Kelly Chibale

Kelly Chibale

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Kelly Chibale

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Pharmacokinetics and Organ Distribution of C-3 Alkyl Esters as Potential Antimycobacterial Prodrugs of Fusidic Acid.

ACS Infect Dis 2020 Mar 3;6(3):459-466. Epub 2020 Feb 3.

Division of Clinical Pharmacology, Department of Medicine, Groote Schuur Hospital, University of Cape Town, Cape Town, South Africa.

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http://dx.doi.org/10.1021/acsinfecdis.9b00405DOI Listing
March 2020

Synthesis and evaluation of the performance of a small molecule library based on diverse tropane-related scaffolds.

Bioorg Med Chem 2020 Mar 16:115442. Epub 2020 Mar 16.

School of Chemistry, University of Leeds, Leeds LS2 9JT, UK. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2020.115442DOI Listing
March 2020

Combining Stage Specificity and Metabolomic Profiling to Advance Antimalarial Drug Discovery.

Cell Chem Biol 2020 Feb 5;27(2):158-171.e3. Epub 2019 Dec 5.

Department of Microbiology and Immunology, Columbia University Irving Medical Center, New York, NY 10032, USA. Electronic address:

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http://dx.doi.org/10.1016/j.chembiol.2019.11.009DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7031696PMC
February 2020

Design and synthesis of novel ferrocene-quinoline conjugates and evaluation of their electrochemical and antiplasmodium properties.

Eur J Med Chem 2020 Feb 13;187:111963. Epub 2019 Dec 13.

SynBioC Research Group, Department of Green Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000, Ghent, Belgium. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2019.111963DOI Listing
February 2020

The quest for the holy grail: new antitubercular chemical entities, targets and strategies.

Drug Discov Today 2020 Feb 13. Epub 2020 Feb 13.

Drug Discovery and Development Centre (H3D), University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, Department of Chemistry and Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.drudis.2020.02.003DOI Listing
February 2020

Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present).

J Med Chem 2020 Jan 23. Epub 2020 Jan 23.

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

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http://dx.doi.org/10.1021/acs.jmedchem.9b01622DOI Listing
January 2020

Exploring the Antiplasmodial 2-Aminopyridines as Potential Antitrypanosomal Agents.

ChemMedChem 2019 Dec 12;14(24):2034-2041. Epub 2019 Nov 12.

Rhodes University, Grahamstown, 6140, South Africa.

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http://dx.doi.org/10.1002/cmdc.201900492DOI Listing
December 2019

Structure elaboration of isoniazid: synthesis, in silico molecular docking and antimycobacterial activity of isoniazid-pyrimidine conjugates.

Mol Divers 2019 Oct 18. Epub 2019 Oct 18.

Department of Chemistry, UGC Centre of Advance Study-II, Guru Nanak Dev University, Amritsar, 143 005, India.

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http://dx.doi.org/10.1007/s11030-019-10004-1DOI Listing
October 2019

Azaaurones as Potent Antimycobacterial Agents Active against MDR- and XDR-TB.

ChemMedChem 2019 Aug 25;14(16):1537-1546. Epub 2019 Jul 25.

Instituto de Investigação do Medicamento (iMed.ULisboa), Faculdade de Farmácia, Universidade de Lisboa, Av. Prof. Gama Pinto, 1649-003, Lisboa, Portugal.

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http://dx.doi.org/10.1002/cmdc.201900289DOI Listing
August 2019

Cocrystal and Salt Forms of an Imidazopyridazine Antimalarial Drug Lead.

J Pharm Sci 2019 Jul 25;108(7):2349-2357. Epub 2019 Feb 25.

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

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http://dx.doi.org/10.1016/j.xphs.2019.02.006DOI Listing
July 2019

Incorporation of an intramolecular hydrogen bonding motif in the side chain of antimalarial benzimidazoles.

Medchemcomm 2019 Mar 19;10(3):450-455. Epub 2019 Feb 19.

Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa . Email: ; ; Tel: +27 21 6502553.

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http://dx.doi.org/10.1039/c8md00608cDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6457172PMC
March 2019

Structure-activity relationship studies of antiplasmodial cyclometallated ruthenium(II), rhodium(III) and iridium(III) complexes of 2-phenylbenzimidazoles.

Eur J Med Chem 2019 Jan 10;161:11-21. Epub 2018 Oct 10.

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

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https://linkinghub.elsevier.com/retrieve/pii/S02235234183088
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http://dx.doi.org/10.1016/j.ejmech.2018.10.019DOI Listing
January 2019

Investigating Sulfoxide-to-Sulfone Conversion as a Prodrug Strategy for a Phosphatidylinositol 4-Kinase Inhibitor in a Humanized Mouse Model of Malaria.

Antimicrob Agents Chemother 2018 12 26;62(12). Epub 2018 Nov 26.

Drug Discovery and Development Centre (H3D), Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, South Africa

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http://dx.doi.org/10.1128/AAC.00261-18DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6256810PMC
December 2018

Antiplasmodial imidazopyridazines: structure-activity relationship studies lead to the identification of analogues with improved solubility and hERG profiles.

Medchemcomm 2018 Oct 6;9(10):1733-1745. Epub 2018 Sep 6.

Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa . Email: ; ; Tel: +27 21 6502553.

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http://xlink.rsc.org/?DOI=C8MD00382C
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http://dx.doi.org/10.1039/c8md00382cDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6194489PMC
October 2018

3D-QSAR Modeling and Synthesis of New Fusidic Acid Derivatives as Antiplasmodial Agents.

J Chem Inf Model 2018 08 7;58(8):1553-1560. Epub 2018 Aug 7.

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

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http://dx.doi.org/10.1021/acs.jcim.8b00105DOI Listing
August 2018

Pyrimidine-chloroquinoline hybrids: Synthesis and antiplasmodial activity.

Eur J Med Chem 2018 Mar 9;148:39-53. Epub 2018 Feb 9.

Department of Chemistry, UGC-Centre for Advanced Studies-II, Guru Nanak Dev University, Amritsar 143005, India. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2018.02.021DOI Listing
March 2018

Recent updates in the discovery and development of novel antimalarial drug candidates.

Medchemcomm 2018 Mar 2;9(3):437-453. Epub 2018 Feb 2.

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

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http://dx.doi.org/10.1039/c7md00637cDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6071755PMC
March 2018

Correction: Recent updates in the discovery and development of novel antimalarial drug candidates.

Medchemcomm 2018 03 2;9(3):590. Epub 2018 Mar 2.

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

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http://xlink.rsc.org/?DOI=C8MD90009D
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http://dx.doi.org/10.1039/c8md90009dDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6144541PMC
March 2018

Reversed isoniazids: Design, synthesis and evaluation against Mycobacterium tuberculosis.

Bioorg Med Chem 2018 02 29;26(4):833-844. Epub 2017 Dec 29.

Department of Chemistry, University of Cape Town, Rondebosch, 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch, 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, Department of Chemistry, University of Cape Town, Rondebosch, 7701, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2017.12.047DOI Listing
February 2018

The Design and Development of a Potent and Selective Novel Diprolyl Derivative That Binds to the N-Domain of Angiotensin-I Converting Enzyme.

J Med Chem 2018 01 21;61(1):344-359. Epub 2017 Dec 21.

Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Observatory 7925, South Africa.

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http://dx.doi.org/10.1021/acs.jmedchem.7b01478DOI Listing
January 2018

Antimicrobial activity of organometallic isonicotinyl and pyrazinyl ferrocenyl-derived complexes.

Dalton Trans 2017 Aug 17;46(30):9875-9885. Epub 2017 Jul 17.

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

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http://dx.doi.org/10.1039/c7dt01952aDOI Listing
August 2017

Insights into Integrated Lead Generation and Target Identification in Malaria and Tuberculosis Drug Discovery.

Acc Chem Res 2017 07 21;50(7):1606-1616. Epub 2017 Jun 21.

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

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http://dx.doi.org/10.1021/acs.accounts.6b00631DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5518282PMC
July 2017

Identification of steroid-like natural products as antiplasmodial agents by 2D and 3D similarity-based virtual screening.

Medchemcomm 2017 Jun 22;8(6):1152-1157. Epub 2017 Mar 22.

Department of Chemistry , University of Cape Town , Rondebosch 7701 , South Africa . Email: ; Email: ; ; Tel: +1 (305) 348 6661 ; Tel: +27 21 650 2553.

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http://dx.doi.org/10.1039/c7md00063dDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6071788PMC
June 2017

Synthesis and biological evaluation of 4 arylcoumarin analogues as tubulin-targeting antitumor agents.

Bioorg Med Chem 2017 03 27;25(5):1652-1665. Epub 2017 Jan 27.

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2017.01.035DOI Listing
March 2017

Exploration of thiaheterocyclic hHDAC6 inhibitors as potential antiplasmodial agents.

Future Med Chem 2017 03 6;9(4):357-364. Epub 2017 Mar 6.

SynBioC Research Group, Department of Sustainable Organic Chemistry & Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000, Ghent, Belgium.

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http://dx.doi.org/10.4155/fmc-2016-0215DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7099625PMC
March 2017

Intestinal Transport Characteristics and Metabolism of C-Glucosyl Dihydrochalcone, Aspalathin.

Molecules 2017 Mar 30;22(4). Epub 2017 Mar 30.

Biomedical Research and Innovation Platform, South African Medical Research Council, Tygerberg, Cape Town 7130, South Africa.

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http://dx.doi.org/10.3390/molecules22040554DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6154319PMC
March 2017

Synthesis and biological characterisation of ester and amide derivatives of fusidic acid as antiplasmodial agents.

Bioorg Med Chem Lett 2017 02 25;27(3):658-661. Epub 2016 Nov 25.

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2016.11.077DOI Listing
February 2017

Carbon-14 radiolabeling and tissue distribution evaluation of MMV390048.

J Labelled Comp Radiopharm 2016 12 20;59(14):680-688. Epub 2016 Sep 20.

DST/NWU, Preclinical Drug Development Platform, North-West University, Potchefstroom, South Africa.

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http://dx.doi.org/10.1002/jlcr.3445DOI Listing
December 2016

The Dynamic Nonprime Binding of Sampatrilat to the C-Domain of Angiotensin-Converting Enzyme.

J Chem Inf Model 2016 12 13;56(12):2486-2494. Epub 2016 Dec 13.

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

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http://dx.doi.org/10.1021/acs.jcim.6b00524DOI Listing
December 2016

The Role of Natural Products in Drug Discovery and Development against Neglected Tropical Diseases.

Molecules 2016 Dec 31;22(1). Epub 2016 Dec 31.

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

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http://dx.doi.org/10.3390/molecules22010058DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155950PMC
December 2016

Preparation and Physicochemical Characterization of an Inclusion Complex Between Dimethylated β-Cyclodextrin and a Drug Lead From a New Class of Orally Active Antimalarial 3,5-Diaryl-2-Aminopyridines.

J Pharm Sci 2016 11 15;105(11):3344-3350. Epub 2016 Sep 15.

Department of Chemistry, Centre for Supramolecular Chemistry Research, University of Cape Town, Rondebosch, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.xphs.2016.07.030DOI Listing
November 2016

Bioisosteric ferrocenyl-containing quinolines with antiplasmodial and antitrichomonal properties.

Dalton Trans 2016 Nov;45(47):19086-19095

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

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http://dx.doi.org/10.1039/c6dt03175gDOI Listing
November 2016

Characterisation of artemisinin-chloroquinoline hybrids for potential metabolic liabilities.

Xenobiotica 2016 4;46(3):234-40. Epub 2015 Sep 4.

a Department of ADMET/PK & BAC , African Institute of Biomedical Science and Technology , Harare , Zimbabwe .

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http://www.tandfonline.com/doi/full/10.3109/00498254.2015.10
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http://dx.doi.org/10.3109/00498254.2015.1070975DOI Listing
October 2016

Esterase phenotyping in human liver in vitro: specificity of carboxylesterase inhibitors.

Xenobiotica 2016 Oct 18;46(10):862-7. Epub 2016 Feb 18.

a Department of Drug Metabolism and Pharmacokinetics , Integrated Drug Disposition Section, Novartis Institutes for BioMedical Research , Basel , Switzerland .

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http://dx.doi.org/10.3109/00498254.2015.1133867DOI Listing
October 2016

Design, Synthesis, and Evaluation of Novel Hybrid Efflux Pump Inhibitors for Use against Mycobacterium tuberculosis.

ACS Infect Dis 2016 10 6;2(10):714-725. Epub 2016 Sep 6.

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

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http://dx.doi.org/10.1021/acsinfecdis.6b00111DOI Listing
October 2016

Antiplasmodial drug targets: a patent review (2000 - 2013).

Expert Opin Ther Pat 2016 13;26(1):107-30. Epub 2015 Nov 13.

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

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http://dx.doi.org/10.1517/13543776.2016.1113258DOI Listing
September 2016

Design, synthesis, and In vitro antituberculosis activity of 2(5H)-Furanone derivatives.

IUBMB Life 2016 08 27;68(8):612-20. Epub 2016 Jun 27.

Division of Molecular Biology and Human Genetics, Faculty of Medicine and Health Sciences, SAMRC Centre for TB Research, DST-NRF Centre of Excellence for Biomedical Tuberculosis Research, Stellenbosch University, Tygerberg, Cape Town, South Africa.

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http://dx.doi.org/10.1002/iub.1526DOI Listing
August 2016

Chloroquine-containing compounds: a patent review (2010 - 2014).

Expert Opin Ther Pat 2015 1;25(9):1003-24. Epub 2015 Jun 1.

a 1 University of Cape Town, Department of Chemistry , Rondebosch 7701, South Africa.

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http://dx.doi.org/10.1517/13543776.2015.1050791DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC7103710PMC
May 2016

Cyclopalladated organosilane-tethered thiosemicarbazones: novel strategies for improving antiplasmodial activity.

Dalton Trans 2016 Apr 25;45(13):5514-20. Epub 2016 Feb 25.

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

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http://dx.doi.org/10.1039/c5dt04918kDOI Listing
April 2016

Identification of New Human Malaria Parasite Plasmodium falciparum Dihydroorotate Dehydrogenase Inhibitors by Pharmacophore and Structure-Based Virtual Screening.

J Chem Inf Model 2016 Mar 8;56(3):548-62. Epub 2016 Mar 8.

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

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http://dx.doi.org/10.1021/acs.jcim.5b00680DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4871132PMC
March 2016

Computer-Aided Drug Discovery Approaches against the Tropical Infectious Diseases Malaria, Tuberculosis, Trypanosomiasis, and Leishmaniasis.

ACS Infect Dis 2016 01 16;2(1):8-31. Epub 2015 Nov 16.

Department of Pharmaceutical Chemistry and ‡Division of Pharmacology, School of Pharmacy, University of Nairobi , P.O. Box 19676-00202, Nairobi, Kenya.

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http://dx.doi.org/10.1021/acsinfecdis.5b00093DOI Listing
January 2016

New Verapamil Analogs Inhibit Intracellular Mycobacteria without Affecting the Functions of Mycobacterium-Specific T Cells.

Antimicrob Agents Chemother 2015 Dec 7;60(3):1216-25. Epub 2015 Dec 7.

Department of Chemistry and South African Medical Research Council Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch, South Africa Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch, South Africa.

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http://dx.doi.org/10.1128/AAC.01567-15DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4775996PMC
December 2015

Antiplasmodial activity, in vivo pharmacokinetics and anti-malarial efficacy evaluation of hydroxypyridinone hybrids in a mouse model.

Malar J 2015 Dec 16;14:505. Epub 2015 Dec 16.

Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, Cape Town, 7925, South Africa.

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http://dx.doi.org/10.1186/s12936-015-1032-5DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4681141PMC
December 2015

Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization.

Bioorg Med Chem 2015 Nov 22;23(22):7240-50. Epub 2015 Oct 22.

Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2015.10.021DOI Listing
November 2015

Antimalarial benzoheterocyclic 4-aminoquinolines: Structure-activity relationship, in vivo evaluation, mechanistic and bioactivation studies.

Bioorg Med Chem 2015 Sep 30;23(17):5419-32. Epub 2015 Jul 30.

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2015.07.051DOI Listing
September 2015

Structure-Activity Relationship Studies of Orally Active Antimalarial 2,4-Diamino-thienopyrimidines.

J Med Chem 2015 Sep 8;58(18):7572-9. Epub 2015 Sep 8.

Drug Discovery and Development Centre (H3D), Department of Chemistry, University of Cape Town , Rondebosch, Cape Town 7701, South Africa.

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http://dx.doi.org/10.1021/acs.jmedchem.5b01156DOI Listing
September 2015

New developments in antiinfectives research for tropical infectious diseases.

Authors:
Kelly Chibale

Bioorg Med Chem 2015 Aug 4;23(16):5085-6. Epub 2015 May 4.

Department of Chemistry and Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2015.04.077DOI Listing
August 2015

Synthesis, antiplasmodial activity and mechanistic studies of pyrimidine-5-carbonitrile and quinoline hybrids.

Eur J Med Chem 2015 Aug 12;101:52-62. Epub 2015 Jun 12.

Department of Chemistry, UGC-Centre of Advance Study-II, Guru Nanak Dev University, Amritsar 143005, India. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2015.06.024DOI Listing
August 2015

Primaquine-pyrimidine hybrids: synthesis and dual-stage antiplasmodial activity.

Eur J Med Chem 2015 Aug 29;101:266-73. Epub 2015 Jun 29.

Department of Chemistry, UGC-Centre for Advanced Studies-II, Guru Nanak Dev University, Amritsar 143005, India. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2015.06.045DOI Listing
August 2015

Ferrocene-pyrimidine conjugates: Synthesis, electrochemistry, physicochemical properties and antiplasmodial activities.

Eur J Med Chem 2015 Jul 30;100:1-9. Epub 2015 May 30.

Department of Chemistry, UGC-Centre for Advanced Studies-II, Guru Nanak Dev University, Amritsar 143005, India. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2015.05.043DOI Listing
July 2015

Synthesis, antimycobacterial evaluation and pharmacophore modeling of analogues of the natural product formononetin.

Bioorg Med Chem Lett 2015 Jun 28;25(12):2510-3. Epub 2015 Apr 28.

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council, Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2015.04.064DOI Listing
June 2015

A Pharmacokinetic Study of Antimalarial 3,5-Diaryl-2-aminopyridine Derivatives.

Malar Res Treat 2015 29;2015:405962. Epub 2015 Mar 29.

Division of Clinical Pharmacology, Department of Medicine, University of Cape Town, Observatory, Cape Town 7925, South Africa.

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http://dx.doi.org/10.1155/2015/405962DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4393935PMC
April 2015

Synthesis of functionalized 3-, 5-, 6- and 8-aminoquinolines via intermediate (3-pyrrolin-1-yl)- and (2-oxopyrrolidin-1-yl)quinolines and evaluation of their antiplasmodial and antifungal activity.

Eur J Med Chem 2015 Mar 12;92:91-102. Epub 2014 Dec 12.

SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000, Ghent, Belgium. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2014.12.020DOI Listing
March 2015

Synthesis and structure-activity-relationship studies of thiazolidinediones as antiplasmodial inhibitors of the Plasmodium falciparum cysteine protease falcipain-2.

Eur J Med Chem 2015 Jan 2;90:507-18. Epub 2014 Dec 2.

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council, Drug Discovery and Development Unit, University of Cape Town, Rondebosch 7701, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.ejmech.2014.11.061DOI Listing
January 2015

Recent approaches to chemical discovery and development against malaria and the neglected tropical diseases human African trypanosomiasis and schistosomiasis.

Chem Rev 2014 Nov 11;114(22):11138-63. Epub 2014 Jul 11.

Novartis Institute for Tropical Diseases , Singapore 138670, Singapore.

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http://dx.doi.org/10.1021/cr500098fDOI Listing
November 2014

Structure-activity relationship studies of antiplasmodial aminomethylthiazoles.

Bioorg Med Chem Lett 2014 Nov 2;24(22):5207-11. Epub 2014 Oct 2.

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2014.09.071DOI Listing
November 2014

Physicochemical and drug metabolism characterization of a series of 4-aminoquinoline-3-hydroxypyridin-4-one hybrid molecules with antimalarial activity.

Expert Opin Drug Metab Toxicol 2014 Oct;10(10):1313-24

African Institute of Biomedical Science and Technology, Department of ADMET/PK and BAC , Dominion House, 211 Herbert Chitepo Street, Harare , Zimbabwe +263 4 710563 ;

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http://dx.doi.org/10.1517/17425255.2014.954547DOI Listing
October 2014

Kojic acid derived hydroxypyridinone-chloroquine hybrids: synthesis, crystal structure, antiplasmodial activity and β-haematin inhibition.

Bioorg Med Chem Lett 2014 Aug 14;24(15):3263-7. Epub 2014 Jun 14.

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery & Development Research Unit, Institute of Infectious Diseases and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2014.06.012DOI Listing
August 2014

Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery.

Bioorg Med Chem 2014 Aug 16;22(16):4453-61. Epub 2014 Jun 16.

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease & Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Electronic address:

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http://dx.doi.org/10.1016/j.bmc.2014.06.012DOI Listing
August 2014

Effects of a domain-selective ACE inhibitor in a mouse model of chronic angiotensin II-dependent hypertension.

Clin Sci (Lond) 2014 Jul;127(1):57-63

§Institute of Infectious Diseases and Molecular Medicine and Division of Medical Biochemistry, University of Cape Town, Cape Town, South Africa.

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http://www.clinsci.org/content/ppclinsci/127/1/57.full.pdf
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http://dx.doi.org/10.1042/CS20130808DOI Listing
July 2014

Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c.

Bioorg Med Chem Lett 2014 Jul 16;24(14):2985-90. Epub 2014 May 16.

Department of Chemistry, University of Cape Town, Rondebosch 7701, South Africa; South African Medical Research Council Drug Discovery and Development Research Unit, University of Cape Town, Rondebosch 7701, South Africa; Institute of Infectious Disease and Molecular Medicine, University of Cape Town, Rondebosch 7701, South Africa. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S0960894X140052
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http://dx.doi.org/10.1016/j.bmcl.2014.05.022DOI Listing
July 2014

Pharmacokinetic evaluation of lisinopril-tryptophan, a novel C-domain ACE inhibitor.

Eur J Pharm Sci 2014 Jun 20;56:113-9. Epub 2014 Feb 20.

Cardiovascular Research Unit, Chris Barnard Division of Cardiothoracic Surgery, University of Cape Town, Department of Health Sciences, Cape Town, South Africa. Electronic address:

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https://linkinghub.elsevier.com/retrieve/pii/S09280987140005
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http://dx.doi.org/10.1016/j.ejps.2014.01.012DOI Listing
June 2014

Synthesis of halogenated 4-quinolones and evaluation of their antiplasmodial activity.

Bioorg Med Chem Lett 2014 Feb 4;24(4):1214-7. Epub 2014 Jan 4.

SynBioC Research Group, Department of Sustainable Organic Chemistry and Technology, Faculty of Bioscience Engineering, Ghent University, Coupure Links 653, B-9000 Ghent, Belgium. Electronic address:

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http://dx.doi.org/10.1016/j.bmcl.2013.12.067DOI Listing
February 2014

Synthesis and in vitro and in vivo pharmacological evaluation of new 4-aminoquinoline-based compounds.

ACS Med Chem Lett 2013 Dec 1;4(12):1198-202. Epub 2013 Oct 1.

Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa ; Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Rondebosch 7701, South Africa.

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http://dx.doi.org/10.1021/ml400311rDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4027225PMC
December 2013

CRIMALDDI: platform technologies and novel anti-malarial drug targets.

Malar J 2013 Nov 5;12:396. Epub 2013 Nov 5.

Liverpool School of Tropical Medicine, Pembroke Place, Liverpool L3 5QA, UK.

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http://dx.doi.org/10.1186/1475-2875-12-396DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3827883PMC
November 2013

Design, Synthesis, and Antiplasmodial Activity of Hybrid Compounds Based on (2R,3S)-N-Benzoyl-3-phenylisoserine.

ACS Med Chem Lett 2013 Jul 22;4(7):637-41. Epub 2013 May 22.

Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa ; Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Rondebosch 7701, South Africa.

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http://dx.doi.org/10.1021/ml400164tDOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4027494PMC
July 2013

Synthesis, Antiplasmodial Activity, and β-Hematin Inhibition of Hydroxypyridone-Chloroquine Hybrids.

ACS Med Chem Lett 2013 Jul 20;4(7):642-6. Epub 2013 May 20.

Department of Chemistry, University of Cape Town , Rondebosch 7701, South Africa ; Institute of Infectious Disease and Molecular Medicine, University of Cape Town , Rondebosch 7701, South Africa.

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http://dx.doi.org/10.1021/ml4001084DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4027233PMC
July 2013