Doctor of Philosophy, Miami University, 2010, Chemistry and Biochemistry

EPR spectroscopic techniques provide powerful methods to study the structural dynamics, topology, and distance measurements of peptides/proteins in membranes and solutions. Cholesterol containing bicelles were studied using X- and Q-band EPR spectroscopy. Cholestane-bicelle EPR spectra were better aligned at Q-band than X-band yielding hyperfine splittings closer to the rigid limit values and resulting in higher order parameters. Increasing cholesterol content in bicelles resulted in lower membrane fluidity and a higher phase transition temperature. Three site-specifically labeled PLB samples were studied using aligned EPR spectroscopy. The transmembrane helical tilt of WT-PLB was determined to be (13 ± 4)°. EPR line-shape analysis revealed highly restricted motion in transmembrane domain of PLB. Both the loop and the cytoplasmic domain were found to have two distinct conformational states, which agrees with previous studies in the literature. The major T-conformer interacts with membrane with slower dynamics, and the minor R-conformer has faster dynamics with minimal membrane interaction. The distance and orientation between two TOAC nitroxides on AChR M2δ were determined using aligned EPR spectroscopy coupled with rigorous spectral simulations. An internitroxide distance of 14.6 A was obtained from a dual-labeled peptide, matching closely with modeling results (14.5 A). The orientational angles of the two nitroxides were also determined from simulations, which compared favorably to the molecular studies. DEER spectroscopy was used to measure the distance between two monomers in a GCN4-LZ dimer using TOAC spin labels. We observed a 13-fold increase in sensitivity by collecting DEER spectra at Q-band when compared to X-band. This increased sensitivity represented a 169-fold decrease in data collection time and revealed a greatly improved frequency spectrum with higher quality distance data. Three GCN4-LZ peptides and one Aβ-40 peptide were synthesized, purified, an (open full item for complete abstract)

Honors Theses, Ohio Dominican University, 2021, Honors Theses

Leishmaniasis is a neglected tropical disease which affects millions of people every year across 6 continents. Current antileishmanial drugs have become less effective due to resistance, have a high toxicity, and are too expensive for many lower socioeconomic countries. New drug candidates can be explored and synthesized by natural drug synthesis and high throughput screening (HTS). This paper aimed to explore both methods in search of novel antileishmanial compounds. For the natural product approach, the ABC ring of berberine will be optimized to improve its antileishmanial properties. For the HTS approach, a piperazine based small molecule has been synthesized and will be evaluated for its antileishmanial properties.

PHD, Kent State University, 2018, College of Arts and Sciences / Department of Chemistry and Biochemistry

Iron plays an irreplaceable role in the cell and is found in numerous proteins that use iron as a biological catalyst to perform cell maintenance, growth and cell division. In tumor cells, as well as in normal cellular proliferation, there is a dependence on iron and its availability. With the recognized need to create and test new anti-tumor agents, utilizing the fact that cancer cells disproportionately tend to take up greater amounts of iron than do normal cells, this allows a pathway to be exploited using other metals such as gallium that can interfere in iron metabolism. Gallium ion possesses unique medicinal properties due to its resemblance to iron and is a known mimic of this essential metal. Therefore showing promise for treatment of a variety of diseases and disorders, particularly cancer and bacterial infection due to its antitumorigenic properties and antimicrobial activity. Use of simple soluble inorganic gallium salts, represented by Ganite® for treating a variety of diseases have already reached clinical applications. However, there are still several drawbacks of using gallium salts to deliver gallium at the cellular level, including (1) low-transport capacity of gallium because of the limited plasma concentrations of apo-Tf available for Ga(III)-binding in the blood stream; (2) slow kinetics due to the need to recycle the Tf after the Ga(III) ion is delivered inside the cell; and (3) hydrolysis of Ga(III) ions is a concentration-limiting factor and the origin of renal toxicity of drugs based on soluble gallium salts. To circumvent these limitations of the transferrin-receptor mediated uptake. Gallium nanoparticles with pH sensitivity are synthesized on a PVP (polyvinylpyrrolidone) template for cell culture viability studies on various cancer cell lines. Three gallium-based nanoparticle systems are synthesized and investigated here which confirm cellular uptake in tumorigenic cells and/or cytotoxicity to tumor cells. Effectively bypassing the l (open full item for complete abstract)

MS, University of Cincinnati, 2018, Engineering and Applied Science: Electrical Engineering

Various technical and business challenges make it difficult for every IC company to own and maintain its own foundry. This makes the role of third party foundries very important. Since, the fabrication process involves significant third party handling, the IC design is exposed to various risks and vulnerabilities. The designers send GDSII layout to different foundries for fabrication. In this process there is a huge possibility of presence of malicious foundries, which account for overproduction, counterfeit, theft or inserting trojans. Over the time, significant amount of research has been done to overcome these issues in hardware security. With increased popularity of High-level synthesis, a lot of research is being done for hardware security in high level synthesis. Furthermore, this research can be divided into three main streams, namely, designing an attack methodology, developing attack prevention methods and detecting an inserted trojan. Under 'designing an attack methodology', one state-of-the-art attack claims to decrypt the finite state machine of a design developed through High-level synthesis flow by using Boolean Satisfiability (SAT). This attack formulates a SAT problem by using high level synthesis design constraints, and recovers the correct finite state machine. Few countermeasures have been developed for this threat model which try to harden the FSM of the design in different ways. One of the countermeasures uses decoys to harden the design's finite state machine. The aim of our thesis is to develop a method to decrypt designs with decoy based countermeasure. For our experimentation we used yet another state-of-the-art SAT attack. This SAT attack was originally designed to unlock an encrypted logic design. We used few different approaches to recover the control flow graph of the decoy-encrypted designs. We tried to increase efficiency of SAT attack on our designs by introducing random input patterns and dividing the design into multiple blocks (open full item for complete abstract)

Doctor of Philosophy, The Ohio State University, 1980, Graduate School

Doctor of Philosophy, The Ohio State University, 2016, Biochemistry Program, Ohio State

Total protein synthesis allows the preparation of proteins with chemically diverse modifications. The numerous advantages of total synthesis are sometimes offset by some major limitations. Protein synthesis is a non-trivial task involving many chemical steps, and these steps increase with the size of the protein. Therefore, larger proteins are difficult to synthesize with high yield. We have developed a strategy which we term hybrid-phase native chemical ligation (NCL) to overcome some of the limitations of size and yield. Hybrid-phase NCL combines ligating peptides on a solid support (solid-phase NCL) and in solution (solution-phase NCL) to maximize synthetic yield. We have successfully used this method to synthesize triple-acetylated histone H4-K5ac,K12ac,K91ac and, for the first time, acetylated centromeric histone CENP-A-K124ac (CpA-K124ac). In order to improve the yield of CENP-A total synthesis, we have incorporated a convergent ligation element in our hybrid-phase strategy. This new approach reduced the number of purification steps, leading to a synthetic yield that was almost triple that of the original approach. Finally, we introduce the convergent solid-phase hybrid NCL approach that allows the preparation of a long peptide segment bearing a masked thioester on a solid support. Through a newly developed resin-anchoring strategy, cleavage of the product from solid-phase generated a ligation-compatible segment that could be used directly with no purification. This method has the potential to synthesize large proteins in good yield, effectively overcoming the size and yield limits of protein total synthesis.

Master of Science, University of Toledo, 2015, Chemistry

Tuberculosis, caused by Mycobacterium tuberculosis (Mtb), is the leading cause of bacterial infection related death in the world. The emergence of extensively drug-resistant tuberculosis (XDR-TB) necessitates the study of Mtb and its enzymes to gain an understanding of its essential biosynthetic pathways to aid in the development and design of drug targets and new classes of inhibitors. Maltosyltransferase GlgE encoded by Mtb is involved in a-glucan biosynthesis, and is a promising drug target due to evidence supporting it is essential for cell viability. Deletion of GlgE results in rapid cell death due to accumulation of its substrate, a-1,4-glucan, maltose-1-phosphate (M1P). Creating a library of substrate analogs could be useful for characterizing the enzyme. This thesis illustrates the preliminary results in synthesizing di-, tetra-, and hexasaccharides in a library of a-1,4-glucan, M1P substrate analogs of TB enzyme GlgE. Subsequent glycosylations combined with the highly convergent nature of our synthetic route will yield longer oligomers that will aid in the investigation of this enzyme. Also discussed are alternative synthetic routes to avoid some unforeseen challenges encountered in the original synthesis. Regardless of the origin of the oligosaccharide probes, gaining an understanding of this biosynthetic pathway will aid in the development drug targets and new classes of inhibitors.

Master of Sciences (Engineering), Case Western Reserve University, 2015, Chemical Engineering

We present an alternating current (AC)-powered atmospheric-pressure microplasma for gas-phase synthesis of nanoparticles. The microplasma is formed inside a quartz tube with a powered copper ring electrode on the outside and a tungsten wire on the inside, in contact with the plasma. The electrical properties of the plasma including the voltage and current waveforms are characterized as a function of input power. The plasma length is found to increase with increasing power, reaching a maximum of 4.3 cm at a peak-to-peak voltage of 4 kV. As proof-of-concept, we demonstrate the synthesis of nickel nanoparticles from nickelocene vapor. The particles are monitored in real time by aerosol mobility measurements. Particle size distributions are obtained as a function of nickelocene vapor concentration and input power. Increasing the nickelocene concentration is found to increase the mean diameter and produce a broader range of particle sizes. Interestingly, at higher powers and longer plasma lengths, the particle diameter is found to decrease. Finally, we show that this design allows arrays of microplasmas to be formed with a single power supply and mass flow controller, offering a potential route to scaling up nanoparticle synthesis.

MS, University of Cincinnati, 2014, Engineering and Applied Science: Computer Engineering

As semiconductor technology reaches to nanometer scale, the impact of process uncertainties are increasing, leading to performance and power loss, and consequently reducing the yield. These process parameter variations necessitate the use of suitable variation-aware design techniques. There are some architecture level, circuit level, and post silicon techniques with certain overheads to reduce the effect of such variations. Along with good design techniques, variation-aware analysis plays a major role in determining the efficacy of variation tolerant design. Conventional way of min-max static timing analysis is no more a reliable option; we need to use Statistical Static Timing Analysis (SSTA). Although various techniques for variation tolerant design have been proposed, no major emphasis was given to the initial design phases of the ASIC design flow. In this work, we focused on logic synthesis stage to nullify the effects of process variations. For that, we proposed a novel technique called Library Adaptation for Variation Aware (LAVA) technique and automated the flow for the creation of process variation tolerant design. In LAVA technique a new approach is used to create variation aware libraries by re-characterization of existing libraries and new variation tolerant standard cells are created on demand. This work proposes a design methodology from RTL to GDSII that incorporates LAVA technique at logic synthesis stage for creating variation tolerant design with negligible overhead. The primary goal of our methodology is to capture the statistical aspects of variation from transistor-level of abstraction into gate-level i.e., standard cell library. This newly created variation-aware standard cell library is provided to the existing logic synthesis tool to select the better design at higher level of design cycle, thus making the design more robust to process variations. We have used accurate SSTA using PrimeTime VX by providing variation aware libraries (open full item for complete abstract)

Master of Science, The Ohio State University, 2013, Chemistry

Three-dimensional structure of proteins is an intrinsic property of every protein, and is directly related to its biological function. Studying protein structure is thus of immense importance to understand the mechanism by which the proteins perform such functions. In principle, the backbone structure of a protein can be completely described by a set of torsional angles. Indeed, a significant amount of structural studies of proteins have involved measuring the torsional angles defined by C'-N-Cα-C' atoms (denoted φ) and N-Cα-C'-N atoms (denoted ψ). Little has been done, however, to study the third of the triplet, the ω-torsional angle, defined by the Cα-C'-N-Cα atoms, which is usually assumed to be planar, with the atoms arranged in a trans-like conformation. However, cis-like peptide bonds are known to exist, often at or near active sites, which make them biologically significant, although there are no reliable experimental methods apart from crystallographic studies to differentiate cis-peptide bonds form their trans- counterparts. This thesis is aimed at developing a new solid-state NMR experiment to study the peptide bond geometry. The primary objective is to differentiate cis- and trans-peptide bonds in polypeptides and proteins. Chapter 2 describes the synthesis of isotopically labeled model compounds with trans- and cis-peptide bond. The former, glycylglycine, was synthesized by solid phase peptide synthesis following standard protocols, with minor modifications to increase the yield. The latter, 2,5-diketopiperazine, was synthesized using microwave-assisted synthesis, a protocol recently published. Both the compounds could be obtained in high purity and integrity, as shown by their solution 1H and 13C NMR spectra. Chapter 3 describes the design of the NMR pulse sequence which can achieve this goal. The fundamental idea is to allow correlated evolution of two different anisotropic interactions under magic-angle spinning. Such evolutions are sensitive (open full item for complete abstract)

Master of Science in Chemistry, Youngstown State University, 2010, Department of Chemistry

Sodium azide has traditionally been used as the source of azide anion for the synthesis of alkyl azides. Besides difficulties with solubility, sodium azide is toxic, can be absorbed through the skin, and forms potentially explosive compounds with H2O, Brønsted acids, CH2Cl2, and CHCl3. To avoid these dangers, a new azide transfer reagent was developed from the reaction of 4-acetamidobenzenesulfonyl azide (p-ABSA) and 1,8-diazabicyclo[5.4.0]-undec-7-ene (DBU). It is much safer than sodium azide and was used for the synthesis of alkyl and acyl azides. Alkyl azides thus obtained were employed in an attempted in situ generation of 1,2,3-triazoles, which are aromatic five-membered ring heterocycles having two carbon atoms and three nitrogen atoms, and are biologically important. A known one-pot procedure for 1,2,3-triazole synthesis, described by Fokin and colleagues, was repeated and the formation and ease of isolation of the triazole products was compared with the new chemistry described herein.

Master of Science in Chemistry, Youngstown State University, 2008, Department of Chemistry

This thesis deals with a novel “one-pot” synthesis of organic azides from simple alcohols as well as protected sugars. Experimentation led to the successful azidation of both classes of compounds while providing for the isolation and characterization of unexpected byproducts and side reactions. All findings were strongly supported by previous literature while yields of azide products isolated in this research were more than adequate.

Master of Science in Chemistry, Youngstown State University, 2007, Department of Chemistry

The aim of this project was the synthesis of several phosphonate esters via reaction of the salt of bis (2,2,2 trifluoroethyl) phosphite and a given alpha halo carbonyl compound in a Michealis-Becker reaction scheme. As an alternative to the use of strong base, we employed cesium carbonate as a mild reagent in hopes of successfully synthesizing our target compounds in high yields.

MS, University of Cincinnati, 2001, Arts and Sciences : Physics

Radio astronomy is the science of collecting extra-terrestrial radiation in the range of 15 MHz to 600 GHz to gain understanding of celestial objects. In this thesis I discuss both the single parabolic reflector radio telescope and the two-telescope radio interferometer used in radio astronomy. The total power received by a parabolic reflector is dependent on the size of the antenna, the efficiency of the reflector, the wavelength of light under observation, and the angular response of the antenna, called the "normalized power pattern". Diffraction effects limit the resolution of the single parabolic reflector. The two-telescope interferometer has increased resolution because the main beam that would be created by a single antenna is split into multiple beams through interference, with the width of one beam corresponding to the angular resolution of the interferometer. A commonly used typed of interferometer is the correlating interferometer that integrates the product of the voltages received at each telescope. The correlating interferometer does not measure the received power directly, but rather the Fourier transform of it called the visibility function. By taking many measurements with different baselines, the visibility function can be sampled over the Fourier transform (or u-v plane) space. The visibility function can then be inverted to create a radio map of the brightness distribution of the source.

PhD, University of Cincinnati, 2006, Engineering : Computer Science and Engineering

Reconfigurable computing (RC) is going mainstream where FPGA plays an essential role. Synthesizing the application from concept and prototyping onto reconfigurable FPGAs has emerged as one of the main challenges in design automation area. A large number of new applications show the huge potentials of synthesis strategy and architecture development for FPGAs. The work presented in this dissertation deals with the synthesis and novel architecture of FPGAs. In particular, it tries to address physical aware high level synthesis (PAHLS) methodology to ensure the synthesis integrity for FPGAs. Motivated by the study of PAHLS, a hybrid interconnect structure is proposed to increase the performance and reconfigurability for FPGAs or FPGA-like reconfigurable platforms. We first present a performance-driven PAHLS where relational placement is combined with the macro generation strategy during high level synthesis. Second, we present an automated framework to integrate physical placement information into high-level synthesis that is believed to be the first on-line synthesis methodology for partially reconfigurable FPGAs. The presented synthesizer allocates the FPGA resources adaptively and is incremental in nature. The algorithm is designed to be linear in terms of the number of operations to ensure its on-line usage. We then present a transformation mechanism to extend the synthesis frontier to heterogeneous configurable architectures. We develop an automatic synthesis methodology which attacks both memory and logic assignments by interacting with behavioral synthesis. Next, we present a hybrid interconnect structure which takes advantages of both mesh and tree interconnect topologies. The presented architecture is investigated with a combinatorial analysis which examines the number of switches needed. Our evaluation demonstrates that the presented model has less switch accrued effects due to the introduction of tree networks. Finally we extend that hybrid interconnect struc (open full item for complete abstract)

MS, University of Cincinnati, 2006, Engineering : Computer Engineering

For the past few decades, research and design of CAD tools have focused on developing a set of tools that will guarantee designers first-pass fabrication success. There have been many variations of digital design “suites” that make this claim. With the increase in integrated circuit complexity and the drive for systems-on-a-chip (SoC), companies and universities are now focusing their efforts on creating design tools addressing the analog and RF domains. System-level design is one of the most important and challenging elements in the mixed-signal design process. Currently, many system designs are approached from a bottom-up perspective where components are designed individually and then assembled at the system-level. Concepts such as analog and digital interfacing, defining component specifications, and system verification are typically lacking or are addressed too late. Rapid modeling and component-level trade-offs are important in the design of systems. Many of these integration issues can be addressed early in the design phase by having the capability to predict and model component-level effects. In order to address these issues of system design and synthesis, four primary tools have been developed. These tools include (1) a continuous-time delta-sigma system modeler and designer, (2) a circuit sizer, (3) a performance analysis system, and (4) a parameterized module layout generator. Various analog synthesis flows have been developed using these tools. The first goal of this thesis is to provide the design community with a behavioral environment that will model and aid in the creation of continuous-time single-loop single-bit baseband delta-sigma analog-to-digital modulators using MATLAB and Simulink. The second goal is to use the designs from the delta-sigma toolbox to produce component-level specifications derived from system-level requirements. In this thesis, the developed tools were used in a synthesis loop to design, implement, and verify two continuous-tim (open full item for complete abstract)

PhD, University of Cincinnati, 2005, Engineering : Computer Science and Engineering

With the ever increasing complexity of integrated circuits and constantly shrinking device sizes, the need to develop entire dystems on chip (SoC) has received a significant momentum. With this need,comes the responsibility of bringing about mature computer-aided design (CAD) techniques to handle the complexity of designing such systems. Although mature commercial techniques exist for designing the digital components in a system, design automation for the irreplaceable analog and radio-frequency (RF) circuits in a system remains incipient. Circuit sizing is one of the most important and challenging constituents of any analog design process. Given a set of high-level specifications and a circuit topology, sizing aims to determine the device dimensions and biasing information in order to meet the desired specifications. In this dissertation, we address two major problems ailing the sizing process. One of the most important challenges in analog synthesis is to design a circuit which meets the input specifications at the post-layout stage. The other problem we seek to address in this dissertation is the enormous time spent in sizing due to the overhead of running thousands of simulations for performance estimation. Analog and RF circuits are extremely sensitive to layout parasitics. This extreme dependence of the behavior of analog circuits, on layout-induced parasitics, is responsible for several silicon runs before a functional chip can be designed. We propose two techniques to introduce layout awareness during circuit sizing. The first approach is based on developing fast and accurate models of the layout parasitics. The parasitic capacitance models are used inside a circuit sizing framework to estimate the layout parasitics and account for them in the performance evaluation process. This approach relies on procedural layout generators (PLGs) for developing the parasitic models. The second approach proposed for layout-aware design draws a similarity between layout pa (open full item for complete abstract)

PhD, University of Cincinnati, 2002, Engineering : Computer Science and Engineering

A Reconfigurable Computer (RC) is a hardware platform that typically includes several programmable devices, memory devices, and possibly specialized devices such as analog-to-digital converters. Such high-performance platforms are capable of accommodating large designs while avoiding the time-to-market associated with ASIC implementations. This work addresses the process of mapping data structures of an application onto the storage elements of RCs with hierarchical memories. In order to optimize the placement of data, several aspects of data mapping are addressed. Input specification styles and synthesis-related issues, physical resource conflicts and arbitration issues, several memory mapping techniques, and interaction between memory mapping and logic partitioning are presented and discussed. The state-of-the-art in reconfigurable computers and their memory subsystems is reviewed and RCs are classified based on their architectures. The importance of hierarchical memories in RCs and the trend in increasing complexity is discussed. A specification model that is well-suited for the memory mapping problem is introduced and the synthesis mechanism involved is described. Several memory mapping techniques are presented and their applicability on existing hardware platforms is discussed. Integer Linear Programming (ILP) formulations are used and assignment techniques that cater to different RC features are developed. With this Technique, small to medium sized designs are solved in a reasonable amount of time. Furthermore, these solutions are optimal. On the other hand, with large sized designs, these ILP techniques become time consuming. Because of their slow execution speed and the complexity of the problem, a novel methodology that speeds up the execution while retaining a high mapping quality is introduced. This methodology divides the mapping process into two, global/detailed, sequential steps (ILP-based) and produces fast mappings at a relatively small quality cost. (open full item for complete abstract)

MS, University of Cincinnati, 2002, Engineering : Computer Engineering

This thesis addresses applications of satisfiability techniques in a reconfigurable computer (RC) synthesis framework. The two areas explored are the interconnect synthesis problem and the verification of synthesized register transfer level (RTL) designs. Traditionally, binary decision diagrams (BDD), an efficient canonical form for boolean expressions, have been applied to these problems. The disadvantage was the need of a good variable ordering to solve the problem efficiently. Most reconfigurable field programmable gate array (FPGA) architectures have programmable interconnection networks that can be reconfigured to implement various interconnection patterns among the FPGA's on the board. Partitioning tools for such architectures must produce the necessary interconnect configuration. This process is called Interconnect Synthesis. In our research, interconnect synthesis is based on a boolean satisfiability solver (SAT) using the Impulse Response technique. An appropriate methodology is needed to hierarchically specify the target interconnection network. An architecture description language called the Performance Description Language (PDL+), is used as the front end tool for modeling reconfigurable processors. These models are then elaborated in a symbolic environment called the Analyzer of Reconfigurable Computer (ARC). Boolean SAT solvers guarantee routing, if one exists. The results of SAT solvers are verified by feeding the obtained values back into the symbolic environment. Interconnect synthesis is performed on Wildforce and Corel RC processors. Grasp, Sato and Chaff solvers have been used. Experimental results show that large interconnect synthesis problems can be solved using SAT solvers and that Chaff has superior performance than the other solvers. In a high-level synthesis (HLS) flow, the behavioral specification in VHDL is subjected to scheduling, binding, interconnect and controller generation to obtain a register-transfer-level (RTL) design. In a succ (open full item for complete abstract)

Doctor of Philosophy, University of Toledo, 2010, Chemistry

The hydrophobic nature of the Mycobacterium tuberculosis (M.tb) cell wall contributes significantly to the organism's drug resistance and virulence. Antigen 85 (Ag85), a class of related mycolyltransferase enzymes (Ag85A, Ag85B and Ag85C), plays a major role in the mycobacterial cell wall synthesis through the generation of trehalose dimycolate (TDM) and mycolyarabinogalactan (mAG), major hydrophobic components of the M.tb cell wall. We have extended the search for new inhibitors of mycobacterial cell wall synthesis by making a number of α-D-trehalose and b-D-arabinose-derived thioester, sulfonamide and 1,2-dicarbonyl compounds as synthetic probes or inhibitors of Ag85. Our effort to develop new Ag85 synthetic probes started with synthesis of three thioester derivatives potentially useful for development of new mycolytransferase assays. Starting with commercially available materials, we have modified α-D-trehalose and α-D-methylglucoside at the C-6 position to make thioacetate and benzothioate analogs in fairly good yields (77% to 90%). Continuing our search for potent inhibitors of Ag85, we have also synthesized three classes of D-trehalose and b-D-arabinose-derived esters, a-ketoesters and a-ketoamides, as transition state inhibitors of Ag85C. Incorporation of an ester, α-ketoester or α-ketoamide at the C-6 position was accomplished using Swern conditions to oxidize the primary hydroxyl group, followed by a Horner-Wadsworth-Emmons condensation to obtain the methyl ester. Treatment of the ester with LiOH resulted in a carboxylic acid derivative which was then coupled with a cyanophosphorane in the presence of EDCI to obtain cynanoketo-phosphorane derivative. Oxidation of the phosphorane with DMDO, followed by amidation of the resulting a-ketonitrile with relevant alkyl amines yielded α-ketoamide analogs. Inhibitory study using a newly developed colorimetric assay revealed that an arabinose methyl ester showed weak inhibition of Ag85C at 25 mM concentration, and (open full item for complete abstract)