Digital Commons Network^™

Fabrication Of Electrospun Cellulose-Derived Nanofiber Membranes With Enhanced Stability Properties Of Arginase, Ceyhun Işik, Mustafa Teke

Turkish Journal of Chemistry

In this study, cellulose acetate (CA)/polyvinylpyrrolidone (PVP) and CA/PVP/Mn2+ nanofibers were produced by the electrospinning method, and these cellulose-derived membranes were used as carriers for arginase immobilization for the first time. The structural and morphological analysis of these cellulose-derived nanofibers were determined by attenuated total reflection-Fourier to transform infrared spectroscopy (FTIR), thermogravimetric analysis (TGA), X-ray diffraction (XRD), and scanning electron microscopy (SEM). After the immobilization process, it was observed that the thermal properties of the cellulose-derived nanofibers especially improved. The optimum temperature value for free arginase was found to be 35 °C, and this value was found to be 40 …

Comprehensive Evaluation Of Reseda Lutea L. (Wild Mignonette) And 7 Isolated Flavonol Glycosides: Determination Of Antioxidant Activity, Anti-Alzheimer, Antidiabetic And Cytotoxic Effects With In Vitro And In Silico Methods, Hati̇ce Kiziltaş

Turkish Journal of Chemistry

In this study, anticholinergic, antidiabetic, antioxidant and cytotoxic activities of Reseda lutea L. (R. lutea) were determined. Ethanol extracts of R. lutea (EERL) and water extract of R. lutea (WERL) were prepared for biochemical analysis. The antioxidant capacities of EERL and WERL were evaluated with 6 different methods. In addition, acetylcholinesterase (AChE), α-amylase and α-glycosidase enzyme inhibition by EERL were measured. According to the results, EERL exhibited high inhibition effects against α-amylase, α-glycosidase and AChE enzymes. The IC50 values of EERL against AChE (2.21 μg/mL), α-glycosidase (1.38 μg/mL), and α-amylase (0.11 μg/mL) were determined. Also, high cytotoxic effect of EERL …

A Simple Quantitative Method Using Tlc-Image Analysis To Determine Fructooligosaccharides (Fos) In Food Samples, Diana Beatriz Muñiz Márquez, Marco Antonio Mártinez Cervantes, Alain Martinez, Cristobal Aguilar, Pedro Agui̇lar Zarate, Jorge Enrique Wong Paz

Turkish Journal of Chemistry

The thin-layer chromatography technique (TLC) is a simple and inexpensive analysis commonly used to identify qualitatively the presence of carbohydrates in food samples such as mono- di and oligosaccharides particularly. TLC assay could be improved using image processing software for the semiquantitative determination of this type of compound. In the present work, TLC-image analysis with Silica Gel 60 TLC plates was used for the semiquantitative determination of 6 standards of carbohydrates (glucose, fructose, sucrose, 1-kestose, nystose, and fructofuranosylnystose). Subsequently, the areas of the spots of each compound were determined by digitizing in a conventional office scanner. Then, the segmentation of …

Utilization Of The Yamamoto Cyclotrimerization Reaction Towards The Synthesis Of Polycyclic Aromatic Compounds, Josh Ledrew

Theses and Dissertations (Comprehensive)

The overall theme of this research was to synthesize and study the structure-property relationships of novel polycyclic aromatic compounds capable of self-assembling to form liquid crystalline, and microporous structures, as well as molecules capable of molecular recognition. The unifying theme that connects this research is the utilization of the Yamamoto coupling reaction to access the desired polycyclic aromatic hydrocarbon targets. More specifically, the scope of the Yamamoto coupling reaction was explored for the synthesis of electron-deficient triphenylene derivatives that are otherwise difficult to prepare. The molecules prepared via the Yamamoto coupling reaction are expected to be further utilized as intermediates …

Influence Of Dissolved Organic Matter On Phosphate Interactions With Hydrous Ferric Oxides, Alaa Hasan Alsherbi

Theses and Dissertations (Comprehensive)

Phosphorus, iron oxides, and dissolved organic matter (DOM) are components present in all aquatic systems. Excess amounts of phosphorus in aquatic systems have the potential for toxic effects, in particular, contributing to eutrophication. Most of the previous studies performed looked at the surface complexation of inorganic phosphate anions (P) to mineral surfaces such as hydrous ferric oxide (HFO). However, the role of DOM on the interactions between HFO and P is unknown. This study investigates the influence of DOM on the surface complexation of P onto HFO surfaces. Moreover, this study looks at the possibility of cation bridging formation (Ca …

Review Of The Effects Of Asphalt Fume Emission (Vocs And Pahs) In Vitro, In Vivo And Human Studies, Omran Taqi, Nastassja Lewinski, Elham Fini, Eran Rozewski, Judith Klein-Seetharaman

UROP Posters

Review of the effects of Asphalt fume emission (VOCs and PAHs) in vitro, in vivo and human studies

Omran Taqi, Nastassja Lewinski¹

1) Department of Chemical and Life Science Engineering, Virginia Commonwealth University, Richmond, VA

Background

Asphalt is abundantly available around human operations including road paving and roofing sites. However, their emissions and fumes (specifically volatile organic compounds (VOCs) and polycyclic aromatic hydrocarbons (PAHs)) have been found to have adverse effects on health. Asphalt fumes are a class 2A carcinogen and exposure can increase the risk of lung cancer, asthma, headache, fatigue, and other cardiovascular diseases.

Methods

We used …

Novel Modes Of Synchronization And Extreme Events In Coupled Chemical Oscillators, David Allen Mersing

Graduate Theses, Dissertations, and Problem Reports (ETD)

We experimentally and computationally investigate dynamical behaviors in coupled chemical oscillators. These networks of chemical oscillators are created using catalytic Ru(bpy)₃²⁺ loaded cation exchange beads submerged in catalyst-free Belousov-Zhabotinsky (BZ) solutions. Various network structures are created by utilizing the photosensitive nature of the Ru(bpy) ₃²⁺ catalyst. The response of the oscillators due to light stimuli can be characterized by constructing a phase response curve (PRC). The PRC quantifies the excitatory and inhibitory responses of BZ oscillators due to applied light perturbations as a function of the oscillators' phase. Different initial concentrations of reactants in the BZ reaction …

Modeling, Fabrication, And Characterization Of Rf-Based Passive Wireless Sensors Composed Of Refractory Semiconducting Ceramics For High Temperature Applications, Kavin Sivaneri Varadharajan Idhaiam

Graduate Theses, Dissertations, and Problem Reports (ETD)

Real-time health monitoring of high temperature systems (>500^oC) in harsh environments is necessary to prevent catastrophic events caused by structural failures, varying pressure, and chemical reactions. Conventional solid-state temperature sensors such as resistance temperature detectors (RTDs) and thermocouples are restricted by their operating environments, sensor dimensions and often require external power sources for their operation. The current work presents the research and development of RF-based passive wireless sensing technology targeting high temperatures and harsh environmental conditions. Passive wireless devices are generally classified as near-field and far-field devices based on the interrogation distance. Near-field sensors are placed at …

Advancing Compound Detection And Identification Using Vibrating Sharp-Edge Spray Ionization, Anthony Paul Debastiani

Graduate Theses, Dissertations, and Problem Reports (ETD)

Advancing Compound Detection and Identification Using Vibrating Sharp-Edge Spray Ionization

Anthony Paul DeBastiani

‘Omics consists of various areas, including genomics, proteomics, lipidomics, and metabolomics with a goal of detection and identification of biomolecules present within each of these classes within an organism. Current omic analytical methods include the use of mass spectrometry (MS) coupled with various separation techniques, including liquid chromatography (LC), with the use of heated nebulization gas assisted electrospray ionization (HESI). Although the rapid progress in LC-MS platform development has lead to significant enhancements in omic studies, significant limitations in the detection and identification of low abundant species …

Multifunctional Organoboron Compounds And Boralactonate Salts, Randika T. Abeysinghe

Graduate Theses, Dissertations, and Problem Reports (ETD)

Organoboron compounds have gathered an important significance within the chemistry community on account of their wide range of applications in synthesis, catalysis, and medicinal chemistry. Even though the uses of boron compounds in drug discovery have been overlooked until the last several decades, boronic acid containing molecules have garnered increased attention due to the unique chemical properties of the boron center. Boron-functionalized ��-aryl propionic acid non-steroidal anti-inflammatory drug derivatives (bora-NSAIDs) can be accessed via copper(I)-catalyzed alkene boracarboxylation, using CO2 and B2pin2. To explore and expand the current synthetic and future medicinal chemistry applications of these bora-NSAIDs, methods …

Fluorescence Probes For Bioimaging: Synthesis, Photophysical Properties And Applications, Mehrun Nahar Uddin

Dissertations

Fluorescent probes are a vital tool in the study of cell imaging. There are many types of fluorescent probes ranging from inorganic and organic nanoparticles to organic molecules. When used judiciously, they can help provide essential information on cellular structure and function. The introduction of two-photon microscopy has expanded the need for new probes, in particular near-infrared (NIR) absorbing and emitting fluorescent probes. The photochemical and photophysical properties of NIR probes play a crucial role in their effectiveness in cell imaging by both conventional and two-photon excitation (2PE) microscopy. In this research, the synthesis, photophysical properties, and two-photon absorption (2PA) …

Bodipy Based Photodynamic Therapy And Potassium Probes, Xiangshan Liu

Dissertations

Boron dipyrromethene (BODIPY) has become more and more popular in photophysical and biological applications. BODIPY based fluorescence compounds have numerous advantage properties including low toxicity, high absorption extinction coefficients, high fluorescence quantum yields, sharp fluorescence emissions, and resistance to photobleaching. All the good properties lead to the wide applications of BODIPY based compounds. In this research, two different kinds of BODIPY are synthesized. Firstly, BDBrC containing carbazole and BODIPY core is synthesized. Cellular uptake research shows BDBrC can target on lysosome and singlet oxygen generation research result indicates that BDBrC can be used in photodynamic therapy. BDBrC also shows pH-sensitive …

Optical And Chemical Properties Of Fragaria Ananassa And Galena: Potential Photosensitizers In A Natural Dye-Sensitized Solar Cell, Ibukun S Akinsola, Aderemi B Alabi, Coppede Nicola

Tanzania Journal of Science

Dye is one of the major components for high power conversion efficiency in a dye-sensitized solar cell. There are challenges natural dyes encounter, especially with quick degradation of the dye molecules. This work considered mineral dye in comparison with plant dye to address the challenge of degradation of natural plant dyes. The optical properties and functional groups of the two natural dyes were studied in this work. The absorption spectra, the optical band gaps and the absorption coefficients of the dyes were reported and found to be suitable for use as photosensitizers in a dye-sensitized solar cell (DSSC), as they …

Physico-Chemical Properties Of Mechanically Extracted Banana Juice At Different Ripening Stages, Mathayo G Mathias, Lilian D Kaale, Oscar Kibazohi

Tanzania Journal of Science

This paper presents the findings of a study on physico-chemical properties of low viscosity banana juice from five banana cultivars: Pisang Awak (PSA) an ABB genome, Yangambi km5 (YKM5) an AAA genome and cultivars from AAA-EA genome, namely Mbilabile, Ndeshi and Mlonga. Low viscosity banana juice was extracted using improved mechanical method at five ripening stages. The physico-chemical properties significantly varied according to cultivars and ripening stages (p < 0.05). Yields, total soluble solids (TSS), titratable acidity (TA) and pH were in the range of 19.50–74.03%, 7.33–27.64 ºBrix, 0.37–0.76% malic acid equivalent and 4.09–4.70, respectively. Yields decreased in the order of Mbilabile > Ndeshi > Mlonga > YKM5 > PSA whereas the total soluble solids increased as follows Mlonga < Mbilabile < Ndeshi < YKM5 < PSA. Furthermore, ashes and mineral contents decreased with ripening stages whereas the low viscosity banana juice was rich in potassium and magnesium. Finally, the study recommends stage 5 of the ripeness as ideal for producing low viscosity banana juice. Keywords: Mechanical extraction, Banana cultivar, Ripening stage, Tannin, Banana juice.

Effects Of Ripeness And Blending Speed On The Extraction Yield And Physical Chemical Properties Of Low Viscosity Banana Juice, Oscar Kibazohi, Victor V Matabura

Tanzania Journal of Science

Low viscosity banana juice can be extracted from banana by blending and pressing the resulted semi-solid pulp to separate the juice. This juice extraction technology is relatively new and further studies to understand key parameters for juice release is vital for scaling up production and commercialisation. This study, investigated the influence of blending speed and ripeness stage on banana juice yield using two banana cultivars; the East African highland banana (Mbile) and the exotic banana (Pisang awak). Types of sugars and organic acids in the juice were analysed using an HPLC. Changes with ripening of fruit firmness, juice pH and …

Mathematical Characterization Of Biological Control Of Cassava Pests Model, Yidiat O. Aderinto, Faith O. Ibiwoye, Michael O. Oke, Folashade M. Jimoh

Tanzania Journal of Science

Pests are major constraints to the effective growth and development of every crop through their damage, and can be controlled effectively by the use of their natural enemies which is referred to as the biological pest control. In this study, the biological control model of cassava pests through optimal control theory was presented in order to minimize the population of the pests and stabilize the natural enemies population so as not to affect the crop negatively. A mathematical model was formulated via the Lotka-Volterra model, and the model was characterized. The optimality system was established, the equilibrium point with its …

Self-Assembly Of Black Cumin Oil-Based Nanoemulsion On Various Surfactants: A Molecular Dynamics Study, Aulia Fikri Hidayat, Taufik Muhammad Fakih

Makara Journal of Science

Black cumin is commonly used as traditional medicine due to its wide range of pharmacological potential. Black cumin oil (BCO) was often prepared as nanoemulsion to improve its solubility, stability, and bioavailability. This study was conducted to investigate the molecular behavior as well as structural evolution of BCO-surfactant systems during self-assembly micellization using molecular dynamics (MD) simulations. Several BCO constituents and variations of surfactants were employed to model BCO-surfactant systems. 50 ns of MD simulations were performed to elucidate their evolution of structures and physicochemical properties during formation. Results showed that BCO-tween20 and BCO-lecithin were able to form spherical-shaped micelles …

Exploring The Relationships Among Stoichiometric Coefficients, Number Of Transferred Electrons, Mean Oxidation Number Of Carbons, And Oxidative Ratio In Organic Combustion Reactions, Pong Kau Yuen, Cheng Man Diana Lau

Faculty Publications

Combustion reactions, stoichiometry, and redox reactions are some of the basic contents in chemistry curriculum. Although the counting of transferred electrons is critical in redox reactions, assigning mean oxidation number of organic carbons (ONc) is not always easy. Even though the relationship between the oxidative ratio (OR) and ONc is known, the relationship between the number of transferred electrons (Te−) and OR has not been thoroughly studied. The H-atom method has already been developed to balance and deduct organic combustion reactions. It can be used further to help establish the relationships among the stoichiometric coefficients (SC), the number of transferred …

Nitrogen-Sulfur Co-Doped Porous Carbon Preparation And Its Application In Lithium-Sulfur Batteries, Gui-Xiang Zhao, Wail Hafiz Zaki Ahmed, Fu-Liang Zhu

Journal of Electrochemistry

In recent years, lithium-sulfur (Li-S) batteries have been considered as a promising candidate for the next generation of energy storage system due to their ultrahigh theoretical capacity (1675 mAh·g^-1) and energy density (2600 Wh·kg^-1). However, the practical application of Li-S batteries is seriously limited by their insulating nature of sulfur, the shuttle effect of polysulfides (LiPSs), and volume expansion during charging and discharging. To overcome those disadvantages, one of the commonly methods is to infiltrate sulfur into porous conductive carbon framework, such as porous carbon, hollow carbon spheres, graphene, carbon nanotubes and some composites of the …

Photoelectrochemical Sensing Based On Zr-Mofs For Homocysteine Detection, Wen-Xia Dong, Guang-Ming Wen, Bin Liu, Zhong-Ping Li

Journal of Electrochemistry

Due to the independent form of the light source and detection system, photoelectrochemical (PEC) sensor has the advantages of low background, high sensitivity and simple operation. So far, PEC systems have been widely used in the fields including the actual detection of metal ions, biological antibodies or antigens in environmental pollutants. When the photosensitive material is irradiated by a light source with an energy being equal to or greater than its band gap, electrons (e^-) transition occurs from the valence band to the conduction band, leaving a hole (h⁺), at the same time, the generated electron-hole …

A Nanoscale Shape-Discovery Framework Supporting Systematic Investigations Of Shape-Dependent Biological Effects And Immunomodulation, Wei Zhang, Hender Lopez, Luca Boselli, Paolo Bigini, André Perez-Potti, Zengchun Xie, Valentina Castagnola, Qi Cai, Camila P. Silveira, Joao M. De Araujo, Laura Talamini, Nicolò Panini, Giuseppe Ristagno, Martina B. Violatto, Stéphanie Devineau, Marco P. Monopoli, Mario Salmona, Valeria A. Giannone, Sandra Lara, Kenneth A. Dawson, Yan Yan

Articles

Since it is now possible to make, in a controlled fashion, an almost unlimited variety of nanostructure shapes, it is of increasing interest to understand the forms of biological control that nanoscale shape allows. However, a priori rational investigation of such a vast universe of shapes appears to present intractable fundamental and practical challenges. This has limited the useful systematic investigation of their biological interactions and the development of innovative nanoscale shape-dependent therapies. Here, we introduce a concept of biologically relevant inductive nanoscale shape discovery and evaluation that is ideally suited to, and will ultimately become, a vehicle for machine …

High-Resolution Cryo-Electron Microscopy Structure Of Photosystem Ii From The Mesophilic Cyanobacterium, Synechocystis Sp. Pcc 6803, Christopher J. Gisriel, Jimin Wang, Jinchan Liu, David A. Flesher, Krystle M. Reiss, Hao-Li Huang, Ke R. Yang, William H. Armstrong, M. R. Gunner, Victor S. Batista, Richard J. Debus, Gary W. Brudvig

Publications and Research

Photosystem II (PSII) enables global-scale, light-driven water oxidation. Genetic manipulation of PSII from the mesophilic cyanobacterium Synechocystis sp. PCC 6803 has provided insights into the mechanism of water oxidation; however, the lack of a highresolution structure of oxygen-evolving PSII from this organism has limited the interpretation of biophysical data to models based on structures of thermophilic cyanobacterial PSII. Here, we report the cryo-electron microscopy structure of PSII from Synechocystis sp. PCC 6803 at 1.93-Å resolution. A number of differences are observed relative to thermophilic PSII structures, including the following: the extrinsic subunit PsbQ is maintained, the C terminus of the …

Exploration Of Carbon-Oxygen And Carbon-Nitrogen Bond Formation Utilizing Trichloroacetimidates And Investigations Of New Reactions Mediated By Oxoammonium Salts, Rowan Meador

Dissertations - ALL

Mono-O-alkylated 1,1′-bi-2-naphthols (BINOLs) are often used as the source of chirality for catalysts or ligand systems that are employed in asymmetric organic transformations. However, these BINOLs can be hard to synthesize. The O-alkylation of BINOL can be accomplished with primary and secondary alkyl halides or under Mitsunobu conditions, the yields of these alkylations with tertiary halides or alcohols are very low. A new protocol was developed utilizing trichloroacetamide electrophiles to install bulky groups onto one of the phenolic oxygens. Trichloroacetimidates are also shown to be useful reactions for the synthesis of esters. These reagents proceeded through a symbiotic activation pathway. …

The Phase Behavior Of Ubqln Proteins And Implications For Protein Quality Control, Yiran Yang

Dissertations - ALL

The ubiquitin-proteasome system (UPS) and autophagy are essential pathways for maintaining protein quality control (PQC) in cells. Misfolded proteins and large aggregates are cleared by UPS and autophagy signaled by ubiquitin (Ub) or polyubiquitin (polyUb) chains. Shuttle proteins facilitate cargo transporting by interacting with both ubiquitin and degradation machineries. Previously, our lab discovered that the shuttle protein Ubiquilin-2 (UBQLN2) is recruited to stress granules in cells and undergoes liquid-liquid phase separation (LLPS) in vitro. LLPS is a biophysical process by which proteins separate themselves from the surrounding aqueous solution by forming protein-rich droplets. The overarching goals of this work are …

Formation Of Pyrroloindolines And Alkylation Of N-Heterocycles With Trichloroacetimidates And Synthesis Of Quinoline Based Small Molecule Inhibitors Of Ghrelin O-Acyltransferase (Goat), Bhaskar Joshi

Dissertations - ALL

Pyrroloindolines and related systems are present in a large number of complex natural products. These core structures have generated considerable synthetic interest, as many of the compounds possess challenging, elaborate structures and interesting biological properties. Recently we have focused on using trichloroacetimidates for the synthesis of these fascinating molecules. Trichloroacetimidates can be used an electrophilic source of an alkyl group to form the pyrroloindoline directly from tryptamine derivatives. In this manner trichloroacetimidates provide a flexible solution to accessing highly functionalized pyrroloindoline core structures, needing only a catalytic amount of a Lewis acid to effect the requisite transformations.

Isatin (1H-indol-2,3-dione) based …

Leveraging The 1,3-Azadiene-Anhydride Reaction For The Synthesis Of Functionalized Piperidines Bearing Up To Five Contiguous Stereocenters, Jorge Garcia, Jane Eichwald, Jayme Zesiger, Timothy K. Beng

Student Published Works

A modular and scalable strategy, which remodels 3-methylglutaric anhydride to 2-oxopiperidines bearing at least three contiguous stereocenters is described. The approach relies on the chemoselective and stereocontrolled annulation of 1,3-azadienes with the anhydride component. The resulting acid-tethered allylic 2-oxopiperidines are then engaged in several selective fragment growth processes, including catalytic denitrative alkenylation, halolactonization, and Vilsmeier–Haack functionalization.

Mansouramycins E–G, Cytotoxic Isoquinolinequinones From Marine Streptomycetes, Mohamed Shaaban, Khaled A. Shaaban, Gerhard Kelter, Heinz Herbert Fiebig, Hartmut Laatsch

Center for Pharmaceutical Research and Innovation Faculty Publications

Chemical investigation of the ethyl acetate extract from the marine-derived Streptomyces sp. isolate B1848 resulted in three new isoquinolinequinone derivatives, the mansouramycins E–G (1a–3a), in addition to the previously reported mansouramycins A (5) and D (6). Their structures were elucidated by computer-assisted interpretation of 1D and 2D NMR spectra, high-resolution mass spectrometry, and by comparison with related compounds. Cytotoxicity profiling of the mansouramycins in a panel of up to 36 tumor cell lines indicated a significant cytotoxicity and good tumor selectivity for mansouramycin F (2a), while the activity profile of E ( …

The Immobilization Of Ticagrelor On Implant Materials And Corrosion And Biofouling Inhibition By Novel Layered Polymer Thin Films For Marine Application, Tell Lovelace

Electronic Theses and Dissertations

Percutaneous coronary interventions are a widely used cardiovascular surgery which is typically accompanied by the insertion of a vascular stent. After the procedure patients are put on dual anti-platelet therapy (DAPT) to prevent stent thrombosis, a common complication to this procedure in which platelets aggregate in the blood vessel on the inserted stent. Systemic deactivation of platelets in patients via oral DAPT results in patients becoming bleeding risks in future medical procedures, necessitating the development of a localized delivery system for anti-platelet medications from the surface of the stent. A novel anti-thrombogenic vascular stent coating has been prepared by covalent …

Functional Structure Of Biomacromolecules In Plant Biomass Using Solid-State Nmr And Dynamic Nuclear Polarization, Alex Kipchirchir Kirui

LSU Doctoral Dissertations

This dissertation summarizes the recent findings on complex biomacromolecules in cell wall of plants and fungi which perform important roles in cell recognition, structural build up, and energy storage. Because of the technical difficulty in characterizing these biomacromolecules, which are often polymorphic and disordered in structure, the functional structure of these biomacromolecules remains elusive. In this dissertation, I present two solid-state nuclear magnetic resonance (ssNMR) and dynamic nuclear polarization (DNP) studies of carbohydrate-rich biosystems: the energy-rich plant biomass and disease-relevant, pathogenic fungi.

First, we have investigated the secondary cell wall of plant biomass which is a carbohydrate-rich biosystem using solid …

Design And Synthesis Of Small Molecular Probes For Cns And Kidney Disorders, Swagat H. Sharma

Theses & Dissertations

The G protein regulated inwardly rectifying potassium channels (GIRK) are a family of inwardly rectifying potassium channels and are key effectors in signaling pathways. GIRK 1/2 channel subunit, predominantly found in the brain, is involved pathophysiology of various neurological disorders including, but not limited to, epilepsy, anxiety, Parkinson's, pain, reward, and addiction. Previously, our laboratory had identified a series of urea containing molecules as GIRK1/2 preferring activators. Unfortunately, the urea series suffers from significant PK liabilities (solubility, brain penetration and high clearance). The chapter 1 of the dissertation describes our efforts in developing three new series of activators with improved …