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Showing 1 to 20 of 21 for “"Diversity oriented synthesis"”.
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Novel Photochemical Methodologies for Diversity Oriented Synthesis and Screening of Combinatorial Libraries
… a rapid increase in molecular complexity and diversity of the target scaffolds.</p> <p>To develop this novel methodology further and explore its generality, we directed our attention to the <em>Diels-Alder</em> adducts based on various chromones. We discovered that the <em>Diels-Alder</em> …
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A Diversity-Oriented Synthesis Approach to Functionalized Azaheterocycles using Cyclic Alpha-Halo Eneformamides
… a step-economical, cost-effective, scalable, and diversity-oriented synthesis approach to highly functionalized N-heterocycles through the intermediacy of α-halo enamines/enamides. The synthetic utility of the method is exemplified through the construction of quaternary cyclic propargylic and …
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I. Microwave-Influenced Diversity-Oriented Synthesis Of Biologically Relevant Small & Natural-Product-Like Molecules Via Multicomponent Coupling Reactions Ii. Synthetic Studies Toward The Total Synthesis Of The Repeating Tetrasaccharide Unit Of Zwitterionic Polysaccharide Ps A1
<p>Microwave-influenced diversity-oriented synthesis of biologically relevant small and natural-product-like molecules via multicomponent coupling reactions (MCCRs) have been investigated. Cheap, readily available starting materials in conjunction of microwave irradiation and employment of …
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Development of decarboxylative strategies towards the synthesis of fluorinated pharmacons
… Over the past few decades, fluoro(oxo) diversity has been accessed through oxidation state manipulations from the parent trifluoromethyl ketone, either by carbonyl reduction to give the trifluoroethanol or elimination to yield the difluoromethyl ketone. As such, synthetic chemists are …
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Cascade Annulation and Ring-Opening Reactions of Castagnoli-Cushman-Derived Allylic and Benzylic Thiomorpholinonates
… In this context, there is a growing need for the synthesis of sulfur-containing compounds in ways that are practical and cost-effective. One approach taken to achieve this goal is to employ diversity-oriented synthesis (DOS), which produces diverse complex molecules with similar core structures …
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To Design and Develop Semi-Saturated and Unsaturated Bicyclic Heterocycles for Fragment-Based Drug Discovery (FBDD) Campaigns
… the concept of reagent- and scaffold-based Diversity-Oriented Synthesis (DOS). This approach was undertaken on three privileged heterocycles, armed with two key functionalities for the bicyclic construction.<br/><br/>Chapter 3 discusses the application of diverse chemistry to construct …
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Synthesis and antibacterial evaluation of diverse small molecules
… First we extend organocatalysis to the field of diversity-oriented synthesis as a powerful means to generate molecular diversity and complexity in small molecule screening collections. We then study a family of potential biofilm inhibitors identified from a diverse screening collection, and for …
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Design and Synthesis of Antimycobacterial Agents
… more chemical space. After its extensive work in diversity-oriented synthesis, the Spring group has developed such a library. A collection of these compounds was evaluated in a phenotypic screen against *Mycobacterium abscessus*, producing four lead compounds, two of which, **13H8** and **14F8**, …
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Exploration of [2+2+2] cyclotrimerisation reactions of alkynes. A new methodology for the synthesis of small molecules to probe biological systems
… 2.120a) were successfully synthesised. Several cyclotrimerisations were attempted, with the best yields being obtained when diethylacetylene dicarboxylate 2.113a was used as the monoalkyne and Cp*Ru(cod)Cl as the catalyst in refluxing toluene. New heterocyclic compounds with …
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Exploration of [2+2+2] cyclotrimerisation reactions of alkynes. A new methodology for the synthesis of small molecules to probe biological systems
… 2.120a) were successfully synthesised. Several cyclotrimerisations were attempted, with the best yields being obtained when diethylacetylene dicarboxylate 2.113a was used as the monoalkyne and Cp*Ru(cod)Cl as the catalyst in refluxing toluene. New heterocyclic compounds with …
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OPENING NEW CHEMICAL SPACE IN DRUG DISCOVERY
… size is not decisive, the concept of library diversity, in terms of molecular structure and, more importantly, molecular function, has become crucial, making the efficient creation of functionally diverse small molecule collections a formidable challenge. When a specific biological target is …
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Synthesis of Partially Saturated Bicyclic Heteroaromatics: sp3-Enriched Scaffolds for Drug Discovery
… and have identified the lack of scaffold diversity and poor physicochemical properties in screening libraries as the leading causes. In an attempt to address this issue drug discovery strategies such as fragment-based drug discovery and lead-oriented synthesis have been developed which …
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Photoassisted Synthesis of Complex Polyheterocycles via Rational Design of Tailored Photoprecursors
… the most common source for drug leads, although diversity-oriented synthesis of unnatural complex molecules is gaining momentum. Our lab has been developing experimentally simple and straightforward approaches to complex molecular architectures via photochemical reactions involving a minimal …
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Strategies and Tactics for the Synthesis of Polycyclic Alkaloids
… elegant spectroscopic studies. Furthermore, the synthesis of these alkaloids has attracted the attention of the synthetic community, with several syntheses of the monomeric myrmicarins completed. Significant effort has been put forth toward the synthesis of the higher order structures, though no …
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Synthesis of a Diverse and Three-Dimensional Fragment Collection and The Development of a Novel Platform for Antibody Dual Functionalisation
… describes two projects. The first focuses on the synthesis of a library 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, …
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Fragment synthesis: pharmacophore and diversity oriented approaches
… the highly conserved ATP pocket. Analogues were synthesised of this fragment leading to a candidate with a better IC50. Additionally, computer modelling of the interface site suggested that a series of spirocyclic compounds would inhibit this protein. These were synthesised and tested in vitro. …
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Small Molecules and Their Conjugates with Peptides: Chemical Strategies to Tackle Resistant Bacteria
… target peptide–drug conjugate was successfully synthesised together with control compounds. Unfortunately, upon testing of the quorum sensing inhibitor controls, the desired anti-biofilm effects were not observed, which justified the lack of observed activity of the target conjugate. The other …
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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
… Within the two last decades, however, organic synthesis has been identified as a limiting factor in this regard owing to the historically uneven exploration of chemical space. Whilst fragment-based screening has proven a fruitful strategy for identifying novel bioactive small molecules, in a …
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Photoassisted Generation of Complex N, O, S Polyheterocycles
<p>This research set out to continue the exploration and diversification of excited state <em>o</em>-azaxylylene cycloadditions, utilizing both pre-photochemical and post-photochemical modifications.</p> <p>Pre-photochemical modifications came through the addition of heteroatoms, namely nitrogen …
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Advances in Heterocyclic Synthesis through Ring Expansions and Flow Chemistry
… pure analogs with spatial and functional diversity. This regiodivergent rearrangement, and the concept of using chiral reagents to effect regiocontrol in chiral natural products, adds value to late-stage natural product diversification programs. New Variations of the Schmidt Reaction: A …
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