Treatment of benzylic bromides with Zn and LiCl, followed by the reaction with i-butyl nitrite gave N-arylmethyl-N-arylmethyleneamine N-oxides in moderate yields. The present reaction is a novel and simple method for the preparation of nitrones from benzylic bromides, although the yields are mod...

Cell Penetrating Peptides -CPPs- are short aminoacidic stretches present in proteins that have the ability to translocate the plasma membrane and facilitate delivery of various molecules. They are usually rich in basic residues, and organized as alpha helices. NF-Y is a transcription factor hete...

One hypothesis accounting for major histocompatibility complex (MHC) restriction by T cell receptors (TCRs) holds that there are several evolutionary conserved residues in TCR variable regions that contact MHC. While this “germline codon” hypothesis is supported by various lines of evidence, i...

Seven A2-binding peptides were tested by the HLA class I α-chain refolding assay previously described for their direct binding to HLA class I α chains derived from a panel of 18 HLA-homozygous B-cell lines of various HLA specificities, including four A2 subtypes: A∗0201, A∗0204, A∗0205, and A∗...

The non-classical HLA-E is a conserved class I molecule that mainly presents monomorphic leader peptides derived from other HLA class I molecules. These leader peptides comprise an optimized sequence for tight and deep binding into the HLA-E groove. In a TAP-deficient environment, as it can be g...

In the direct cell membrane penetration, arginine-rich cell-penetrating peptides are thought to penetrate into cells across the hydrophobic lipid membranes. To investigate the effect of the amphipathic property of arginine-rich peptide on the cell-penetrating ability, we designed a novel amphipa...

T-cell-mediated destruction of pancreatic β cells leads to Type 1 diabetes (TID). Vitamin D-Binding Protein (VDBP) has been identified as an autoantigen and T cell reactivity against VDBP increases in the development of T1D. Autoreactive cytotoxic T lymphocytes (CTLs) recognize β-cell-derived ...

In an endeavor to find a new class of antimicrobial agents, a series of 2-(1H-benzimidazol-2-yl)-5-(diethylamino)phenol, 2-(1,3-benzoxazol-2-yl)-5-(diethylamino)phenol, 2-(1,3-benzothiazol-2-yl)-5-(diethylamino)phenol and their derivatives were synthesized starting from p-N,N-diethyl amino salic...

The excited-state intramolecular proton transfer (ESIPT) fluorescence of the synthesised 2-(1,3-benzothiazol-2-yl)-5-(N,N- diethylamino)phenol (1) was studied using spectroscopic and theoretical methods. The changes in the electronic transition, energy levels, and orbital diagrams were investiga...

The rotational re-orientations times of the 3-(1,3-benzothiazol-2-yl)-7-(diethylamino) chromen-2-one (3-BDC) dye molecule have been examined in ethanol and octanol solvents when macroscopic solvent viscosity parameter is varied by varying the temperature, by employing the steady-state fluorescen...

The oxidation of spermidine or homospermidine with bovine serum amine oxidase (BSAO) was monitored in situ, using proton nuclear magnetic resonance spectroscopy in water with 10% D2O. NMR assignments were performed by spin decoupling and COSY spectra or by comparison with data from synthetic ami...

Infrared spectra were obtained for Cl(CH2)4I and Cl(CH2)5I in the liquid and solid states. Zero-order normal coordinate calculations were made for the five conformers of each compound that have all the carbon atoms coplanar. Comparison of the observed and calculated wavenumbers led to the conclu...

The optimization of a series of benzimidazole glucokinase activators is described. We identified a novel and potent achiral benzimidazole derivative as an allosteric GK activator. This activator was designed and synthesized via removal of the chiral center of the lead compound, 6-(N-acylpyrrolid...

An efficient synthetic pathway to a series of novel “reverse” fosmidomycin analogues has been developed, commencing from substituted benzylamines. In these analogues, the fosmidomycin hydroxamate moiety is reversed and the tetrahedral methylene carbon adjacent to the phosphonate moiety is repl...

Benzene kresoxim-methyl (BKM) is an effective strobilurin fungicide for controlling fungal pathogens but limited information is available on its degradation and metabolism. This study explored the degradation and metabolic profiling for BKM in soils by carbon-14 tracing and HPLC-TOF-MS2 analyzin...

The increased demand for the consumption of vegetable oils has led to the generation of high quantities of by-products, such as palm and soybean fatty acid distillates (PFAD, SFAD), as a result of the refining process. In this study PFAD and SFAD were used as raw materials for the enzymatic prod...

Density (ρ) and viscosity (η) are measured for glycine, DL-α-alanine DL-α-valine, and DL-α-leucine in 0.05, 0.10, 0.15 and 0.20 mol·L−1 aqueous metformin hydrochloride at 308.15, 313.15 and 318.15 K. The measured values are used to estimate some important parameters, such as partial molal ...

Histone deacetylase (HDAC) is a clinically validated target for antitumor therapy. In order to increase HDAC inhibition and efficiency, we developed a novel series of saccharin hydroxamic acids as potent HDAC inhibitors. Among them, compounds 11e, 11m, 11p exhibited similar or better HDACs inhib...

A series of novel 2,5,7-tricarbo-substituted indoles were prepared via sequential Sonogashira and Suzuki–Miyaura cross-coupling of 2-amino-5-bromo-3-iodoacetophenone with terminal acetylenes and aryl/styrylboronic acids followed by palladium chloride-mediated heteroannulation of the incipient 5...

Glycine anion (4) and glycine cation (8) synthons are used in efficient syntheses of 4-substituted analogues of HA-966 (1). A stereospecific route to cis derivatives involves hydrogenation of enamines such as 16. Introduction of a chiral auxiliary leads to an enantioselective synthesis of 2a (L-...