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Showing 1 to 13 of 13 for “"library synthesis"”.
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Selective Chemical Reactions for Nucleic Acid Sequencing and DNA-Encoded Library Synthesis
Part One: The ability to map methylation sites in the human genome and epitranscriptome has transformed our understanding of how these modifications govern and influence a host of cellular processes and human diseases. Amongst the most widely studied methylations is N6-methyladenine, known as 6mA …
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Studies within Fragment-Based Drug Discovery: Library Synthesis and Hit-to-Lead Optimisation
… spirocyclic scaffolds. Importantly, this library was structurally diverse, comprising three (a total of six in collaboration) pharmacophore-like heterocycles and carbocycles. Moreover, numerous three-dimensional exit vectors were incorporated within each core spirocycle, and the ability of …
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Chemical biology of matrix metalloproteases
… of each individual MMP, it is imperative to synthesise small molecule/probes which can selectively target a particular MMP instead of those which exhibit broad spectrum inhibition against the whole family. In this project, we aim at profiling MMPs substrate specificities in a high-throughput …
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Use of Structure-And Ligand-Based Drug Design Tools for the Discovery of Small Molecule Inhibitors of Cysteine Proteases for the Treatment of Malaria and Sars Infection
… A combined data mining and combinatorial library synthesis approach was performed to discover analogs of virtual screening hits and establish the structure-activity relationships (SAR). However, the resulting SAR of the identified hits was unusually steep in some cases and could not be …
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The preparation of heterocycles by [2+2+2] cyclization and inverse electron demand Dels-Alder reactions of arynes with 1,2,4-triazines
… that were utilized further in a small molecule library synthesis. Using this methodology, sixteen new annulated pyridazines were prepared. Inverse electron demand Diels-Alder (IEDDA) reactions of arynes and 1,2,4-triazines were also investigated for the generation of isoquinoline core …
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Discovery of macrocyclic inhibitors of challenging protein-protein interactions
… methods have enabled the purification-free synthesis of chemically diverse macrocycles and the generation of de novo libraries for high-throughput screening and identification of functional macrocycle inhibitors. However, bottlenecks existed in these approaches which limited peptide …
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Automating reaction development: hardware and software for fully-automated high-fidelity navigation of high-dimensional chemical reaction space
… to capture reacted droplets and thereby enable library synthesis. The software and hardware developed in this thesis can together enable accelerated process development that minimizes delays between the discovery of transformative medicines and their delivery to patients in need.
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The Use of Natural Product Substrates for the Synthesis of Libraries of Biologically Active, New Chemical Entities
… griseus ETH A7796, is an ideal candidate for the synthesis of new antimicrobial drugs. This secondary metabolite is composed of two units of (+)-nonactic acid 49 and two units of (-)-nonactic acid 50. Whereas nonactin does not possess a synthetically useful chemical `handle', the nonactic acid …
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The Use of Natural Product Substrates for the Synthesis of Libraries of Biologically Active, New Chemical Entities
… griseus ETH A7796, is an ideal candidate for the synthesis of new antimicrobial drugs. This secondary metabolite is composed of two units of (+)-nonactic acid 49 and two units of (-)-nonactic acid 50. Whereas nonactin does not possess a synthetically useful chemical `handle', the nonactic acid …
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CHEMICAL SYNTHESIS AND BIOLOGICAL EVALUATION OF CHONDROITIN SULFATE DISACCHARIDES
Glycosaminoglycans (GAGs) are heterogeneous polysaccharides comprising of repeating uronic acid and amino sugar disaccharide units. Recently, it was shown that the sulfate groups present in chondroitin sulfate GAGs (CS) encode important functional information for the regulation of physiological …
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High-throughput protein engineering tools for efficient exploration and quantitative mapping of protein fitness landscapes
… the process of error-prone DNA translesion synthesis. Furthermore, I characterize the mutational spectrum and frequency of the YeastIT-generated libraries and compare them with the existing methods (error-prone PCR, PACE, MutaT7, eMutaT7, OrthoRep, TRIDENT, EvolVR), demonstrating comparable …
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Diverse Applications of Flow Technology in Discovery Chemistry
… throughput, safety, and convenience of organic synthesis. The last two chapters describe the use of microfluidic technology as a platform for rapid reaction discovery. Working with researchers at Abbott Laboratories, a droplet-based library method was developed. This approach allowed for the …