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Browsing by Author "Chibale, Kelly"

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Anti-cancer and anti-malarial 4-aminoquinoline derivatives : synthesis and solid-state investigations

Author: Melo, Candice Soares de Date: 2006 The work presented in this thesis is two-fold: (i) development of single agents that provide inhibition of both the growth of malaria parasites and of tumour cells in vitro, and (ii) inclusion of these potential novel inhibitors in cyclodextrin ... Read more
Anticancer properties of distinct antimalarial drug classes

Author: Hooft van Huijsduijnen, Rob ; Guy, R Kiplin ; Chibale, Kelly ; Haynes, Richard K ; Peitz, Ingmar ; Kelter, Gerhard ; Phillips, Margaret A ; Vennerstrom, Jonathan L ; Yuthavong, Yongyuth ; Wells, Timothy N C Date: 2013 We have tested five distinct classes of established and experimental antimalarial drugs for their anticancer potential, using a panel of 91 human cancer lines. Three classes of drugs: artemisinins, synthetic peroxides and DHFR (dihydrofolate ... Read more c b
Antimalarial activity and pharmacokinetic properties of new chemical entities

Author: Dambuza, Ntokozo Shirley Date: 2013 Includes abstract. Includes bibliographical references. Read more
Antimalarial and cysteine protease inhibitor pharmacophores as scaffolds for new antimalarial agents

Author: Musonda, Chitalu Christopher Date: 2005 The work in this thesis is threefold: (i) A new series of antiplasmodial agents were initially designed based on the β-amino alcohol bioactiphore, a subunit that is found in a number of antimalarial agents. (ii) Various thiosemicarbozones ... Read more
Antimalarial benzimidazoles and related structures incorporating an intramolecular hydrogen bonding motif: medicinal chemistry and mechanistic studies

Author: Attram, Henrietta Dede Date: 2021 Malaria, an infectious disease caused by Plasmodium parasites, continues to take an enormous toll on human health, particularly in tropical regions. According to the World Health Organization (WHO), progress against malaria eradication has ... Read more
Antimalarial drug rescue through safety improvement: design, synthesis and evaluation of amaodiaquine analogues

Author: Ongarora, Dennis Sure Bagwasi Date: 2014 Malaria is a major cause of morbidity and mortality globally, resulting in over 200 million cases and 650, 000 deaths in 2010 according to the 2012 WHO Malaria Report. Furthermore, malaria endemicity is associated with poor economic growth. ... Read more
Antimalarial imidazopyridazines and aminopyrazines: synthesis, physicochemical optimization and structure-activity relationships

Author: Cheuka, Peter Mubanga Date: 2018 According to the World Health Organization (WHO) world malaria report released in 2017, about 445,000 malaria deaths were recorded in 2016, a similar mortality as that recorded in the preceding year (446,000 deaths in 2015). Once effective ... Read more
Antimalarials based on the arylpiperazine privileged substructure

Author: Molyneaux, Carrie-Anne Date: 2005 Based on a previous study, arylpiperazines (2-chlorophenylpiperazine, 2-ethoxyphenylpiperazine and phenylpiperazine) were found to be significantly more potent against the chloroquine-resistant (K1) strain than against the chloroquine-sensitive(DIO) ... Read more
Antimycobacterial 2-aminoquinazolinones and benzoxazole-based oximes: synthesis, biological evaluation, physicochemical profiling and supramolecular derivatization

Author: Njaria, Paul Magutu Date: 2017 Tuberculosis (TB) is a life-threatening infectious disease caused by Mycobacterium tuberculosis (Mtb). Globally, TB is a major public health burden with an estimated 10.4 million new cases and 1.8 million deaths reported in 2015. Although TB ... Read more
Antiplasmodial neolignans from Trema orientalis : identification, synthesis and analogue generation.

Author: Pillay, Pamisha Date: 2011 Trema orientalis, a widely distributed evergreen tree with various medicinal properties including the treatment of malaria, was investigated as a potential source of new antimalarial lead compounds. Organic extracts of the young growing twigs ... Read more
The antiplasmodial, toxicity and pharmacokinetic properties of synthetic derivatives of the natural product Curcumin

Author: Okalebo, Faith Apolot Date: 2008 Includes bibliographical references. Read more
Antiprotozoal quinolines containing electrophilic moieties

Author: Ganto, Mlungiseleli Macdonald Date: 2004 Compounds containing the quinoline moiety have been the mainstay of antimalarial chemotherapy. However, the emergence of resistant strains of Plasmodium falciparum, the causative agent of malaria, has compromised the efficacy of these ... Read more
The application of the Multi-Component Reaction (MCR) strategy in the design and synthesis of new antiplasmodial and antimycobacterial agents

Author: Tukulula, Matshawandile Date: 2012 Malaria and tuberculosis are ancient diseases that continue to have a profound impact on mankind, 5 millennia after their first documentation. Malaria is endemic in more than 100 countries and about 50% of the world's population is at risk ... Read more
Approaches toward the enantioselective total synthesis of amarogentic

Author: Stevens, Anne Therese Date: 2001 Three different, but complementary strategies for the enantioselective synthesis of the secoiridoid core of amarogentin were evaluated. The first is based on the enantioselective desymmetrisation of meso-anhydrides using titanium TADDOLates. ... Read more
Bioactive chloroquine-based ligands and their gold complexes as potential novel antimalarial agents

Author: Watermeyer, Nicholas D Date: 2008 Chloroquine(CO)-derived 4-aminoquinolines have proven to be the most efficacious antimalarial drugs for both the treatment and prophylaxis of malaria. However, with the advent of drug resistance, their ability to treat the disease has been ... Read more
Chemical modification and pharmacological evaluation of the antimalarial natural product totarol

Author: Tacon, Claire Date: 2004 Includes bibliographical references. Read more
Chemogenomic approaches to drug design : docking-based virtual screening of nematode GPCRs for potential anthelmintic agents

Author: Masuka, Raban Wilfred Date: 2016 Among common problems affecting human health and veterinary medicines, helmintic infections are major. The pathogens affect 550-750 Million people worldwide, and affect childhood growth, pregnancies, and development of the intellect. Helminths ... Read more
Cloning, expression, purification and drug targeting of Plasmodium falciparum hypoxanthine guanine xanthine phosphoribosyltransferase (HGXPRT)

Author: Mbewe, Boniface Date: 2005 The research concerns sub-cloning the gene for HGXPRT from Plasmodium falciparum from a vector with a His-tag facility to one without, expression of the protein in E. coli, and purification. On an analytical scale (40 ml culture), a purification ... Read more
Computer-aided drug design and the biological evaluation of anti-cancer drugs

Author: Moorad, Razia Date: 2016 Computer-aided drug design has become a promising alternative to high-throughput screening by identifying potential hits in silico for in vitro evaluation. In this study a combination of ligand-based and structure-based virtual screening was ... Read more
CRIMALDDI: a co-ordinated, rational, and integrated effort to set logical priorities in anti-malarial drug discovery initiatives

Author: Boulton, Ian C ; Nwaka, Solomon ; Bathurst, Ian ; Lanzer, Michael ; Taramelli, Donatella ; Vial, Henri ; Doerig, Christian ; Chibale, Kelly ; Ward, Steve A Date: 2010 Despite increasing efforts and support for anti-malarial drug R&D, globally anti-malarial drug discovery and development remains largely uncoordinated and fragmented. The current window of opportunity for large scale funding of R&D into malaria ... Read more c b

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