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 “"Bioisostere"”.
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Development of biotin protein ligase inhibitors from Staphylococcus aureus as new antibiotics
… studies on the utility of a 1,2,3-triazole as a bioisostere of the phosphoroanhydride linker of biotinyl-5’-AMP 1.03 are also discussed. Chapter two further examines 1,2,3-triazole analogues of lead SaBPL bisubstrate inhibitors 1.22 and 1.23. Specific chemical modifications were carried out at …
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Exploring the synthesis and functionalisation of methano[10]annulene
… molecules. One method to achieve this is through bioisosteres. Bioisosteres are “groups or molecules which have chemical and physical similarities producing broadly similar biological effects”. For this thesis, the proposed bioisostere of naphthalene, methano[10]annulene was investigated. …
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Synthesis of phosphorus/sulfur-based antivirals
… functional group as a suitable bioisostere. An in-depth review of the conversion of alkyl halides to alcohols is also outlined in this chapter. The preparation of the antiviral agent adefovir is detailed in Chapter 2. The derivatisation of adefovir via the corresponding …
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Design, Synthesis and Evaluation of Organic and Metal Based Antimicrobial Agents
… acid, (1) the well-known carboxylic acid bioisostere, the (1H)-tetrazole, and (2) a hydroxamic acid. Both the (1H)-tetrazole and hydroxamic acid derivatives were found to exhibit bacteriostatic activity similar to that of their carboxylic acid analogues. Finally, the synthesis of a family …
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Prediction of Metabolic Stability and Bioavailability with Bioisosteric Replacements
Drug development is a long and expensive process. Potential drug candidates can fail clinical trials due to numerous issues, including metabolic stability and efficacy issues, wasting years of research effort and resource. This thesis detailed the development of in silico methods to predict the …
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1,3-Disubstituted-tetrahydro-β-carbolines: A New Method for Stereochemical Assignment and Synthesis of Potential Antimalarial Agents
Malaria is a serious mosquito-borne disease affecting the majority of Earth's southern hemisphere. While consistent efforts to curb malaria spread throughout 20th and early 21st century were largely successful, the recent rise in resistance to antimalarial treatments resulted in an increasing …