Search Results - "Freund, Yvonne R"
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A potent antimalarial benzoxaborole targets a Plasmodium falciparum cleavage and polyadenylation specificity factor homologue
Published in Nature communications (06-03-2017)“…Benzoxaboroles are effective against bacterial, fungal and protozoan pathogens. We report potent activity of the benzoxaborole AN3661 against Plasmodium…”
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Identification of a potent benzoxaborole drug candidate for treating cryptosporidiosis
Published in Nature communications (27-06-2019)“…Cryptosporidiosis is a leading cause of life-threatening diarrhea in young children and causes chronic diarrhea in AIDS patients, but the only approved…”
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Benzoxaborole Antimalarial Agents. Part 5. Lead Optimization of Novel Amide Pyrazinyloxy Benzoxaboroles and Identification of a Preclinical Candidate
Published in Journal of medicinal chemistry (13-07-2017)“…Carboxamide pyrazinyloxy benzoxaboroles were investigated with the goal to identify a molecule with satisfactory antimalarial activity, physicochemical…”
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Discovery of a Novel Class of Boron-Based Antibacterials with Activity against Gram-Negative Bacteria
Published in Antimicrobial Agents and Chemotherapy (01-03-2013)“…OA Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley…”
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5
Targeting Toxoplasma gondii CPSF3 as a new approach to control toxoplasmosis
Published in EMBO molecular medicine (01-03-2017)“…Toxoplasma gondii is an important food and waterborne pathogen causing toxoplasmosis, a potentially severe disease in immunocompromised or congenitally…”
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Plasmodium falciparum Resistance to a Lead Benzoxaborole Due to Blocked Compound Activation and Altered Ubiquitination or Sumoylation
Published in mBio (28-01-2020)“…New antimalarial drugs are needed. The benzoxaborole AN13762 showed excellent activity against cultured , against fresh Ugandan isolates, and in murine malaria…”
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Host-parasite co-metabolic activation of antitrypanosomal aminomethyl-benzoxaboroles
Published in PLoS pathogens (01-02-2018)“…Recent development of benzoxaborole-based chemistry gave rise to a collection of compounds with great potential in targeting diverse infectious diseases,…”
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In vivo efficacy of the boron-pleuromutilin AN11251 against Wolbachia of the rodent filarial nematode Litomosoides sigmodontis
Published in PLoS neglected tropical diseases (01-01-2020)“…The elimination of filarial diseases such as onchocerciasis and lymphatic filariasis is hampered by the lack of a macrofilaricidal-adult worm killing-drug. In…”
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Discovery and structure–activity relationships of 6-(benzoylamino)benzoxaboroles as orally active anti-inflammatory agents
Published in Bioorganic & medicinal chemistry letters (01-11-2013)“…In vitro SAR of benzoxaborole derivatives against the release of three cytokines, mouse pharmacokinetics, and in vivo activities in mice are reported…”
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Cryptosporidium and Toxoplasma Parasites Are Inhibited by a Benzoxaborole Targeting Leucyl-tRNA Synthetase
Published in Antimicrobial agents and chemotherapy (01-10-2016)“…The apicomplexan parasites Cryptosporidium and Toxoplasma are serious threats to human health. Cryptosporidiosis is a severe diarrheal disease in malnourished…”
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Antimalarial Benzoxaboroles Target Plasmodium falciparum Leucyl-tRNA Synthetase
Published in Antimicrobial agents and chemotherapy (01-08-2016)“…There is a need for new antimalarials, ideally with novel mechanisms of action. Benzoxaboroles have been shown to be active against bacteria, fungi, and…”
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Identification of a 4-fluorobenzyl l-valinate amide benzoxaborole (AN11736) as a potential development candidate for the treatment of Animal African Trypanosomiasis (AAT)
Published in Bioorganic & medicinal chemistry letters (01-01-2018)“…[Display omitted] Novel l-valinate amide benzoxaboroles and analogues were designed and synthesized for a structure-activity-relationship (SAR) investigation…”
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Boron-based phosphodiesterase inhibitors show novel binding of boron to PDE4 bimetal center
Published in FEBS letters (21-09-2012)“…► Novel boron-containing small molecule inhibitors of phosphodiesterase 4. ► Co-crystal structure shows unique binding compared to catechol inhibitors. ► Boron…”
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Boron-Pleuromutilins as Anti-Wolbachia Agents with Potential for Treatment of Onchocerciasis and Lymphatic Filariasis
Published in Journal of medicinal chemistry (14-03-2019)“…A series of pleuromutilins modified by introduction of a boron-containing heterocycle on C(14) of the polycyclic core are described. These analogs were found…”
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Benzoxaborole Antimalarial Agents. Part 4. Discovery of Potent 6‑(2-(Alkoxycarbonyl)pyrazinyl-5-oxy)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles
Published in Journal of medicinal chemistry (09-07-2015)“…A series of 6-hetaryloxy benzoxaborole compounds was designed and synthesized for a structure–activity relationship (SAR) investigation to assess the changes…”
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Synthesis and structure–activity relationships of novel benzoxaboroles as a new class of antimalarial agents
Published in Bioorganic & medicinal chemistry letters (15-01-2011)“…A series of boron-containing benzoxaborole compounds was designed and synthesized for a SAR investigation for discovering a new antimalarial treatment…”
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Benzoxaborole antimalarial agents. Part 2: Discovery of fluoro-substituted 7-(2-carboxyethyl)-1,3-dihydro-1-hydroxy-2,1-benzoxaboroles
Published in Bioorganic & medicinal chemistry letters (01-02-2012)“…A series of new boron-containing benzoxaborole compounds was designed and synthesized for a continuing structure–activity relationship (SAR) investigation…”
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Structure–activity relationships of 6-(aminomethylphenoxy)-benzoxaborole derivatives as anti-inflammatory agent
Published in Bioorganic & medicinal chemistry letters (15-03-2013)“…Cytokine release inhibitory activity and pharmacokinetics of novel benzoxaborole derivatives are reported. A series of novel…”
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Inhibition of Toll-like receptor-mediated inflammation in vitro and in vivo by a novel benzoxaborole
Published in The Journal of pharmacology and experimental therapeutics (01-02-2013)“…Pro-inflammatory cytokines play a critical role in the development of autoimmune and inflammatory diseases. Targeting the cytokine environment has proven…”
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Macrofilaricidal Benzimidazole–Benzoxaborole Hybrids as an Approach to the Treatment of River Blindness: Part 1. Amide Linked Analogs
Published in ACS infectious diseases (14-02-2020)“…A series of benzimidazole–benzoxaborole hybrid molecules linked via an amide linker are described that exhibit good in vitro activity against Onchocerca…”
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