39 research outputs found

    Sugar amino acids and related molecules: some recent developments

    Get PDF
    To meet the growing demands for the development of new molecular entities for discovering new drugs and materials, organic chemists have started working on many new concepts that can help to assimilate knowledge-based structural diversities more efficiently than ever before. Emulating the basic principles followed by Nature to build its vast repertoire of biomolecules, organic chemists are developing many novel multifunctional building blocks and using them to create 'nature-like' and yet unnatural organic molecules. Sugar amino acids constitute an important class of such polyfunctional scaffolds where the carboxyl, amino and hydroxyl termini provide an excellent opportunity to organic chemists to create structural diversities akin to Nature's molecular arsenal. In recent years, sugar amino acids have been used extensively in the area of peptidomimetic studies. Advances made in the area of combinatorial chemistry can provide the necessary technological support for rapid compilations of sugar amino acidbased libraries exploiting the diversities of their carbohydrate frameworks and well-developed solid-phase peptide synthesis methods. This perspective article chronicles some of the recent applications of various sugar amino acids, furan amino acids, pyrrole amino acids etc. and many other related building blocks in wide-ranging peptidomimetic studies

    SAR Studies Leading to the Identification of a Novel Series of Metallo-β-lactamase Inhibitors for the Treatment of Carbapenem-Resistant Enterobacteriaceae Infections That Display Efficacy in an Animal Infection Model

    Get PDF
    The clinical effectiveness of carbapenem antibiotics such as meropenem is becoming increasingly compromised by the spread of both metallo-β-lactamase (MBL) and serine-β-lactamase (SBL) enzymes on mobile genetic elements, stimulating research to find new β-lactamase inhibitors to be used in conjunction with carbapenems and other β-lactam antibiotics. Herein, we describe our initial exploration of a novel chemical series of metallo-β-lactamase inhibitors, from concept to efficacy, in a survival model using an advanced tool compound (ANT431) in conjunction with meropenem

    A Highly Efficient Azide-Based Protecting Group for Amines and Alcohols

    No full text
    The azide-based carbamate or carbonate protecting group (Azoc) shown above can be removed in less than 2 min under neutral conditions using trimethyl or tributyl phosphine as well as polymer-bound triphenyl phosphine. It was shown to be orthogonal to Fmoc and Mtt for peptide synthesis and to afford β-glycoside with a 2-aminoglucosyl donor by virtue of the neighboring group participation

    Sugar amino acids in designing new molecules

    No full text
    Emulating the basic principles followed by Nature to build its vast repertoire of biomolecules, organic chemists are developing many novel multifunctional building blocks and using them to create 'nature-like' and yet unnatural organic molecules. Sugar amino acids constitute an important class of such polyfunctional scaffolds where the carboxyl, amino and hydroxyl termini provide an excellent opportunity to organic chemists to create structural diversities akin to Nature's molecular arsenal. This article describes some of our works on various sugar amino acids and many other related building blocks, like furan amino acids, pyrrole amino acids etc. used in wide-ranging peptidomimetic studies

    Synthesis and characterization of pure and Cu-doped WO3 thin films for high performance of toxic gas sensing applications

    No full text
    Oxygen vacancies and the high surface area of nanostructured materials offers stronger gas adsorption active sites for improved gas sensing performance. In the present work, we have deposited WO3-based thin films using a chemical spray pyrolysis technique at a substrate temperature of 400 °C with other optimized preparation parameters. Besides, this study reports the influence of Cu doping at various weight percentages on the structural, morphological, optical and toxic gas sensing properties of WO3 films in detail. The crystalline structure of the material was investigated using the X-ray diffraction technique. Each X-ray diffraction analysis of the films demonstrated a polycrystalline nature, matching the hexagonal phase of WO3 with the (200) plane of preferential orientation of crystal growth. The optical characteristics of the thin film's material were analyzed by UV–Vis absorption spectroscopy. The optical energy bandgap (Eg) of the deposited thin films was estimated using the Tauc relation, and the value was decreased along with the increase in the Cu-doping concentration. The surface roughness of the films has been investigated using atomic force microscopy. The TEM patterns of sprayed Cu-doped WO3 thin films exhibit nanocrystalline features. Detecting toxic gasses is of great importance across the globe due to an alarming enhancement in respiratory, ocular, skin, and lung diseases. Hence, cost-effective and room temperature-operated Cu-doped WO3 thin film sensors to trace low concentrations of toxic gasses have been investigated and systematically reported. It is observed that the sensor response is to be increased with the increase in Cu-doping concentration, particularly the 4 wt.% Cu-doped sensor exhibited a response value of 7.2 and fast response and recovery times in the presence of 50 ppm ammonia vapor
    corecore