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 9 of 9 for “"semisynthesis"”.
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Semisynthesis of amphotericin B and its derivatives via iterative cross-coupling
… effective endgame strategy, we proceeded with a semisynthesis of AmB. Degradation of the natural product allowed access to an excellent model for an advanced intermediate in the proposed total synthesis. The iterative cross-coupling strategy then proved effective in converting this intermediate …
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Electronic tuning of site selectivity and semisynthesis of C2'-deoxyamphotericin B
The small molecule Amphotericin B (AmB) is a natural product that is utilized in the treatment of systemic fungal infections. AmB is effective against a broad spectrum of fungi, and resistance to this potent antifungal agent is rare. However, the use of AmB is limited due to its high toxicity. All …
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Caged phosphopeptides and phosphoproteins : probes to dissect the role of phosphorylation in complex signaling pathways
… to these techniques, the synthesis and semisynthesis of probes that enable researchers to observe the downstream effects of kinase-mediated phosphorylation in "real time" are presented in this thesis. The release of a physiologically-relevant concentration of a phosphopeptide with …
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Structural Studies on the Regulation of Sporulation in Bacillus and Antibiotic Sulfation
… synthetic chemistry, and protein semisynthesis, we have: (1) Solved the X-ray crystal structure of a Geobacillus stearothermophilus sporulation histidine kinase in complex with an inhibitor of the kinase reaction (Chapter 2). (2) Developed an approach using the methods of protein …
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Anticancer and antibiotic leads from marine organis
… and its algal diet Bryopsis pennata. Our semisynthesis approach was aimed to improve the efficacy or prolong the half-life resulted in 15 KF analogues. These analogues included eight elongation products with nonpolar amino acid residues, four analogues with modified amino group at the Orn …
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Characterization of the Central Cavity of a Potassium Channel: Helix Dipoles, Conformational Plasticity and Inhibition
… the role of helix dipoles in KcsA using protein semisynthesis in order to modify the backbone of KcsA and reduce the dipoles of the implicated helix termini. The modified protein was studied by both X-ray crystallography and electrophysiology, demonstrating that the pore helix dipoles may play an …
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Stress relief: Exercising Lewis acid catalysis for donor-acceptor cyclopropane ring-opening annulations, a basis for new reaction methodologies
… effects require further derivatization because semisynthesis is not sufficient to refine adverse pharmacokinetics. For some active molecules, isolation results in poor yields. In addition to small quantity isolation, many natural products, reflecting the immense complexity of biology itself, …
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Semisynthetic Development of Blasticidin S as an Antibiotic Lead and Development of Other Anti-Infectives
Recent decades have seen a decline in discovery of new classes of antibiotics. This lack of new antibiotics is punctuated by the spread of antibiotic resistance and has placed society in a global health crisis. To mitigate the potentially devastating effects of widespread antibiotic resistance, new …