Chemistry Commons^™

Synthesis And Characterization Of Antimony Cyanoximates For Microbiological Studies, Seth Adu Amankrah

MSU Graduate Theses

Antibiotic-resistant pathogenic microorganisms (such as MRSA and alike) represent a real and significant threat to the health and wellbeing of the general population. The search for new compounds of non-antibiotic nature that act as antimicrobial agents is an important task with obvious practical applications in the biomedical field. Metal-based coordination and organometallic compounds that demonstrate antimicrobial activity was found to exhibit a completely different mode of action compared to antibiotics. That suggests the absence of the mechanism of developing tolerance to these types of compounds at least for 30 - 40 years. Thus, there are numerous organotin (IV), silver (I), …

Studies Of Polyacrylate Based Nanoparticle Emulsions, Faeez Mahzamani

USF Tampa Graduate Theses and Dissertations

Self-stabilizing polyacrylate nanoparticle emulsions were previously investigated in the Turos laboratory, and provided a new model for delivering antibiotics via encapsulation or covalent binding of the desired bioactive compound within the polymer nanoparticles. The method used the in water, free radical emulsion polymerization of butyl acrylate/styrene mixture to form the polymer chain stabilized with a surfactant. Current research in this dissertation further explores the versatility of related nanoparticle emulsion systems. Chapter 2 provides an overview of the loading of certain therapeutic drugs, such as 5-aminosalicylic acid and derivatives thereof, for the treatment of irritable bowel syndrome. Chapter 3 explores homo-polymer …

Part – I: Development Of A Two-Step Regiospecific Synthetic Route For Multigram Scale Synthesis Of Β-Carboline Analogs For Studies In Primates As Anti-Alcohol Agents,Part – Ii: Design And Synthesis Of Novel Antimicrobials For The Treatment Of Drug Resistant Bacterial Infections Part – Iii: A Novel Synthetic Method For The Synthesis Of The Key Quinine Metabolite (3s)-3-Hydroxyquinine, Veera Venkata Naga Phani Babu Tiruveedhula

Theses and Dissertations

PART – I

Development of a Two-Step Regiospecifc Synthetic Route for Multigram-Scale Synthesis of β-Carboline Analogs for Studies in Primates as Anti-Alcohol Agents

β-Carboline and their derivatives are important structural motifs in synthetic organic and medicinal chemistry because of their novel biological activity, especially in regard to the reduction of alcohol self-administration [binge drinking (BD)], a major problem increasing day by day in modern society. This anti-alcohol effect is proposed to be due to the activity of ligands at the benzodiazepine site of the GABAA receptor in the central nervous system acting as antagonists at the α1 subunit. The past …

Metabolomics Approaches To Decipher The Antibacterial Mechanisms Of Yerba Mate (Ilex Paraguariensis) Against Staphylococcus Aureus And Salmonella Enterica Serovar Typhimurium, Caroline Sue Rempe

Doctoral Dissertations

The increasing prevalence of drug-resistant pathogens is an urgent problem that requires novel methods of bacterial control. Plant extracts inhibit bacterial pathogens and could contain antibacterial compounds with novel mechanisms of action. Yerba mate, a common South American beverage made from Ilex paraguariensis, has antibiotic activity against a broad range of bacterial pathogens. In this work, an attempt was first made to characterize the antibacterial source of an aqueous yerba mate extract by generating a series of extract fractions, collecting GC-MS and antibacterial activity profiles, and then ranking the hundreds of compounds by their presence in fractions with high antibacterial …

Synthesis, And Prediction Of Molecular Properties And Antimicrobial Activity Of Some Acylhydrazones Derived From $N$-(Arylsulfonyl)Methionine, Esra Tatar, Sevi̇l Şenkardeş, Hasan Erdi̇nç Selli̇tepe, Şükri̇ye Güni̇z Küçükgüzel, Şengül Alpay Karaoğlu, Ari̇f Bozdeveci̇, Erik De Clercq, Christophe Pannecouque, Tai̇bi̇ Ben Hadda, İlkay Küçükgüzel

Turkish Journal of Chemistry

A series of 38 new acylhydrazones [3-40], derived from (2$S)$-4-(methylsulfanyl)-2-[[(4-methylphenyl)sulfonyl] amino]butanoic acid hydrazide [2], were synthesized and evaluated for their anti-HIV and antimicrobial activity with the further aim to develop acylhydrazones carrying an amino acid side chain. All tested compounds possess stronger activity against gram (+) bacteria. Compound 23 was found active against methicillin-resistant Staphylococcus aureus (MRSA) with a MIC value of 3.9 $\mu $g/mL. The MIC value of compound 30 against Enterococcus faecalis, Listeria monocytogenes, and Bacillus cereus was 8 $\mu $g/mL. A computational study for prediction of ADME and drug-like properties (solubility, drug-likeness, and drug score) as well …

The Genesis And Emergence Of Community-Associated Methicillin-Resistant Staphylococcus Aureus (Ca-Mrsa): An Example Of Evolution In Action?, Alan L. Gillen, Jason Conrad, Michael Cargill

Faculty Publications and Presentations

Staphylococcus aureus infections are a common cause of disease, particularly in colonized persons. Recently, a series of published articles have reported that community-acquired methicillin-resistant S. aureus (CA-MRSA) strains are evolving and increasingly becoming prevalent in households while health care acquired MRSA (HA-MRSA) is declining in the USA. The changing superbugs have often been used as an example of evolution in action. Although MRSA infections have become increasingly reported in the community, population-based studies of students preparing for the health professions having S. aureus and MRSA colonization are lacking. During the 2014–2015 school year 544 students were tested for MRSA carriage …

N-Acyl Ciprofloxacins: Synthesis, Antibacterial Activity And Effects On Molecular Loading Of Poly(Vinyl Benzoate) Nanoparticles, Ryan Cormier

USF Tampa Graduate Theses and Dissertations

Bacterial infections are becoming progressively more difficult to treat due to antibiotic resistance and the decreasing rate at which new antibiotics are brought to market. The Turos laboratory has attempted to tackle this problem for the last 15 years with the discovery of N-thiolated β-lactams leading to the design of polyacrylate nanoparticles to deliver these and other drugs. Chapter 1 discusses many reported instances of utilizing different types of polymeric nanoparticles to deliver antibiotics. Poly(lactic-co-glycolic acid) (PLGA), poly(alkyl cyanoacrylate) (PACA), poly(styrene-co-butylacrylate), and chitosan are the main polymers used to make nanoparticles. Chapter 2 describes the synthesis, antibacterial activity, and mechanism …

Drug Discovery From Floridian Mangrove Endophytes, Jeremy Beau

USF Tampa Graduate Theses and Dissertations

A significant challenge of the 21st century is the growing health threat stemming from drug-resistant infectious diseases. There is an undeniable need to discover new, safe and effective drugs with novel mechanisms of action to combat this threat. A study of drugs currently on the market showed that natural products account for approximately 75% of new anti-infective drugs, either as new agents or analogs based upon their structure. Unfortunately, major pharmaceutical companies have cut back tremendously in natural products research in part due to the frustrating obstacle of frequent rediscovery of compounds. Fungi in particular are difficult to work with …

Synthesis And Anti-Mrsa Activity Of Hydrophilic C3-Acylated N-Thiolated Β-Lactams And N-Acyl Ciprofloxacin-N-Thiolated Β-Lactam Hybrids, Biplob Bhattacharya

USF Tampa Graduate Theses and Dissertations

The Turos laboratory has been working with N-thiolated β-lactams for years trying to understand the mode of action and structural features it needs to have biological activity. Over the years new data has shown promising inhibitory activity against various microbes.

In this dissertation, a review of the vast amount of work carried out on N-thiolated β-lactams in Turos laboratory has been done and their novelty, in terms of structure and mechanism has been discussed. A complete outline of our work in the discovery and ongoing development of these compounds, starting from our initial, unexpected finding of antimicrobial activity for one …

Synthesis And Antimicrobial Activities Of S,S'-Heterosubstituted Disulfides, Praveen Ramaraju

USF Tampa Graduate Theses and Dissertations

Antibiotic resistance is a particularly critical health concern and has increased dramatically over the past two decades. For over a decade the Turos laboratory has been designing small molecules to target pathogenic microbes such as Staphylococcus aureus and the resistant variants like methicillin-resistant Staphylococcus aureus (MRSA). Previously, N-thiolated Β-lactams, N-thiolated 2-oxazolidinones and aromatic disulfides that were synthesized in Dr. Turos' lab have shown strong activity against these bacteria. The present work describes the synthesis and antimicrobial activities of a related structural class called S,S'-heterosubstituted disulfides. For ages, sulfur (elemental) has been used as an antibacterial for controlling infestation and bacterial …