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Chemistry

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Structure Activity Relationship

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The Use Of Synthetic Mixture Based Libraries To Identify Hit Compounds For Eskape Pathogens, Leishmaniasis, And Inhibitors Of Palmitoylation, Marcello Giulianotti Apr 2016

The Use Of Synthetic Mixture Based Libraries To Identify Hit Compounds For Eskape Pathogens, Leishmaniasis, And Inhibitors Of Palmitoylation, Marcello Giulianotti

USF Tampa Graduate Theses and Dissertations

The goal of this work is to demonstrate the utility of using systematically formatted mixture based libraries as part of the drug discovery processes. While there are a number of different valid approaches for identifying hit and tool compounds, systematically formatted mixture based libraries, such as those described in this study, offer the ability to develop a significant amount of structure activity relationship data from the testing of very few samples. In support of this claim a review of recent developments in the area of systematically formatted mixture based libraries as well as three case studies are presented. The three …


An Investigation Into The Antifungal Activities Of N-Thiolated Beta- Lactams Against Selected Candida Species, Marci Culbreath May 2006

An Investigation Into The Antifungal Activities Of N-Thiolated Beta- Lactams Against Selected Candida Species, Marci Culbreath

USF Tampa Graduate Theses and Dissertations

β-lactam antibiotics have long been a reliable course of treatment for bacterial infections. However, with recent increases in resistance and rising populations of immunocompromised patients new β-lactams have been synthesized and tested. The Turos laboratory has recently discovered novel β-lactams that have a mode of action distinct from penicillin and other β-lactam antibiotics as cell lysis is not observed. In the current investigations, these compounds are shown to also have antifungal properties. The rising incidence and prevalence of invasive fungal infections has become an increasing concern. The most common fungal pathogens involved in these infections are species in the genus …