A5005811573- Biochemical and Molecular Research
- Carbohydrate Chemistry and Synthesis
- Glycosylation and Glycoproteins Research
- Sulfur-Based Synthesis Techniques
- Tuberculosis Research and Epidemiology
- Fungal Infections and Studies
- Antimicrobial Peptides and Activities
- Antifungal resistance and susceptibility
- Organoselenium and organotellurium chemistry
- Genomics, phytochemicals, and oxidative stress
- Mycobacterium research and diagnosis
- Chemical Synthesis and Analysis
- thermodynamics and calorimetric analyses
- X-ray Diffraction in Crystallography
- Synthesis and Biological Evaluation
- Metal complexes synthesis and properties
- CAR-T cell therapy research
- Crystallization and Solubility Studies
- Organic Chemistry Cycloaddition Reactions
- Click Chemistry and Applications
- Fluorine in Organic Chemistry
- Synthesis and biological activity
- Monoclonal and Polyclonal Antibodies Research
- Biosimilars and Bioanalytical Methods
Fox Chase Chemical Diversity Center
2020
University of Toledo
2014-2018
University of Pennsylvania
2018
University Surgical Associates
2015
2-Alkyl-1,2-benzisoselenazol-3(2H)-ones, represented by ebselen (1a), are being studied intensively for a range of medicinal applications. We describe both new thermal and photoinduced copper-mediated cross-coupling between potassium selenocyanate (KSeCN) N-substituted ortho-halobenzamides to form 2-alkyl-1,2-benzisoselenazol-3(2H)-ones containing C–Se–N bond. The copper ligand (1,10-phenanthroline) facilitates C–Se bond formation during heating via mechanism that likely involves atom...
Ebselen (EBS) is an organo-selenium-containing compound that has anti-inflammatory, antitumor, and antibacterial properties. EBS being explored as a possible treatment for reperfusion injury stroke under clinical trials mimetic of lithium the bipolar disorder [Mota et al. Synapse 2020, 74 (7), 1−6] noise-induced hearing loss result these actives [Martini J. Psychiatr. Res. 2019, 109, 107−117. Slusarczyk Neural Regener. 17 1255–1261. Thangamani PLoS One 2015, 10 e0133877. Kil Lancet 2017, 390...
Tuberculosis (TB) is an epidemic disease and the growing burden of multidrug-resistant (MDR) TB world wide underlines need to discover new drugs treat disease.
New 2-aminothiophenes (2AT) were identified with MICs = 0.23–0.44 μM against drug sensitive and resistant strains of<italic>Mycobacterium tuberculosis</italic>.
Previous studies identified ebselen as a potent in vitro and vivo inhibitor of the Mycobacterium tuberculosis (Mtb) antigen 85 (Ag85) complex, comprising three homologous enzymes required for biosynthesis mycobacterial cell wall. In this study, Mtb Ag85C enzyme was cocrystallized with azido adamantyl derivatives, resulting two crystallographic structures 2.01 1.30 Å resolution, respectively. Both displayed anticipated covalent modification solvent accessible, noncatalytic Cys209 residue...
Long treatment times, poor drug compliance, and natural selection during of Mycobacterium tuberculosis (Mtb) have given rise to extensively drug-resistant (XDR-TB). As a result, there is need identify new antituberculosis targets. Mtb GlgE maltosyl transferase involved in α-glucan biosynthesis. Mutation increases the concentration maltose-1-phosphate (M1P), one substrate for GlgE, causing rapid cell death. We designed 2,5-dideoxy-3-O-α-d-glucopyranosyl-2,5-imino-d-mannitol (9) act as an...
Oligosaccharide synthesis on organic solvent soluble, high molecular weight poly(2-hydroxyethylmethylacrylate) (pHEMA) is described. The pHEMA-bound oligosaccharide could be recovered after each reaction in 90-95% yield using a precipitation method. methodology was used to synthesize model tri-galactoside 48% overall and trisaccharide from the outer core domain of Pseudomonas aeruginosa lipopolysacchride (LPS) 39% yield. use photo-cleavable linker also demonstrated produce reducing-end...
Correction for ‘Synthesis of 2-deoxy-2,2-difluoro-α-maltosyl fluoride and its X-ray structure in complex with <italic>Streptomyces coelicolor</italic> GlgEI-V279S’ by Sandeep Thanna <italic>et al.</italic>, <italic>Org. Biomol. Chem.</italic>, 2015, DOI: 10.1039/c5ob00867k.
Ebselen was previously found to potently inhibit the essential Mycobacterium tuberculosis ( Mtb ) Antigen 85s through allosteric, covalent oxidation of a solvent exposed, conserved cysteine residue. In this study, we sought better understand in vitro inhibitory properties recently synthesized 1 st generation library ebselen derivatives with respect Ag85C. To protein‐inhibitor interactions, Ag85C successfully co‐crystalized two bulky, chemically dissimilar derivatives, resulting X‐ray crystal...
Abstract Background We are developing a series of small nonpeptide mimics host defense proteins (smHDPs) for antifungal applications. MICs &lt; 0.1 µg/ ml have been demonstrated against multiple yeast and mold species. Their potential therapeutic utility has evaluated in animal models disseminated fungal infections. Methods Susceptibility testing clinical isolates Candida albicans (CA) Aspergillus fumigatus (AF) was done according to CLSI guidelines. Cytotoxicity (CC50) mouse 3T3 human...