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.
Results
Showing 1 to 10 of 10 for “"screening collections"”.
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Discovery of high quality molecular leads and screening collections for CNS drug targets
… synthesis of diverse and highly lead-like screening libraries is presented specifically with the objective of providing improved molecular starting points for CNS drug discovery.
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Discovery and biological evaluation of ferroptocide
… traits different from those in most screening collections, and as such are a rich source for biological discovery. Herein, we subject the complexity-to-diversity library of compounds to an anticancer phenotypic screen. This effort resulted in identification of an active class of …
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Chemical diversification of the natural products quinine, abietic acid and pleuromutilin by ring distortion
… found in approved drugs but lacking in other screening collections used in drug discovery. The chapters herein emphasize the utility of ring distortion reactions for modifying complex molecules and assert the potential of ring distortion as strategy for the synthesis of complex and diverse …
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Studies within Fragment-Based Drug Discovery: Library Synthesis and Hit-to-Lead Optimisation
… to address deficiencies within fragment screening collections. This involved the development of a modular, robust and scalable route to access α,α-disubstituted amino ester building blocks, which in turn were derivatised to allow the rapid assembly of five (a total of eight in …
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Synthesis and antibacterial evaluation of diverse small molecules
… of new scaffolds, limitations of target-based screening, and poor target validation each contribute to the current bottleneck in the antibiotic pipeline. In turn, I argue that the development and application of chemical probes is a more fruitful way to make progress towards new antibiotics with …
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OPENING NEW CHEMICAL SPACE IN DRUG DISCOVERY
… of macromolecules comprising living systems. Screening collections or libraries of small molecules is the most common way to identify new chemical modulators of protein function and constitutes one of the bases of medicinal chemistry. While a general consensus has emerged that library size is …
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Synthesis of Partially Saturated Bicyclic Heteroaromatics: sp3-Enriched Scaffolds for Drug Discovery
… have been afflicted with low hit rates during screening campaigns and high levels of candidate attrition during clinical trials. Subsequent studies have looked to explore the underlying factors to these challenges and have identified the lack of scaffold diversity and poor physicochemical …
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Synthesis of a Diverse and Three-Dimensional Fragment Collection and The Development of a Novel Platform for Antibody Dual Functionalisation
… of small molecules suitable for fragment-based screening. Over the past two decades, fragment-based drug discovery (FBDD) has emerged as a powerful strategy for early-stage drug discovery. However, despite its many successes, FBDD often suffers from the lack of synthetic tractability, …
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Synthesis of Structurally Diverse N-Substituted Quaternary Carbon Containing Small Molecules and Their Application as Novel Starting Points for Drug Discovery
… of chemical space. Whilst fragment-based screening has proven a fruitful strategy for identifying novel bioactive small molecules, in a similar vein to high-throughput screening approaches, obstacles within this paradigm have been recognised. This relates to a lack of fragment novelty, the …
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Advances in high-throughput screening: better compounds, novel targets, enhanced sensors
High throughput screening (HTS) is the dominant force in modern drug discovery. Through the evaluation of large structure collections, novel drug leads can be rapidly assessed for modulation of medicinally-relevant biological targets. This occurs through the interplay of three intrinsically linked …