Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 6 of 6 for “"Lead Optimisation"”.
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Studies within Fragment-Based Drug Discovery: Library Synthesis and Hit-to-Lead Optimisation
This thesis reports two projects aimed at addressing challenges within fragment-based drug discovery. The first project describes efforts towards utilising synthetic methodology to address deficiencies within fragment screening collections. This involved the development of a modular, robust and …
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Lead optimisation of dehydroemetine as an antimalarial option through drug repositioning and molecular modelling
Malaria is a life-threatening infectious disease caused by a parasitic protozoan belonging to the genus Plasmodium. Resistance has started to emerge for the currently recommended artemisinin combination therapies used to treat malaria. There is a great need for new anti-malarial drugs, but …
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The glyoxylate shunt as a target for antibacterial intervention in Pseudomonas aeruginosa
… and isothermal titration calorimetry. Hit to lead optimisation experiments of the hit compounds provided awareness of their potential for any future development as antibacterial agents. Although the compounds showed promising efficacies, in vitro drug metabolism and safety profiles, I also …
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Development of novel lysine targeting covalent inhibitors for Bruton’s tyrosine kinase and casein kinase 2 and synthesis of novel hybrid androgen receptor inhibitors
Cancer is the lead cause of death worldwide, accounting for 10 million deaths in 2020, or 1 in 6 deaths. While current therapies have significantly advanced in the last decade, they suffer from severe limitations such as resistance, lack of selectivity and life-threatening side effects. Herein we …
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Design and Synthesis of Antimycobacterial Agents
… *Mycobacterium abscessus*, producing four lead compounds, two of which, **13H8** and **14F8**, were chosen for further development. The first project in this dissertation aimed to improve the biological activity of the propiolic ester lead **13H8**, by building on existing knowledge of its …
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The development of small molecule inhibitors for fibrosis drug discovery
… non-lipid-like scaffolds.;Chapter 2 describes a lead-optimisation project targeting the RGD subfamily of the integrin receptors. The RGD integrins are recognised therapeutic targets for thrombosis, fibrosis, and cancer, amongst others. Current inhibitors are designed to mimic the tripeptide …