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484,088 results
  • Dim and Dmoc Protecting Groups for Oligodeoxynucleotide Synthesis. [Journal Article]
    Curr Protoc Nucleic Acid Chem. 2020 Sep; 82(1):e111.Fang S, Eriyagama D, … Halami B
  • This protocol provides details for the preparation of nucleoside phosphoramidites with 1,3-dithian-2-yl-methyl (Dim) and 1,3-dithian-2-yl-methoxycarbonyl (Dmoc) as protecting groups, and a linker with Dmoc as the cleavable function, then using them for solid phase synthesis of sensitive oligodeoxynucleotides (ODNs). Using these Dim-Dmoc phosphoramidites and Dmoc linker, ODN synthesis can be achie…
  • CuH-Catalyzed Asymmetric Reductive Amidation of α,β-Unsaturated Carboxylic Acids. [Journal Article]
    Org Lett. 2020 Jul 06 [Online ahead of print]Link A, Zhou Y, Buchwald SL
  • The direct enantioselective copper hydride (CuH)-catalyzed synthesis of β-chiral amides from α,β-unsaturated carboxylic acids and secondary amines under mild reaction conditions is reported. The method utilizes readily accessible carboxylic acids and tolerates a variety of functional groups in the β-position including several heteroarenes. A subsequent iridium-catalyzed reduction to γ-chiral amin…
  • Catalytic Nitrile Hydroboration: A Route to N,N-Diborylamines and Uses Thereof. [Journal Article]
    Chem Asian J. 2020 Jul 06 [Online ahead of print]Hayrapetyan D, Khalimon AY
  • Catalytic reduction of nitriles is considered as an attractive and atom-economical route to a diversity of synthetically valuable primary amines. Compared to other methods, dihydroboration approach has been developed relatively recently but has already attracted the attention of many research groups due to reasonably mild reaction conditions, selectivity control and the access to N,N-diborylamine…
  • A 2D-Covalent Organic Framework with Interlayer Hydrogen Bonding Oriented Through Designed Non-Planarity. [Journal Article]
    J Am Chem Soc. 2020 Jul 05 [Online ahead of print]Alahakoon SB, Tan K, … Smaldone RA
  • We report the synthesis and characterization of a new class of 2D-covalent organic frameworks, called COFamides, whose layers are held together by amide hydrogen bonds. To accomplish this, we have designed monomers with a non-planar structure that arises from steric crowding, forcing the amide side groups out of plane with the COF sheets orienting the hydrogen bonds between the layers. The presen…
  • Acid-Catalyzed Rearrangements of 3-Aryloxirane-2-Carboxamides: Novel DFT Mechanistic Insights. [Journal Article]
    ChemistryOpen. 2020 Jul; 9(7):743-747.Qu ZW, Zhu H, … Grimme S
  • Efficient synthesis of 3-arylquinolin-2(1H)-ones and N-(2-carboxyaryl)-oxalamides from protic acid-catalyzed rearrangements of 3-aryloxirane-2-carboxamides was achieved recently but not well understood. In contrast to the classical Meinwald rearrangement, extensive DFT calculations reveal that the proximal aryl and amide groups have strong synergetic effects to control the amide-aided and aryl-di…
  • Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives. [Journal Article]
    Eur J Med Chem. 2020 Jun 27; 202:112513.Mohammed AAM, Suaifan GARY, … Okechukwu PN
  • Herein we report the design, synthesis and biological evaluation of structurally modified ciprofloxacin, norfloxacin and moxifloxacin standard drugs, featuring amide functional groups at C-3 of the fluoroquinolone scaffold. In vitro antimicrobial testing against various Gram-positive bacteria, Gram-negative bacteria and fungi revealed potential antibacterial and antifungal activity. Hybrid compou…
  • Novel lipophilic analogues from 2,4-D and Propanil herbicides: Biological activity and kinetic studies. [Journal Article]
    Chem Phys Lipids. 2020 Jul 02 [Online ahead of print]Porciuncula LM, Teixeira AR, … D'Oca CRM
  • This work describes the synthesis of new lipophilic amides and esters analogues of classical organochlorides herbicides by incorporation of long-chains from fatty acids and derivatives. The new fatty esters and amides were synthesized in 96-99% and 80-89% yields, respectively. In general, all compounds tested showed superior in vitro activity than commercial herbicides against growth L. sativa an…
  • Water retention capabilities of collagen, gelatin and peptide as studied by IR/QCM/RH system. [Journal Article]
    Spectrochim Acta A Mol Biomol Spectrosc. 2020 Jun 19; 241:118619.Kudo S, Nakashima S
  • In this study, water retention properties of triple helix collagen, gelatin (separated single chains) and peptide (broken peptide fragments) were studied by using IR micro-spectroscopy equipped with a relative humidity (RH) control system and quartz crystal microbalance (QCM). Adsorbed water ratios (wt%) are found to be in the order of collagen, gelatin and peptide (at about RH = 60%, 22 wt% for …
  • Tandem Photoredox Catalysis: Enabling Carbonylative Amidation of Aryl and Alkylhalides. [Journal Article]
    Angew Chem Int Ed Engl. 2020 Jul 04 [Online ahead of print]Polyzos A, Forni JA, … Weragoda G
  • We report a new visible light-mediated carbonylative amidation of aryl, heteroaryl and alkyl halides. A tandem catalytic cycle of [Ir(ppy) 2 (dtb-bpy)] + generates a potent iridium photoreductant via a second catalytic cycle in the presence of DIPEA which productively engages aryl bromides, iodides and even chlorides as well as primary, secondary and tertiary alkyl iodides. The versatility of the…
  • Calcium phosphate nanoparticles as intrinsic inorganic antimicrobials: mechanism of action. [Journal Article]
    Biomed Mater. 2020 Jul 03 [Online ahead of print]Wu VM, Huynh E, … Uskokovic V
  • This is the final report of the study aimed at assessing the antimicrobial activity of CP nanoparticles delivered in the form of hydroxyapatite (HAp) or amorphous CP (ACP) and understanding the fundamental principles behind their mechanisms of action. Not responding to propidium iodide and causing no gross morphological changes except moderate stress-induced filamentation in E. coli, CP nanoparti…
  • Solvation and the secondary structure of a proline-containing dipeptide: insights from VCD spectroscopy. [Journal Article]
    Phys Chem Chem Phys. 2020 Jul 03 [Online ahead of print]Vermeyen T, Merten C
  • In this study we investigate the IR and VCD spectra of the diastereomeric dipeptide Boc-Pro-Phe-(n-propyl) 1 in chloroform-d1 (CDCl3) and the strongly hydrogen bonding solvent dimethylsulfoxide-d6 (DMSO-d6). From comparison of the experimental spectra, the amide II spectral region is identified as marker signature for the stereochemistry of the dipeptide: the homochiral LL-1 features a (+/-)-patt…
  • Discovery of a Novel Class of State-Dependent NaV1.7 Inhibitors for the Treatment of Neuropathic Pain. [Journal Article]
    Chem Pharm Bull (Tokyo). 2020; 68(7):653-663.Tanaka K, Kobayashi H, … Shinozuka T
  • The discovery of a novel class of state-dependent voltage-gated sodium channel (NaV)1.7 inhibitors is described. By the modification of amide or urethane bond in NaV1.7 blocker III, structure-activity relationship studies that led to the identification of novel NaV1.7 inhibitor 2i (DS01171986) were performed. Compound 2i exhibited state-dependent inhibition of NaV1.7 without NaV1.1, NaV1.5 or hum…
  • Interception of the "Bycroft-Gowland" intermediate in the enzymatic macrocyclization of thiopeptides. [Journal Article]
    J Am Chem Soc. 2020 Jul 01 [Online ahead of print]Bogart JW, Kramer NJ, … Bowers AA
  • Thiopeptides are a broad class of macrocyclic, heavily modified peptide natural products that are unified by the presence of a substituted, nitrogen-containing heterocycle core. Early work indicated that this core might be fashioned from two dehydroalanines by an enzyme-catalyzed aza-[4+2] cycloaddition to give a cyclic-hemiaminal intermediate. This common intermediate could then follow a reducti…
  • Cooperative N-H bond activation by amido-Ge(ii) cations. [Journal Article]
    Dalton Trans. 2020 Jul 01 [Online ahead of print]Zhou X, Vasko P, … Aldridge S
  • N-heterocyclic carbene (NHC) and tertiary phosphine-stabilized germylium-ylidene cations, [R(L)Ge:]+, featuring tethered amido substituents at R have been synthesized via halide abstraction. Characterization in the solid state by X-ray crystallography shows these systems to be monomeric, featuring a two-coordinate C,N- or P,N-ligated germanium atom. The presence of the strongly Lewis acidic catio…
  • Nanogels with selective intracellular reactivity for intracellular tracking and delivery. [Journal Article]
    Chemistry. 2020 Jul 01 [Online ahead of print]Zu G, Mergel O, … van Rijn P
  • A multimodal approach for hydrogel-based nanoparticles was developed to selectively allow molecular conjugated species to either be released inside the cell or remain connected to the polymer network. Using the intrinsic difference in reactivity between esters and amides, nanogels with an amide-conjugated dye could be tracked intracellularly localizing next to the nucleus, while ester-conjugation…
  • Mechanisms of γ-Secretase Activation and Substrate Processing. [Journal Article]
    ACS Cent Sci. 2020 Jun 24; 6(6):969-983.Bhattarai A, Devkota S, … Miao Y
  • Amyloid β-peptide, the principal component of characteristic cerebral plaques of Alzheimer's disease (AD), is produced through intramembrane proteolysis of the amyloid precursor protein (APP) by γ-secretase. Despite the importance in the pathogenesis of AD, the mechanisms of intramembrane proteolysis and substrate processing by γ-secretase remain poorly understood. Here, complementary all-atom si…
  • Protein Conformational Changes in Breast Cancer Sera Using Infrared Spectroscopic Analysis. [Journal Article]
    Cancers (Basel). 2020 Jun 27; 12(7)Ghimire H, Garlapati C, … Perera AGU
  • Protein structural alterations, including misfolding and aggregation, are a hallmark of several diseases, including cancer. However, the possible clinical application of protein conformational analysis using infrared spectroscopy to detect cancer-associated structural changes in proteins has not been established yet. The present study investigates the applicability of Fourier transform infrared s…
  • Non-water-excitation MR spectroscopy techniques to explore exchanging protons in human brain at 3 T. [Journal Article]
    Magn Reson Med. 2020 Jun 30 [Online ahead of print]Dziadosz M, Bogner W, Kreis R
  • CONCLUSIONS: Novel non-water-excitation MRS sequences offer substantial benefits for the detection of metabolite signals that are otherwise suppressed by saturation transfer from water. Avoiding water saturation and using very short echo times allows direct observation of faster exchanging moieties than was previously possible at 3 T and additionally makes the methods less susceptible to fast T2 relaxation.
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