Susan A Charman

Susan A Charman

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Susan A Charman

Susan A Charman

Publications by authors named "Susan A Charman"

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The Development Process for Discovery and Clinical Advancement of Modern Antimalarials.

J Med Chem 2019 Dec 20;62(23):10526-10562. Epub 2019 Aug 20.

The Walter and Eliza Hall Institute of Medical Research , Parkville , Victoria 3052 , Australia.

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http://dx.doi.org/10.1021/acs.jmedchem.9b00761DOI Listing
December 2019

Ozonide Antimalarials Alkylate Heme in the Malaria Parasite .

ACS Infect Dis 2019 Dec 2;5(12):2076-2086. Epub 2019 Dec 2.

Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences , Monash University , 381 Royal Parade , Parkville , Victoria 3052 , Australia.

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http://dx.doi.org/10.1021/acsinfecdis.9b00257DOI Listing
December 2019

Novel Human Aminopeptidase N Inhibitors: Discovery and Optimization of Subsite Binding Interactions.

J Med Chem 2019 Aug 18;62(15):7185-7209. Epub 2019 Jul 18.

Infection and Immunity Program, Biomedicine Discovery Institute and Department of Microbiology , Monash University , Clayton Campus , Clayton , VIC 3800 , Australia.

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http://dx.doi.org/10.1021/acs.jmedchem.9b00757DOI Listing
August 2019

Ozonide Antimalarial Activity in the Context of Artemisinin-Resistant Malaria.

Trends Parasitol 2019 Jul 5;35(7):529-543. Epub 2019 Jun 5.

Drug Delivery, Disposition, and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Victoria, Australia. Electronic address:

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http://dx.doi.org/10.1016/j.pt.2019.05.002DOI Listing
July 2019

Falcipain Inhibitors Based on the Natural Product Gallinamide A Are Potent in Vitro and in Vivo Antimalarials.

J Med Chem 2019 Jun 22;62(11):5562-5578. Epub 2019 May 22.

School of Chemistry , Building F11, The University of Sydney , Sydney , New South Wales 2006 , Australia.

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http://dx.doi.org/10.1021/acs.jmedchem.9b00504DOI Listing
June 2019

SAR of a new antischistosomal urea carboxylic acid.

Bioorg Med Chem Lett 2018 12 25;28(23-24):3648-3651. Epub 2018 Oct 25.

College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, United States. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2018.10.039DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6301076PMC
December 2018

Using Human Plasma as an Assay Medium in Caco-2 Studies Improves Mass Balance for Lipophilic Compounds.

Pharm Res 2018 Sep 17;35(11):210. Epub 2018 Sep 17.

Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, 381 Royal Parade, Parkville, VIC, 3052, Australia.

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http://dx.doi.org/10.1007/s11095-018-2493-3DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6156755PMC
September 2018

Parasite-Mediated Degradation of Synthetic Ozonide Antimalarials Impacts Antimalarial Activity.

Antimicrob Agents Chemother 2018 03 23;62(3). Epub 2018 Feb 23.

Monash Institute of Pharmaceutical Sciences, Faculty of Pharmacy and Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia

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http://dx.doi.org/10.1128/AAC.01566-17DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5826100PMC
March 2018

Progress in antischistosomal N,N'-diaryl urea SAR.

Bioorg Med Chem Lett 2018 02 29;28(3):244-248. Epub 2017 Dec 29.

College of Pharmacy, University of Nebraska Medical Center, 986025 Nebraska Medical Center, Omaha, NE, United States. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2017.12.064DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6026081PMC
February 2018

Novel inhibitors of Plasmodium falciparum based on 2,5-disubstituted furans.

Eur J Med Chem 2017 Jan 11;126:929-936. Epub 2016 Dec 11.

Instituto de Química, Universidade Estadual de Campinas, Barão Geraldo, PO Box 6154, Campinas, SP 13084-971, Brazil. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2016.12.024DOI Listing
January 2017

Revisiting the SAR of the Antischistosomal Aryl Hydantoin (Ro 13-3978).

J Med Chem 2016 12 28;59(23):10705-10718. Epub 2016 Nov 28.

College of Pharmacy, University of Nebraska Medical Center , 986125 Nebraska Medical Center, Omaha, Nebraska 68198, United States.

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http://dx.doi.org/10.1021/acs.jmedchem.6b01410DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5150661PMC
December 2016

Comparison of the Exposure Time Dependence of the Activities of Synthetic Ozonide Antimalarials and Dihydroartemisinin against K13 Wild-Type and Mutant Plasmodium falciparum Strains.

Antimicrob Agents Chemother 2016 08 22;60(8):4501-10. Epub 2016 Jul 22.

Department of Biochemistry and Molecular Biology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Melbourne, VIC, Australia

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http://dx.doi.org/10.1128/AAC.00574-16DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4958167PMC
August 2016

Potent dual inhibitors of Plasmodium falciparum M1 and M17 aminopeptidases through optimization of S1 pocket interactions.

Eur J Med Chem 2016 Mar 13;110:43-64. Epub 2016 Jan 13.

Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus), Parkville, VIC 3052, Australia. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2016.01.015DOI Listing
March 2016

Trioxolane-Mediated Delivery of Mefloquine Limits Brain Exposure in a Mouse Model of Malaria.

ACS Med Chem Lett 2015 Nov 2;6(11):1145-9. Epub 2015 Oct 2.

Department of Pharmaceutical Chemistry and Department of Medicine, University of California San Francisco , 1700 Fourth Street, San Francisco, California 94158, United States.

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http://dx.doi.org/10.1021/acsmedchemlett.5b00296DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4645246PMC
November 2015

ELQ-300 prodrugs for enhanced delivery and single-dose cure of malaria.

Antimicrob Agents Chemother 2015 Sep 29;59(9):5555-60. Epub 2015 Jun 29.

VA Medical Center, Experimental Chemotherapy Laboratory, Portland, Oregon, USA Oregon Health & Science University, Department of Molecular Microbiology and Immunology, Portland, Oregon, USA

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http://dx.doi.org/10.1128/AAC.01183-15DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4538462PMC
September 2015

6-Arylpyrazine-2-carboxamides: A New Core for Trypanosoma brucei Inhibitors.

J Med Chem 2015 Sep 30;58(17):6753-65. Epub 2015 Aug 30.

Medicinal Chemistry, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus) , 381 Royal Parade, Parkville, Victoria 3052, Australia.

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http://dx.doi.org/10.1021/acs.jmedchem.5b00438DOI Listing
September 2015

Transformation of poorly water-soluble drugs into lipophilic ionic liquids enhances oral drug exposure from lipid based formulations.

Mol Pharm 2015 Jun 5;12(6):1980-91. Epub 2015 May 5.

∥ARC Centre of Excellence in Convergent Bio-Nano Science and Technology, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.

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http://dx.doi.org/10.1021/mp500790tDOI Listing
June 2015

Pyridyl benzamides as a novel class of potent inhibitors for the kinetoplastid Trypanosoma brucei.

J Med Chem 2014 Aug 17;57(15):6393-402. Epub 2014 Jul 17.

Medicinal Chemistry, ‡Centre for Drug Candidate Optimisation, and §Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University , Parkville, Victoria 3052, Australia.

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http://dx.doi.org/10.1021/jm500191uDOI Listing
August 2014

Fluorine modulates species selectivity in the triazolopyrimidine class of Plasmodium falciparum dihydroorotate dehydrogenase inhibitors.

J Med Chem 2014 Jun 13;57(12):5381-94. Epub 2014 Jun 13.

Department of Pharmacology, University of Texas Southwestern Medical Center at Dallas , 6001 Forest Park Boulevard, Dallas, Texas 75390-9041, United States.

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http://dx.doi.org/10.1021/jm500481tDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4079327PMC
June 2014

A prodrug approach toward cancer-related carbonic anhydrase inhibition.

J Med Chem 2013 Dec 20;56(23):9623-34. Epub 2013 Nov 20.

Eskitis Institute for Drug Discovery, Griffith University , Nathan, Queensland 4111, Australia.

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http://dx.doi.org/10.1021/jm401163eDOI Listing
December 2013

Structure-activity relationship studies of pyrrolone antimalarial agents.

ChemMedChem 2013 Sep 5;8(9):1537-44. Epub 2013 Aug 5.

Division of Biological Chemistry & Drug Discovery, College of Life Sciences, University of Dundee, Sir James Black Centre, Dow St, Dundee DD1 5EH, UK.

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http://dx.doi.org/10.1002/cmdc.201300177DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3963473PMC
September 2013

Discovery and structure-activity relationships of pyrrolone antimalarials.

J Med Chem 2013 Apr 21;56(7):2975-90. Epub 2013 Mar 21.

Division of Biological Chemistry and Drug Discovery, College of Life Sciences, University of Dundee, Sir James Black Centre, Dundee DD1 5EH, UK.

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http://dx.doi.org/10.1021/jm400009cDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3624797PMC
April 2013

Synthesis of acylated glycoconjugates as templates to investigate in vitro biopharmaceutical properties.

Bioorg Med Chem Lett 2013 Jan 29;23(2):455-9. Epub 2012 Nov 29.

Eskitis Institute for Cell and Molecular Therapies, Griffith University, Nathan, Queensland 4111, Australia.

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http://dx.doi.org/10.1016/j.bmcl.2012.11.056DOI Listing
January 2013

Strategies to address low drug solubility in discovery and development.

Pharmacol Rev 2013 Jan;65(1):315-499

Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.

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http://dx.doi.org/10.1124/pr.112.005660DOI Listing
January 2013

Computational prediction of CNS drug exposure based on a novel in vivo dataset.

Pharm Res 2012 Nov 29;29(11):3131-42. Epub 2012 Jun 29.

Department of Pharmacy Drug Optimization and Pharmaceutical Profiling Platform, Uppsala University, Uppsala Biomedical Center, P.O. Box 580, SE-751 23, Uppsala, Sweden.

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http://dx.doi.org/10.1007/s11095-012-0806-5DOI Listing
November 2012

Probing a potential in vivo drug-excipient interaction: temporal effects of a modified β-cyclodextrin on the intravenous pharmacokinetics of a model high-affinity drug ligand.

J Pharm Sci 2012 Sep 1;101(9):3381-9. Epub 2012 May 1.

Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.

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http://linkinghub.elsevier.com/retrieve/pii/S002235491531447
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http://dx.doi.org/10.1002/jps.23177DOI Listing
September 2012

Assessing the utility of an anti-malarial pharmacokinetic-pharmacodynamic model for aiding drug clinical development.

Malar J 2012 Aug 30;11:303. Epub 2012 Aug 30.

Centre for Molecular, Environmental, Genetic & Analytic Epidemiology, Melbourne School of Population Health, University of Melbourne, Level 3, 207 Bouverie St, Carlton, VIC 3053, Australia.

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http://dx.doi.org/10.1186/1475-2875-11-303DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3546862PMC
August 2012

Metallocene-based inhibitors of cancer-associated carbonic anhydrase enzymes IX and XII.

J Med Chem 2012 Jun 22;55(11):5506-17. Epub 2012 May 22.

Eskitis Institute for Cell and Molecular Therapies, Griffith University, Nathan, Queensland 4111, Australia.

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http://pubs.acs.org/doi/10.1021/jm300427m
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http://dx.doi.org/10.1021/jm300427mDOI Listing
June 2012

The involvement of a Na⁺- and Cl⁻-dependent transporter in the brain uptake of amantadine and rimantadine.

Mol Pharm 2012 Apr 1;9(4):883-93. Epub 2012 Mar 1.

Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria, Australia.

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http://dx.doi.org/10.1021/mp2004127DOI Listing
April 2012

Novel orally active antimalarial thiazoles.

J Med Chem 2011 Nov 11;54(21):7713-9. Epub 2011 Oct 11.

Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa.

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http://dx.doi.org/10.1021/jm201108kDOI Listing
November 2011

Antimalarial pyrido[1,2-a]benzimidazoles.

J Med Chem 2011 Jul 16;54(13):4581-9. Epub 2011 Jun 16.

Department of Chemistry, University of Cape Town, Rondebosch, South Africa.

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http://dx.doi.org/10.1021/jm200227rDOI Listing
July 2011

Preclinical comparison of intravenous melphalan pharmacokinetics administered in formulations containing either (SBE)7 m-β-cyclodextrin or a co-solvent system.

Biopharm Drug Dispos 2010 Nov;31(8-9):450-4

Centre for Drug Candidate Optimisation, Monash Institute of Pharmaceutical Sciences, Monash University (Parkville Campus), 381 Royal Parade, Parkville, Victoria 3052, Australia.

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http://dx.doi.org/10.1002/bdd.725DOI Listing
November 2010

Discovery of Novel Benzo[a]phenoxazine SSJ-183 as a Drug Candidate for Malaria.

ACS Med Chem Lett 2010 Oct 12;1(7):360-4. Epub 2010 Jul 12.

Drug Discovery Science Research Center, Hoshi University, 2-4-41 Ebara, Shinagawa, Tokyo 142-8501, Japan.

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http://dx.doi.org/10.1021/ml100120aDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4007839PMC
October 2010

Brain uptake of diazepam and phenytoin in a genetic animal model of absence epilepsy.

Clin Exp Pharmacol Physiol 2010 May 17;37(5-6):647-9. Epub 2010 Jan 17.

Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Victoria 3052, Australia.

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http://dx.doi.org/10.1111/j.1440-1681.2010.05362.xDOI Listing
May 2010

Sulfonamide linked neoglycoconjugates--a new class of inhibitors for cancer-associated carbonic anhydrases.

J Med Chem 2010 Apr;53(7):2913-26

Eskitis Institute for Cell and Molecular Therapies, Griffith University, 170 Kessels Road, Nathan, Queensland 4111, Australia.

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http://dx.doi.org/10.1021/jm901888xDOI Listing
April 2010