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Nucleotide Pyrophosphatases (NPPs) i.e. NPP1 and 3 are responsible for maintaining the extracellular level of nucleotides and nucleosides and are also involve in the regulation of nucleotide-based intercellular signaling. The overexpression of these isozymes resulted in various pathological disorders including osteoarthritis, type 2 diabetes, calcification, allergies, neurodegenerative diseases and carcinogenesis. Recently, NPP1 and NPP3 inhibitors attracted attention due to their ability to enhance the efficacy of cancer therapeutics. Therefore, we designed and synthesized two new series of diacylhydrazine derivatives as potential NPP inhibitors. Among all synthesized derivatives, the diacylhydrazine derivatives of 2-(5-(pyridin-3-yl)-2H-tetrazol-2-yl) acetohydrazide exhibited higher inhibitory values. The structures of these derivatives were confirmed by FTIR, 1H NMR, 13C NMR and elemental analyses. Moreover, homology modelling and molecular docking studies of both inhibitors were also carried out to suggest their putative binding mode within respective enzymes i.e., h-NPP1 and h-NPP3. [ABSTRACT FROM AUTHOR]

The title compound with the molecular formula C8H9NO3 is synthesized by refluxing 2-amino-5-hydroxybenzoic acid in methanol. The molecular structure of the compound is determined by single crystal X-ray diffraction. Methyl 2-amino-5-hydroxybenzoate crystallizes in the orthorhombic space group P212121 with a = 4.973(2) Å, b = 10.923(5) Å, c = 14.074(6) Å, Z = 4 and V = 764.4(6) Å3. DFT is used to compute HOMO–LUMO energy levels, to predict the reactivity of substituents (NH2 and OH), and to determine the nucleophilic character of these two groups. The orientation and nature of substituents on benzene favors the formation of a stable six-membered ring via hydrogen bonding which plays a key role in the properties of the investigated compound. The natural bond orbital (NBO) population analysis demonstrates that the hyperconjugative effect between the donor lone pairs located on the carbonyl oxygen atom and the N–H group, via the lp O → σ*(N–H) 1,6-remote interaction, is responsible for the preferred conformation. The molecular electrostatic potential (MEP) surface shows the electrical neutrality in the molecule. To get an insight to the intermolecular interactions in the crystal a Hirshfeld surface analysis is also carried out. [ABSTRACT FROM AUTHOR]

The present study is devoted to the synthesis of 4-chloro-2-{[5-(diethylamino)-2-hydroxybenzylidene]amino}phenol and its transition metal complexes. Synthesis of the ligand has been achieved by the condensation reaction of N,N-diethylsalicylaldehyde with 4-chloro-2-aminophenol in acidic medium. Metals complexes of the ligand with different transition metal ions [M2+= Mn(II), Fe(II), Co(II), Ni(II), Cu(II), Zn(II), Cd(II), Hg(II), and Pd(II)] have been accumulated in alcoholic media and characterized by spectroscopic methods. UV-Vis analysis of the complexes indicates the ligand coordination to the metal ions via both OH groups and the azomethine nitrogen atom, acting as a tridentate ligand. Anticancer tests of selected complexes demonstrate moderate in vitro activity of Cu(II) complex against HeLa cell line. [ABSTRACT FROM AUTHOR]

Synthesis of new symmetric bis-pyrazolone acid dye and its 3d transition metal complexes is studied. Bis-pyrazolone is synthesized from (E)-6,6'-(ethene-1,2-diyl)bis(3-hydrazinylbenzenesulfonic acid) and ethyl ace-toacetate. The synthesized bis-pyrazolone is coupled with diazonium salt of 4-sulpho-2-aminophenol in alkaline medium targeting bis-pyrazolone ligand acid dye. Various metal complexes are obtained by treating a methanolic solution of metal salts with ligand acid dye in basic media. Structures of the synthesized ligand dye and its metal complexes are confirmed by UV-Vis, FTIR, and NMR spectra. The ligand acid dye and metal complex dyes demonstrate absorption in UV-Vis in the range of 400–600 nm. Ligand acid dye and its metal complexes demonstrate good to high value of light speed, washing fastness and rubbing fastness on leather. [ABSTRACT FROM AUTHOR]

Maize, a moderately salt sensitive crop, first experiences osmotic stress that cause reduction in plant growth under salt stress. Fluctuation in cell wall elongation is one of the reasons of this reduction. Along with others, two important proteins expansins and xyloglucan endotransglucosylase are involved in regulation of cell wall elasticity, but the role of epigenetic mechanisms in regulating the cell wall related genes is still elusive. The present study was conducted with the aim of understanding the role of DNA methylation in regulating ZmEXPB2 and ZmXET1 genes. One salt sensitive and one salt tolerant maize cultivar was grown under hydroponic conditions at different levels of salt stress: T1 = 1 mM (control), T2 = 100 mM and T3 = 200 mM in three replicates. DNA and RNA were extracted from roots. After bisulfite treatment, Methyl Sensitive PCR was used for the DNA methylation analysis. It was revealed that fragment in promoter of ZmEXPB2 gene showed high level of DNA methylation under T1 in both varieties. Comparison of different stress treatments revealed decrease in DNA methylation with the increase in salt stress, significantly lower methylation appearing in T3. Similarly, the fragment in promoter of ZmXET1 gene also showed high levels of DNA methylation in T1. When different treatments were analysed, this gene significantly hypomethylated at T2 which continued to decrease in T3 in sensitive variety but remain stable in tolerant variety. Although, further in-depth analysis is required, our results demonstrate region-specific and genotype-specific methylation shift in the promoter of the ZmEXPB2 and ZmXET1 genes when subjected to the salt stress confirming the epigenetic regulation of these genes under stress conditions. [ABSTRACT FROM AUTHOR]

Naked-eye colored chemo dosimeters based on symmetrical calix[4]azo dye conjugates A1–3 are synthesized and characterized. Calix[4]azo dye conjugates exhibit high selectivity and sensitivity in detection of Fe2+, Ni2+, Co2+, and Cr3+ ions, and the highest sensitivity is determined for Cu2+. For the rapid monitoring of Cu2+ ions a simple paper test strip system is developed. [ABSTRACT FROM AUTHOR]

A new and simple isocratic high-performance liquid chromatographic method with ultraviolet detection is described for simultaneous determination of active guaiphenesin and preservative sodium benzoate in Liqufruta garlic cough medicine formulation. The chromatographic separation was achieved using a Zorbax CN; 150 mm × 4.6 mm and 5 μm particle size column employing acetonitrile and water (20: 80, v/v) containing 0.1% formic acid (pH 3.5 ± 0.05) as the mobile phase. The method was validated with respect to linearity, range, precision, accuracy, specificity, limit of detection and limit of quantitation. The both analytes were detected by UV-Vis detector at 245 nm. The method was linear over the concentration range of 0.2-0.8 mg/mL and 0.02-0.06 mg/mL for guaiphenesin and sodium benzoate, respectively. The limit of detection was found to be 0.14 μg/mL for GP and 0.06 μg/mL for SB and the quantification limit was 0.54 μg/mL for GP and 0.22 for SB. Accuracy, evaluated as recovery, was in the range of 97.8-100.0%. Intra-day precision and intermediate precision showed relative standard deviation <1% in each case. [ABSTRACT FROM AUTHOR]