decrease in the field efficacy of EMB treatments. Notably, these bioass…

endocrine systemPacific OceanMultidisciplinaryAntiparasitic Agentsanimal diseaseslohimeribiologiatäitresistenssiCopepodakalanviljelySalmonLepeophtheirus salmonisloisetemamektiinibentsoaattiparasitic diseasesAnimalsParasitesVDP::Landbruks- og Fiskerifag: 900::Fiskerifag: 920::Fiskehelse: 923hormones hormone substitutes and hormone antagonistsemamectin benzoate
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