Chemistry Commons^™

Crystal Structure And Hirshfeld Surface Analysis Of 1,2-Ethylene-Bis (Para-Methyl Pyridinium) Dichromate As A New Selective And Mild Agent In Oxidation Of Alcohols, Mostafa Gholizadeh, Mehrdad Pourayoubi, Mohammad Reza Houssiendokht, Hadi Amiri Rudbari, Masoumeh Farimaneh, Anahid Saneei, Giuseppe Bruno

Turkish Journal of Chemistry

1,2-Ethylene-bis(para-methyl pyridinium) dichromate, (C$_{14}$H$_{18}$N$_{2})$[Cr$_{2}$O$_{7}$], is used as a new oxidizing agent in conversion of some alcohols to their corresponding carbonyl compounds in CH$_{3}$CN solvent and also under solvent-free conditions. In both procedures, high conversion percentages are observed. However, a much shorter reaction time is achieved in solvent-free conditions. For allylic alcohols, the C=C bond is not oxidized and the examined saturated alcohol in this work (i.e. cyclo-hexanol) remains intact, which illustrates the mild nature of reagent used. The structure of the reagent is investigated by single-crystal X-ray diffraction analysis. The C--H$\cdots$O and O$\cdots \pi$ interactions are the most important features …

An Efficient Protocol For The Synthesis Of Brominated Norbornene, Norbornadiene, And Benzonorbornadiene, Selçuk Eşsi̇z

Turkish Journal of Chemistry

An efficient protocol for the synthesis of 2-bromonorbornene, 2-bromonorbornadiene, 2-bromoben- zonorbornadiene, 2,3-dibromonorbornene, 2,3-dibromonorbornadiene, and 2,3-dibromobenzonorbornadiene in good yields has been developed. 1,2-Dibromotetrachloroethane is used as the brominating agent for these reactions. The results are discussed in comparison with alternative methods in the literature.

Design, Synthesis, And Evaluation Of The Antimycobacterial Activity Of 3-Mercapto-1,2,4-Triazole--Pyrrole Hybrids, Gheorghe Roman, Andra-Cristina Bostanaru, Valentin Nastasa, Mihai Mares

Turkish Journal of Chemistry

A series of 3-mercapto-1,2,4-triazole--pyrrole hybrids was designed as antimycobacterial agents by employing 5-(4-(1$H$-pyrrol-1-yl)phenyl)-4$H$-1,2,4-triazole-3-thiol as the scaffold onto which several types of moieties were introduced in the triazole ring at N-4 and N-2 and as substituents of the mercapto function. The aforementioned moieties are an allyl or a phenyl moiety at N-4; an aminomethyl group at N-2; or methyl, substituted benzyl, ethoxycarbonylmethyl, or substituted phenacyl at sulfur. Investigation of the compounds in the resulting library as growth inhibitors of Mycobacterium smegmatis showed that their minimum inhibitory concentration was higher than 64 mg/L.

Synthesis And Bioactivity Of Sulfide Derivatives Containing 1,3,4-Oxadiazole And Pyridine, Gang Yu, Shunhong Chen, Feng He, Dexia Luo, Yu Zhang, Jian Wu

Turkish Journal of Chemistry

A series of novel sulfide derivatives containing 1,3,4-oxadiazole and pyridine were synthesized, characterized, and tested for their antibacterial activity against tobacco bacterial wilt and rice bacterial blight and for insecticidal activity toward diamondback moth. The results showed that some compounds had good insecticidal and bactericidal activity, e.g., the activities of compounds 6e and 6g-6j toward tobacco bacterial wilt were much better than those of commercial thiodiazole-copper, and some of the synthesized compounds possessed good insecticidal activity against Plutella xylostella. Compounds 6d, 6h, 6j, 6l, 6p, 6r, and 6p displayed over 93% activity at 500 mg L$^{-1}$.

Characterization And Purification Of 1,2,4-Triazole-Containing Phthalocyanines Synthesized By Microwave Method And Structure Elucidation By Spectroscopic Techniques, Asi̇ye Nas, Ümi̇t Demi̇rbaş, Nurhan Gümrükçüoğlu, Hali̇t Kanteki̇n

Turkish Journal of Chemistry

The complexes of peripherally tetra-substituted metal-free (8), lead(II) 9), and zinc(II) (10) phthalocyanine derivatives were synthesized for the first time in this work. The structures of these new complex compounds have been elucidated using many spectral methods such as electronic absorption, FT-IR, $^{1}$H NMR, $^{13}$C NMR, elemental analysis, and mass spectra. The thermogravimetric behavior of compounds 8-10 was determined by thermogravimetric analysis method in addition to these spectral methods.

Synthesis Of N-Heterocyclic Molecules And Their Applicability Towards Ion Sensing: Polymeric Chemosensors, Aikohi M. Ugboya

College of Graduate Studies: Theses & Dissertations

Critical to biological and environmental processes are anions because often times their relative concentration in our body can be an indicator of one’s well-being. Therefore, highly sensitive and cost-efficient methods for ions recognition is necessary for human health. In recent times, polymeric chemosensors have become a vital tool for sensing ions because of its higher sensitivity and good mechanical properties compared to their monomeric counterparts. These sensors are designed to produce a measurable response in the presence of a targeted ion such as an electrochemical or optical signal. The unique structure and the photophysical properties of the 1,2,3-triazole core coupled …

Computational Study Of Lawesson’S Reagent Mediated Fluorenone Dimerization Forming 9,9’-Bifluorenylidene, Andrew Jourdan Eckelmann

Graduate Theses/Dissertations

The ambition of this work is to start a path to the a priori rational design of high yield production for electron acceptors with finely tuned band gaps, from the comfort of an armchair. To this end, organic photovoltaics offer a cheap and sustainable means of manufacture using readily available materials and avoids the toxicity of some of the heavy metals used in first and second-generation solar cells such as cadmium. The microwave assisted Lawesson’s reagent mediated one-pot one-step solventless synthesis takes less than 3 minutes and results in an 84% yield of 9,9’-bifluorenylidene from two equivalents of fluorenone. While …

Synthesis Of Oxadiazoles And Examination Of Steric Effects In A Cyclodehydration Reaction, Norah Young

Undergraduate Honors Thesis Projects

The objective of this project is to develop a general substrate scope by testing various steric and electronic effects. This is pursued by developing triphenylphosphine dibromide (PPh3Br2) as an effective cyclodehydration reagent for use with a variety of hydrazides and sterically and electronically different benzoic acids. The two phases of the experiment include assessing yield through a cyclodehydration reaction and comparing that yield to the steric hindrance and molecular structure recorded in different databases. The cyclodehydration reaction uses ortho-substituted benzoic acid with store bought PPh3Br2, and compares those yields to the use of a two step-one pot reaction in place …

Synthesis, Biological Evaluation, And In Silico Study Of Some Unique Multifunctional 1,2,4-Triazole Acetamides, Almas Sattar, Aziz Ur Rehman, Muhammad Athar Abbasi, Sabahat Zahra Saddiqui, Shahid Rasool, Hira Khalid, Muhammad Arif Lodhi, Farman Ali Khan

Turkish Journal of Chemistry

The imperative demand for antibacterial agents and enzyme inhibitors prompted us to synthesize some new compounds, 6a-6k, bearing multifunctional moieties. The target acetamides were derived from 4-phenyl-5-(1-tosylpiperidin-4-yl)-4$H$-1,2,4-triazole-3-thiol (3). The structural analysis was carried out using modern spectroscopic techniques including IR, NMR, and EIMS spectral analysis. The antibacterial activity was screened against five bacterial strains including three gram-negative and two gram-positive ones. Enzyme inhibition was carried out against lipoxygenase enzyme and results were supported by in silico study. The synthesized compounds were proved to be potent antibacterial agents and enzyme inhibitors.

$S$-Substituted Derivatives Of 1,2,4-Triazol-3-Thiol As New Drug Candidates For Type Ii Diabetes, Aziz Ur Rehman, Khadija Nafeesa, Muhammad Athar Abbasi, Sabahat Zahra Saddiqui, Shahid Rasool, Syed Adnan Ali Shah, Muhammad Ashraf, Muhammad Arif Lodhi, Farman Ali Khan, Bakht Jahan

Turkish Journal of Chemistry

The therapeutic applications of 1,2,4-triazoles motivated us to synthesize some new derivatives. Two series of $S$-substituted derivatives (8a-8j, 12a-12i) of 5-$\{$1-[(4-chlorophenyl)sulfonyl]-3-piperidinyl$\}$-4-phenyl-4$H$-1,2,4-triazol-3-thiol (6) have been synthesized and evaluated for their biological potential. Using 4-chlorobenzene sulfonyl chloride (1) and ethyl piperidine-3-carboxylate (2), ethyl 1-[(4-chlorophenyl)sulfonyl]piperidine-3-carboxylate (3) was synthesized and converted into 3,4,5-trisubstituted 1,2,4-triazole (6) through formation of the corresponding carbohydrazide (4) and hydrazinecarbothioamide (5). Compound 6 was transformed into 8a-8j by alkyl halides (7a-7j) and into 12a-12i by $N$-aralkyl/aryl-2-bromoacetamides (11a-11i) in an aprotic solvent. The electrophiles, 11a-11i, were synthesized by gearing up $N$-substituted aralkyl/aryl amines (10a-10i) with 2-bromoacetyl bromide (9) under dynamic pH …

A Rapid And Sensitive Spectrofluorometric Method For The Determination Of Au(Iii) Based On Fluorescence Quenching Of A 1,3,5-Triphenyl-2-Pyrazoline, Aysel Başoğlu, Ümmühan Ocak, Seda Fandakli, Nuretti̇n Yayli

Turkish Journal of Chemistry

A simple, rapid, sensitive, and low-cost spectrofluorometric method was developed for the determination of Au(III) using 5-(2,3-dimethoxyphenyl)-3-(4-methoxyphenyl)-1-phenyl-4,5-dihydro-1H-pyrazole (L) in ethanol/water. The method is based on the change in the fluorescence intensity at 464 nm after excitation at 355 nm as a result of the reaction between the ligand and Au(III). The fluorescent emission of ligand at 464 nm decreased with the increasing of Au(III) concentration. The ligand concentration, pH effect, response time, and effect of foreign ions were determined. From the results of fluorescence titration experiments, it was found that the ligand (1 $\times $ 10$^{-7}$ M) was selective and …

Investigation Of The Hydrogen Bond Donating Ability Of 1,8-Naphthalenediol By Nmr Spectroscopy And Its Use As A Hydrogen Bonding Catalyst, Yunus Emre Türkmen

Turkish Journal of Chemistry

The hydrogen bond donating ability of 1,8-naphthalenediol was investigated via a series of $^{1}$H, $^{13}$C, and $^{31}$P NMR experiments. Complexation studies using triphenylphosphine oxide and cyclohexanone as hydrogen bond acceptors revealed that 1,8-naphthalenediol is a more effective hydrogen bond donor compared to 1-naphthol and 8-methoxy-1-naphthol. Afterwards, its effectiveness as a hydrogen bonding catalyst was demonstrated in the Friedel-Crafts-type addition reaction of indole to trans-$\beta $-nitrostyrene.

Synthesis Of Acetamide Derivatives Of 1,2,4-Triazole Bearing Azinane And Their Binding Interactions With Bovine Serum Albumin Using Spectroscopic Techniques, Javed Iqbal, Aziz Ur Rehman, Muhammad Athar Abbasi, Sabahat Zahra Siddiqui, Hira Khalid, Sabina Jhaumeer Laulloo, Nausheen Joondan, Aniisah Banu Taupass, Shahid Rasool, Syed Adnan Ali Shah

Turkish Journal of Chemistry

A new series of acetamide derivatives containing 1,2,4-triazole and azinane moieties has been synthesized and characterized using $^{1}$H NMR, $^{13}$C NMR, IR, and EI-MS spectroscopic analysis. The intermediate triazole was synthesized through a sequential synthesis of carboxylate and carbohydrazide. The bovine serum albumin (BSA) binding of the newly synthesized 1,2,4-triazole derivatives was evaluated along with thermodynamics, site-selective binding, and synchronous study. The results obtained by BSA binding as well as thermodynamic studies justify that all the compounds show spontaneous interaction with BSA and could be effectively distributed and eliminated from the body. Therefore, the triazole-based analogs might be a useful …

Biological Study On Novel Coumarinyl 1,3,4-Oxadiazoles, Maja Molnar, Ana Amic, Valentina Pavic, Tihomir Kovac, Marija Kovac, Elizabeta Has-Schön

Turkish Journal of Chemistry

Coumarinyl 1,3,4-oxadiazoles were synthesized from Schiff bases and acetic anhydride. All compounds were characterized by melting points and their structures confirmed by mass and $^{1}$H and $^{13}$C NMR spectrometry. These novel coumarinyl derivatives were subjected to antibacterial, antifungal, anta atoxigenic, and antioxidant activity. Their activity varied depending on their structure, where 2-(3-acetyl-5-(((4-methyl-2-oxo-2H-chromen-7-yl)oxy)methyl)- 2,3-dihydro-1,3,4-oxadiazol-2-yl)-1,4-phenylene diacetate showed significant antioxidant and antibacterial activity on B. subtilis. 4-(3-Acetyl-5-(((4-methyl-2-oxo-2H-chromen-7-yl)oxy)methyl)-2,3-dihydro-1,3,4-oxadiazol-2-yl)-1,2-phenylene diacetate was found to possess excellent antifungal and antia atoxigenic activity.

Synthesis And Characterizations Of Novel Thiazolyl-Thiadiazole Derivatives As Telomerase Activators, İsmai̇l Kayaği̇l, Ayşe Gül Mutlu, Ülkü Bayhan, İnanç Yilmaz, Şeref Demi̇rayak

Turkish Journal of Chemistry

Pyridine-3/4-thiocarboxamide derivatives were used as starting materials for the synthesis of the target compounds. The pyridine-3/4-thiocarboxamide derivatives were reacted with ethyl 2-chloroacetoacetate in ethanol to give the thiazole derivatives (1, 2). The two ethyl thiazole-carboxylate derivatives (1, 2) thus obtained were treated with sodium hydroxide solution and ethanol and converted to carboxylic acids (3, 4). The carboxylic acid derivatives (3, 4) were reacted with thiosemicarbazide in phosphoroxy trichloride and aminothiadiazole rings (5, 6) were formed. Thus, two thiazolyl-thiadiazole amine derivatives (5, 6) were obtained. These two derivatives (5, 6) were converted into two chloroacetamidothiadiazole derivatives (7, 8) by reaction with …

Synthesis And Evaluation Of Novel 1,3,4-Thiadiazole--Fluoroquinolone Hybrids As Antibacterial, Antituberculosis, And Anticancer Agents, Asli Demi̇rci̇, Kaan Gökçe Karayel, Esra Tatar, Si̇nem Öktem Okullu, Ni̇han Ünübol, Paki̇ze Nesli̇han Taşli, Zühtü Tanil Kocagöz, Fi̇kretti̇n Şahi̇n, İlkay Küçükgüzel

Turkish Journal of Chemistry

A series of 5-substituted-1,3,4-thiadiazole-based fluoroquinolone derivatives were designed as potential antibacterial and anticancer agents using a molecular hybridization approach. The target compounds 16-25 were synthesized by reacting the corresponding $N$-(5-substituted-1,3,4-thiadiazol-2-yl)-2-chloroacetamides with ciprofloxacin or norfloxacin. The purity and identity of the synthesized compounds were determined by the use of chromatographic and spectral techniques (NMR, IR, MS, etc.) besides elemental analysis. Antibacterial, antituberculosis, and anticancer activity of the target compounds were evaluated against selected strains and cancer cell lines. Compound 20 was appreciated as the most active agent representing antibacterial activity against Escherichia coli and Staphylococcus aureus with MIC values of 4 …

Synthesis And Antimicrobial And Antioxidant Activities Of Hybrid Molecules Containing Benzotriazole And 1,2,4-Triazole, Mahesh Chand, Reena Kaushik, Subhash Chand Jain

Turkish Journal of Chemistry

Eleven novel 1,2,4-triazolylbenzotriazoles have been prepared using 1-(hydrazinylcarbonylmethyl)-1$H$-benzot- riazole (3) as a potent intermediate. Compound 3, however, was obtained from benzotriazole in two steps. All synthesized compounds were characterized by detailed spectral studies like IR, $^{1}$H NMR, $^{13}$C NMR, and mass spectrometry. All synthesized compounds were evaluated for their \textit{in vitro} antimicrobial activity against seven strains of bacteria and four strains of fungi. Compounds 13, 17, 19, 20, and 21}were found to possess antibacterial activity comparable to that of ciprofloxacin against a Klebsiella pneumoniae strain. Except for compounds2 and 13, all compounds showed good antifungal activity against an Aspergillus niger …

The Synthesis Of New 3,4-(Bisaryl)-1,8-Naphthalimide And 2,3-(Bisaryl)-7$H$-Benzimidazo[2,1-A]Benzo[D]Isoquinolin-7-One Compounds And An Investigation Of Their Photochromic Properties, Ersi̇n Orhan, Mahmut Köse, Tolga Yazan

Turkish Journal of Chemistry

Three new photochromic compounds, 3-(2,5-dimethyl-3-thienyl)-4-(2-phenyl-5-methyl-4-thiazolyl)-1,8-napht- halimide (1-O), 2,3-bis(2-phenyl-5-methyl-4-thiazolyl)-7$H$-benzimidazo[2,1-a]benzo[de]isoquinolin-7-one (2-O), and 2,5-dimethyl-3-thienyl)-7$H$-benzimidazo[2,1-a]benzo[de]isoquinolin-7-one (3-O), were synthesized and their photochromic properties were studied. Compound 1-O was synthesized by two consecutive Suzuki coupling reactions using 2,5-dimethylthiophene-3-boronic acid and 5-methyl-2-phenylthiazole-4-boronic acid. Photochromic compounds 2-O and 3-O were prepared by multistep reactions starting with 3-iodo-4-bromo-1,8-naphthalic anhydride and 2,5-dimethylthiophene-3-boronic acid or 2-phenyl-5-methylthiazole-4-boronic acid. All photochromic compounds showed a color change from colorless (or light yellow) to blue-green, purple, or orange colors (depending on the nature of the structures) on exposure to UV light at 365 nm in ethyl acetate solutions. The colored solutions can be reversed to …

Formation Of Highly Functionalized Indole Through Carbon-Carbon Bond Cleavage, Ryan A. S. Pike

Chemistry and Chemical Biology ETDs

Indoles are one of the most abundant heterocycles found in nature and have a wide range of functions. There are a wide variety of indole synthesis methods known both in synthetic chemistry and through biosynthesis. Many of the known indole synthesis routes use a benzene derivative or cyclized ring structure derivative as a starting material. Here, we describe a novel synthetic method utilizing 1, 3-diketones and fumaronitrile with a catalytic amount of base to form a highly functionalized indole as our product. We have isolated and characterized 12 functionalized indoles.

Antifungal Potential Of Copper(Ii), Manganese(Ii) And Silver(I) 1,10-Phenanthroline Chelates Against Multidrug-Resistant Fungal Species Forming The Candida Haemulonii Complex: Impact On The Planktonic And Biofilm Lifestyles, Rafael M. Gandra, Pauraic Mc Carron, Mariana F. Fernandes, Lívia S. Ramos, Thaís P. Mello, Ana Carolina Aor, Marta H. Branquinha, Malachy Mccann, Michael Devereux, André L. S. Santos

Articles

Candida haemulonii, Candida haemulonii var. vulnera and Candida duobushaemulonii, which form the C. haemulonii complex, are emerging etiologic agents of fungal infections known to be resistant to the most commonly used antifungals. The well-established anti-Candida potential ofmetal complexes containing 1,10-phenanthroline (phen) ligands encouraged us to evaluate different copper(II), manganese(II), and silver(I) phen chelates for their ability to inhibit planktonic growth and biofilm of C. haemulonii species complex. Two novel coordination complexes, {[Cu(3,6,9-tdda)(phen)2].3H2O.EtOH}n and [Ag2(3,6,9-tdda)(phen)4].EtOH (3,6,9-tddaH2 = 3,6,9-trioxaundecanedioic acid), were synthesized in a similar fashion to the other, previously documented, sixteen copper(II), manganese(II), and silver(I) chelates employed herein. Three isolates of …

Synthesis And In Vitro Anticancer Evaluation Of 1,4-Phenylene-Bis-Pyrimidine-2-Amine Derivatives, Meli̇ha Burcu Gürdere, Erdoğan Kamo, Ayşe Şahi̇n Yağlioğlu, Yakup Budak, Mustafa Ceylan

Turkish Journal of Chemistry

A series of 1,4-phenylene-bis-chalcones 3a-3h were synthesized by the reaction of terephthalaldehyde with substituted arylketones in this study. The novel 1,4-phenylene-bis-pyrimidine-2-amine derivatives 5a-5h were obtained by the addition of guanidine hydrochloride to 1,4-phenylene-bis-chalcone 3a-3h in ethanolic KOH under reflux conditions. The structure of the compounds was explained by means of IR, $^{1}$H NMR, $^{13}$C NMR, and elemental analyses. The anticancer activities of 3a-3h and 5a-5h were investigated against rat brain tumor cells and human uterus carcinoma in vitro$.$ Activity tests were performed as dose-dependent assays at eight concentrations. The positive control was 5-fluorouracil (5-FU). Compounds 3c and 3d were examined …

Efficient Multicomponent Synthesis Of 1,2,3-Triazoles Catalyzed By Cu(Ii) Supported On Pei@Fe$_{3}$O$_{4}$ Mnps In A Water/Peg$_{300}$ System, Zeinab Hassanpour, Aziz Maleki, Morteza Hosseini, Lena Gorgannezhad, Vajihe Nejadshafiee, Ali Ramazani, Ismaeil Haririan, Abbas Shafiee, Mehdi Khoobi

Turkish Journal of Chemistry

A highly dispersible and magnetically recoverable Cu-PEI@Fe$_{3}$O$_{4}$ MNPs catalyst was prepared and successfully applied in one-pot three-component coupling of terminal alkynes, sodium azide, and alkyl bromides/chlorides in water to give 1,4-disubstituted 1,2,3-triazoles with good to excellent yields. The catalyst was fully characterized with FT-IR, TGA, TEM, SEM, VSM, EDX, cyclic voltammetry, and ICP-AES spectroscopic techniques. Furthermore, the catalyst was easily recycled by an external magnet and successfully reused six times in the reaction without significant loss of its catalytic activity and copper leaching. The large-scale reaction was also carried out in the absence of any base and reducing agent even …

Approaches Toward Novel 1,2,3-Triazole Sensors For The Detection Of Anions And Heavy Metal Cations, Richard D. Govan

College of Graduate Studies: Theses & Dissertations

Cations and anions play pivotal roles in biological and physiological processes, however an imbalance in concentration of any ion can be detrimental. Therefore, research into the selective recognition of anions and heavy metal cations has acquired much attention. One approach involves the use of chemosensors. Upon interaction with targeted analytes, chemosensors produce a distinct response, in some cases a fluorescent or colorimetric signal. The 1,2,3-triazole unit has much potential as a chemical sensor due to its unique photophysical properties. The specificity, selectivity, and signaling mechanism of triazole sensors can be tuned with conjugation in the motif and choice and placement …

A Rapid, Eco-Friendly, And Reliable Microplate Method For Determination Of Cr(Vi), Alejandro Coreño Alonso, Gustavo Cruz Jimenez, Leticia Lopez Martinez, Georgina Elena Reyna Lopez, Francisco Javier Acevedo Aguilar

Turkish Journal of Chemistry

In the present work, the reaction of Cr(VI) with 1,5-diphenylcarbazide in microplates (enzyme-linked immunosorbent assay microtiter plate) and a subsequent determination in a plate reader at 540 nm were performed. The final volume utilized for each determination was 200 $\mu $L, and the cost and waste were reduced for hexavalent chromium [Cr(VI)] quantification. The use of microplates allowed for the analysis of a large number of samples, reducing analysis time. No statistically significant differences were observed between the results obtained in the analysis of Cr(VI) in real samples by the conventional procedure and by the proposed methodology in this work …

Nanocomposite Copper Metal As An Efficient Heterogeneous Catalyst In Click Synthesis Of 1,2,3-Triazoles In Aqueous Media, Vajihe Nejadshafiee, Hossein Naeimi

Turkish Journal of Chemistry

Copper/periodic mesoporous organosilica (Cu/PMO) nanocomposites provided a highly active, reusable, globular, solid-phase catalyst for click chemistry. The reaction proceeds by mixing organohalides, sodium azide, alkyne, and the catalyst in an aqueous medium to afford the desired products. The cost efficiency and recyclability of the catalyst up to six runs without appreciable loss of activity and high yields of products make this procedure greener.

The Antibacterial Activity Of Metal Complexes Containing 1, 10-Phenanthroline: Potential As Alternatire Therapeutics In The Era Of Antibiotic Resistance, Livia Viganon, Orla L. Howe, Pauraic Mccarron, Malachy Mccann, Michael Devereux

Articles

The “antibiotic era”, characterized by the overuse and misuse of antibiotics, over the last half-century has culminated in the present critical “era of resistance”. The treatment of bacterial infections is challenging because of a decline in the current arsenal of useful antibiotics and the slow rate of new drug development. The discovery of a new gene (mcr-1) in 2015, which enables bacteria to be highly resistant to polymyxins (such as colistin), the last line of antibiotic defence left, heralds a new level of concern as this gene is susceptible to horizontal gene transfer, with alarming potential to be spread between …

Electrogenerated Chemiluminescence Of Luminophores And Enhancement With Melatonin, Sarah Michelle Roughton

Graduate Theses/Dissertations

The photoluminescent (PL), electrochemical, and electrogenerated chemiluminescent (ECL) properties of 1,5-I-Aedans (N-(iodoacetylaminotheyl)-1-naphthylamine-5-sulfonic acid) in aqueous buffered (KH2PO4) and 50:50 (v/v) acetonitrile:KH2PO4 solutions were obtained. Tri-n-propylamine (TPrA) was used as the oxidative-reductive coreactant. The PL efficiencies (em) were 1.83 in KH2PO4 and 4.81 in mixed solvent compared to Ru(bpy)32+ standard solutions (em = 1.0). 1,5-I-Aedans displayed quasi-reversible oxidative electrochemistry in aqueous solutions and irreversible to quasi-reversible oxidation in mixed solvent. ECL efficiencies (ecl) were obtained by comparison to a Ru(bpy)32+/TPrA (bpy = 2,2'-bipyridine) standard (ecl = 1) and were higher in KH2PO4 (ecl = 6.8 x 10-4) than in the mixed …

Synthesis, Structure-Activity Relationship Study, And Mode Of Action Study Of 1,4-Naphthoquinone Based Anticancer And Antimicrobial Agents, Jaya P. Shrestha

All Graduate Theses and Dissertations, Spring 1920 to Summer 2023

The first three projects involve the synthesis and the mode of action study of 1,4-naphthoquinone based anticancer agents. These anticancer agents are highly potent against a wide range of cancer cell lines. These compounds showed ~8-fold selectivity towards the lung cancer cell line than the normal cell line. We also studied the mode of action and observed that generation of reactive oxygen species is the primary mode of action.

The final project involves the synthesis of multi-cationic antimicrobial agents. These compounds are active against both bacteria and fungi. These compounds are very easy to synthesize and can be scaled up …

Synthetic Methods For The Preparation Of 1,3-S,O-Esters, Α-Phosphonovinyl Triflates, And Α-Alkynylphosphonates, David P. Kercher

Master of Science in Chemical Sciences Theses

A broad and systematic study was conducted on synthetic methods to efficiently synthesize 1,3-S,O-esters, α-phosphonovinyl triflates, and α-alkynylphosphonates under mild reaction conditions. The master’s thesis is composed of two projects; the first project is titled “Synthesis of 1,3-S,O-Esters” and the second project is titled “Synthesis of α-Phosphonovinyl Triflates and α-Alkynylphosphonates.” The first project outlines a synthetic route to conveniently prepare novel α-functionalized 1,3-S,O-esters via an acid-promoted hydrolysis of α-functionalized α-oxoketene dimethylthioacetals. The second project, unrelated to the first project, primarily focuses on extensive synthetic methodology developed to prepare …

Chiral Boro-Phosphates In Asymmetric Catalysis: 1,4-Reduction Of Enones And Reductive Aldol, Susana Sorina Lopez

USF Tampa Graduate Theses and Dissertations

The biological activity of the pharmaceutical drugs often depends on how it fits with a receptor making stereochemistry a key component. Selective reactions can limit or avoid the mixture of enantiomers obtained. One such reaction is the selective reduction of a carbon-carbon double bond in the presence of a carbonyl. Although efficient, current asymmetric synthesis methods have limitations such as harsh reaction conditions, the high costs of chiral catalysts and the toxicity of the metal-based catalysts. Catalysts derived from small organic molecules have become an attractive alternative which have been explored more rigorously in recent years. Using a BINOL-derived boro-phosphate …