Search Results - "Shackleford, David M."
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Nitroheterocyclic drugs cure experimental Trypanosoma cruzi infections more effectively in the chronic stage than in the acute stage
Published in Scientific reports (17-10-2016)“…The insect-transmitted protozoan parasite Trypanosoma cruzi is the causative agent of Chagas disease, and infects 5–8 million people in Latin America. Chagas…”
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An in vitro toolbox to accelerate anti-malarial drug discovery and development
Published in Malaria journal (02-01-2020)“…Modelling and simulation are being increasingly utilized to support the discovery and development of new anti-malarial drugs. These approaches require reliable…”
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Discovery and Structure–Activity Relationships of Quinazolinone-2-carboxamide Derivatives as Novel Orally Efficacious Antimalarials
Published in Journal of medicinal chemistry (09-09-2021)“…A phenotypic high-throughput screen allowed discovery of quinazolinone-2-carboxamide derivatives as a novel antimalarial scaffold. Structure–activity…”
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Enhancing the Oral Absorption of Kinase Inhibitors Using Lipophilic Salts and Lipid-Based Formulations
Published in Molecular pharmaceutics (03-12-2018)“…The absolute bioavailability of many small molecule kinase inhibitors (smKIs) is low. The reasons for low bioavailability are multifaceted and include…”
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Structure–Activity Relationship of the Antimalarial Ozonide Artefenomel (OZ439)
Published in Journal of medicinal chemistry (13-04-2017)“…Building on insights gained from the discovery of the antimalarial ozonide arterolane (OZ277), we now describe the structure–activity relationship (SAR) of the…”
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Discovery and Structure–Activity Relationships of Pyrrolone Antimalarials
Published in Journal of medicinal chemistry (11-04-2013)“…In the pursuit of new antimalarial leads, a phenotypic screening of various commercially sourced compound libraries was undertaken by the World Health…”
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3,5-Diaryl-2-aminopyridines as a Novel Class of Orally Active Antimalarials Demonstrating Single Dose Cure in Mice and Clinical Candidate Potential
Published in Journal of medicinal chemistry (12-04-2012)“…A novel class of orally active antimalarial 3,5-diaryl-2-aminopyridines has been identified from phenotypic whole cell high-throughput screening of a…”
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Selecting an anti-malarial clinical candidate from two potent dihydroisoquinolones
Published in Malaria journal (19-02-2021)“…The ongoing global malaria eradication campaign requires development of potent, safe, and cost-effective drugs lacking cross-resistance with existing…”
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The Anti-Inflammatory Drug Aspirin Does Not Protect Against Chemotherapy-Induced Memory Impairment by Paclitaxel in Mice
Published in Frontiers in oncology (14-12-2020)“…Inflammation has been proposed to play a causal role in chemobrain which-if true-would represent an opportunity to repurpose existing anti-inflammatory drugs…”
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Antimalarial Activity of Pyrroloiminoquinones from the Australian Marine Sponge Zyzzya sp
Published in Journal of medicinal chemistry (28-06-2012)“…A new bispyrroloiminoquinone alkaloid, tsitsikammamine C (1), displayed potent in vitro antimalarial activity with IC50 values of 13 and 18 nM against…”
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Antitrypanosomal Activity of Fexinidazole Metabolites, Potential New Drug Candidates for Chagas Disease
Published in Antimicrobial agents and chemotherapy (01-08-2014)“…This study was designed to verify the in vivo efficacy of sulfoxide and sulfone fexinidazole metabolites following oral administration in a murine model of…”
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Increased In Vivo Exposure of N-(4-Hydroxyphenyl) Retinamide (4-HPR) to Achieve Plasma Concentrations Effective against Dengue Virus
Published in Pharmaceutics (18-07-2023)“…N-(4-hydroxyphenyl) retinamide (4-HPR, or fenretinide) has promising in vitro and in vivo antiviral activity against a range of flaviviruses and an established…”
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The novel compound PBT434 prevents iron mediated neurodegeneration and alpha-synuclein toxicity in multiple models of Parkinson's disease
Published in Acta neuropathologica communications (28-06-2017)“…Elevated iron in the SNpc may play a key role in Parkinson's disease (PD) neurodegeneration since drug candidates with high iron affinity rescue PD animal…”
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Progress in antischistosomal N,N′-diaryl urea SAR
Published in Bioorganic & medicinal chemistry letters (01-02-2018)“…[Display omitted] •Expansion of antischistosomal N,N′-diaryl urea SAR.•3-Trifluoromethyl-4-pyridyl and 2,2-difluorobenzodioxole improve…”
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Pharmacological Characterization, Structural Studies, and In Vivo Activities of Anti-Chagas Disease Lead Compounds Derived from Tipifarnib
Published in Antimicrobial Agents and Chemotherapy (01-09-2012)“…Classifications Services AAC Citing Articles Google Scholar PubMed Related Content Social Bookmarking CiteULike Delicious Digg Facebook Google+ Mendeley Reddit…”
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Synthesis and Biological Evaluation of Polysulfated Oligosaccharide Glycosides as Inhibitors of Angiogenesis and Tumor Growth
Published in Journal of medicinal chemistry (25-02-2010)“…A series of polysulfated penta- and tetrasaccharide glycosides containing α(1→3)/α(1→2)-linked mannose residues were synthesized as heparan sulfate (HS)…”
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PPARα and PPARγ activation is associated with pleural mesothelioma invasion but therapeutic inhibition is ineffective
Published in iScience (21-01-2022)“…Mesothelioma is a cancer that typically originates in the pleura of the lungs. It rapidly invades the surrounding tissues, causing pain and shortness of…”
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Preoperative β-Blockade with Propranolol Reduces Biomarkers of Metastasis in Breast Cancer: A Phase II Randomized Trial
Published in Clinical cancer research (15-04-2020)“…The majority of deaths from breast cancer occur following the development of metastatic disease, a process inhibited by β-blockers in preclinical studies. This…”
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Contribution of lymphatically transported testosterone undecanoate to the systemic exposure of testosterone after oral administration of two andriol formulations in conscious lymph duct-cannulated dogs
Published in The Journal of pharmacology and experimental therapeutics (01-09-2003)“…Orally administered testosterone (T) is ineffective in the treatment of male androgen deficiency syndromes due to extensive presystemic first-pass metabolism…”
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