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Song-Lin Zhang, Ze-Long Yu
Divergent synthesis of indoles, oxindoles, isocoumarins and isoquinolinones is described in this report by using a general Pd-catalyzed tandem reaction of β-hydroxy carbonyl compounds with aryl halides bearing an ortho-nitro, -ester or -cyano substituent. A key retro-aldol/α-arylation reaction is involved that merges classic Pd cross-coupling chemistry with novel Pd-promoted retro-aldol C-C activation to produce α-arylated ketones or esters. Subsequent intramolecular condensation of the carbonyl with the ortho-synthon gives target heterocycles...
October 21, 2016: Organic & Biomolecular Chemistry
Juliana Marioni, María Angel da Silva, José Luis Cabrera, Susana C Núñez Montoya, María Gabriela Paraje
BACKGROUND: Candida tropicalis is increasingly becoming among the most commonly isolated pathogens causing fungal infections with an important biofilm-forming capacity. PURPOSE: This study addresses the antifungal effect of rubiadin (AQ1) and rubiadin 1-methyl ether (AQ2), two photosensitizing anthraquinones (AQs) isolated from Heterophyllaea pustulata, against C. tropicalis biofilms, by studying the cellular stress and antioxidant response in two experimental conditions: darkness and irradiation...
November 15, 2016: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
Shekhar Dethe, M Deepak, Amit Agarwal
BACKGROUND: Bacopa monnieri (L.) Wettst., commonly known as Brahmi, is renowned in Indian traditional system for its potent memory enhancing activity, which has been validated by various scientific studies. OBJECTIVE: The objective of this study was to understand the molecular mechanism of memory enhancing activity of BacoMind(®) (BM), a standardized extract of B. monnieri. MATERIALS AND METHODS: BM was screened in vitro in a panel of cell-free and receptor-transfected cell assays...
July 2016: Pharmacognosy Magazine
Rui-Cheng Gao, Fu-Sheng Guo, Nan-Nan Bai, Yun-Long Wu, Fan Yang, Ji-Ye Liang, Zhen-Jing Li, Yao-Yu Wang
Two new three-dimensional isostructural lanthanide metal-organic frameworks (Ln(III)-MOFs), [LnL(H2O)3]·3H2O·0.75DMF (1-Ln; Ln = Dy(III) and Eu(III) ions, H3L = biphenyl-3'-nitro-3,4',5-tricarboxylic acid, DMF = N,N'-dimethylformamide), were synthesized and characterized. The appearance of temperature-dependent out-of-phase (χ″M) signal reveals that complex 1-Dy displays slow magnetic relaxation behavior with the energy barrier (ΔUeff) of 57 K and a pre-exponential factor (τ0) of 3.89 × 10(-8) s at 1200 Oe direct current field...
October 19, 2016: Inorganic Chemistry
A Rahman, S M Vasenwala, M Iqbal
Glyceryl trinitrate (GTN) has been used widely as a potent vasodilator to treat heart conditions, such as angina pectoris and chronic heart failure. This study aims to elucidate the effect of exogenous nitric oxide (NO) administration, using GTN, on carbon tetrachloride (CCl4)-induced oxidative stress and liver injury in rats. The results obtained demonstrated that NO generated by the administration of GTN affords protection against CCl4-induced oxidative stress and liver injury. Administration of CCl4 resulted in a significant (p < 0...
October 10, 2016: Human & Experimental Toxicology
Tijen Kaya Temiz, Omer Demir, Fatma Simsek, Yusuf Cem Kaplan, Selen Bahceci, Barıs Karadas, Aslı Celik, Gokhan Koyluoglu
AIM: The aim of this study is to investigate whether nitric oxide (NO)-mediated colonic motility was altered in rat irritable bowel syndrome (IBS) model, using different isoforms of NO-synthase (NOS) inhibitors. MATERIALS AND METHODS: The animal model of IBS-like visceral hypersensitivity was induced by intra-colonic infusion of 0.5% acetic acid (AA) in saline once daily from postnatal days 8 to 21. Control animals received saline instead of AA. Experiments were performed at the end of 8 weeks...
July 2016: Indian Journal of Pharmacology
Gorazd Drevenšek, Mojca Lunder, Eva Tavčar Benković, Borut Štrukelj, Samo Kreft
BACKGROUND: Silver fir trunk extract (SFTE) is a complex mixture of antioxidative polyphenols (lignans and phenolic acids) from the trunks of silver fir trees (Abies alba, lignum). In our previous study, we have shown that SFTE exerts strong antioxidative and protective effects against atherogenic, diet-induced arterial wall damage. OBJECTIVE: The aim of the present study was to test the potential protective effects of SFTE and its compounds, two phenolic acids (p-coumaric and protocatechuic acids) in ischemia-reperfusion injury of isolated rat hearts...
2016: Food & Nutrition Research
Tourin Bzeih, Timothée Naret, Ali Hachem, Nada Jaber, Ali Khalaf, Jerome Bignon, Jean-Daniel Brion, Mouad Alami, Abdallah Hamze
A convergent and effective synthesis of 3-aryl-indoles, 2,3-diaryl indoles, and (1-arylvinyl)carbazoles from a one-pot sequence involving the coupling of N-tosylhydrazones with ortho-nitro-haloarenes followed by a cyclization has been developed. Compound 5i exhibits excellent antiproliferative activity in the low nM range against colon cancer cell lines.
October 18, 2016: Chemical Communications: Chem Comm
Qing Zhang, Qing Zhang, Yanxing Guan, Shaozheng Liu, Qingjie Chen, Xiangmin Li
BACKGROUND This study was specifically designed to develop a new 99mTc compound with 3-amino-4-[2-(2-methyl-5-nitro-1H-imidazol)-ethylamino]-4-oxo-butyrate (5-ntm-asp) and to verify whether this compound is feasible to be a radiopharmaceutical for hypoxic tumors. MATERIAL AND METHODS Metronidazole derivative 5-ntm-asp was synthesized and then radio-labeled by Na [99mTcO4], forming 99mTc-5-ntm-asp. Another two complexes of 99mTc-2- and 99mTc-5-nitroimidazole-iminodiacetic acid (99mTc-2-ntm-IDA and 99mTc-5-ntm-IDA) were also synthesized based on previous studies...
October 18, 2016: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
Camila L Madeira, Samuel A Speet, Cristina A Nieto, Leif Abrell, Jon Chorover, Reyes Sierra-Alvarez, Jim A Field
Insensitive munitions, such as 3-nitro-1,2,4-triazol-5-one (NTO), are being considered by the U.S. Army as replacements for conventional explosives. Environmental emissions of NTO are expected to increase as its use becomes widespread; but only a few studies have considered the remediation of NTO-contaminated sites. In this study, sequential anaerobic-aerobic biodegradation of NTO was investigated in bioreactors using soil as inoculum. Batch bioassays confirmed microbial reduction of NTO under anaerobic conditions to 3-amino-1,2,4-triazol-5-one (ATO) using pyruvate as electron-donating cosubstrate...
October 14, 2016: Chemosphere
Jianzhong Ma, Chengzhu Zhu, Jun Lu, Tao Wang, Shuheng Hu, Tianhu Chen
The photochemical reaction between biphenyl (Bp) and N(III) under irradiation at 365 nm UV light was investigated. The results showed that Bp conversion efficiency was strongly influenced by N (III) concentration, Bp initial concentration and pH. Species-specific rate constants determined by reaction of Bp with H2ONO(+) (k1), HONO (k2) and NO2(-) (k3) were k1 = (0.058 ± 0.005 L mol(-1) s(-1)), k2 = (0.12 ± 0.06 L mol(-1) s(-1)) and k3 = (0.0019 ± 0.0003 L mol(-1) s(-1)), respectively...
October 14, 2016: Chemosphere
Brandon A Vara, Jeffrey N Johnston
Preparation of a range of enantioenriched β-fluoro amines (α,β-disubstituted) is described in which the nitrogen and fluorine atoms are attached to sp(3)-hybridized carbons. The key finding is a chiral bifunctional Brønsted acid/base catalyst that can deliver β-amino-α-fluoro nitroalkanes with high enantio- and diastereoselection. A denitration step renders the nitro group "traceless" and delivers secondary, tertiary, or vinyl alkyl fluorides embedded within a vicinal fluoro amine functional group. A synthesis of each possible stereoisomer of a β-fluoro lanicemine illustrates the potential ease with which fluorinated small molecules relevant to neuroscience drug development can be prepared in a stereochemically comprehensive manner...
October 17, 2016: Journal of the American Chemical Society
Shanmugam Karthik, Joseph Ajantha, C M Nagaraja, Shanmugam Easwaramoorthi, Thirumanavelan Gandhi
The synthesis of π-extended 10-aryl-pyrenoimidazoles having different substituents was realised via Ru(ii)-catalyzed oxidative annulation of 10-aryl-pyrenoimidazole with diphenylacetylene. The single crystal X-ray structure of trifluoromethyl and carboxylate substituted annulated-10-aryl-pyrenoimidazoles confirms the near coplanarity of the pyrene and imidazole moieties and the presence of twisted conformation resulting in intermolecular C-Hπ interactions. The lowest energy absorption maximum becomes red-shifted characteristic to the nature of the substituent owing to the extended π-conjugation, and specifically the nitro substituent shows intense absorption in the visible region with the maximum at 440 nm...
October 17, 2016: Organic & Biomolecular Chemistry
Martin van Megen, Guido J Reiss, Walter Frank
The asymmetric unit of the title mol-ecular salt, [C5H7N2(+)][(HO)2OP(CH2)9PO2(OH)(-)], consists of one 4-amino-pyridinium cation and one hydrogen (9-phos-phono-non-yl)phospho-nate anion, both in general positions. As expected, the 4-amino-pyridinium moieties are protonated exclusively at their endocyclic nitro-gen atom due to a mesomeric stabilization by the imine form which would not be given in the corresponding double-protonated dicationic species. In the crystal, the phosphonyl (-PO3H2) and hydrogen phospho-nate (-PO3H) groups of the anions form two-dimensional O-H⋯O hydrogen-bonded networks in the ab plane built from 24-membered hydrogen-bonded ring motifs with the graph-set descriptor R(6)6(24)...
October 1, 2016: Acta Crystallographica. Section E, Crystallographic Communications
Dmitry S Poplevin, Fedor I Zubkov, Pavel V Dorovatovskii, Yan V Zubavichus, Victor N Khrustalev
The isomeric title compounds, C12H13NO4 (Ia) and C12H13NO4 (IIa), the products of an usual thermal C6-epimerization of 5-oxo-1,2,3,5,5a,6,7,9b-octa-hydro-7,9a-ep-oxy-pyrrolo-[2,1-a]iso-indole-6-carb-oxy-lic acid, represent the two different diastereomers and have very similar mol-ecular geometries. The mol-ecules of both compounds comprise a fused tetra-cyclic system containing four five-membered rings (pyrrolidine, pyrrolidinone, di-hydro-furan and tetra-hydro-furan), all of which adopt the usual envelope conformations...
October 1, 2016: Acta Crystallographica. Section E, Crystallographic Communications
Yang Liu, Hai-Hui Liu
In the polymeric title compound, [CdCl2(C6H6N4)] n , the central Cd(II) atom is coordinated by four chloride ligands and two N atoms from a chelating 2,2'-bi-1H-imidazole mol-ecule, leading to a distorted octa-hedral Cl4N2 coordination set. As a result of the μ2-bridging character of the Cl ligands, chains parallel to the c axis are formed, with the chelating 2,2'-bi-1H-imidazole ligands decorated on both sides of the chain. The luminescence properties of the complex dispersed in di-methyl-formamide shows that the emission intensities are significantly quenched by nitro-benzene...
October 1, 2016: Acta Crystallographica. Section E, Crystallographic Communications
Mouna Necibi, Laurent Lanceleur, Nadia Mzoughi, Mathilde Monperrus
A new analytical method for the simultaneous determination of eight synthetic musks compounds (SMs) including five polycyclic musks (PCMs) and three nitro musks (NMs) was validated for sediment samples based on a simple QuEChERS (Quick, Easy, Cheap, Effective, Rugged and Safe) sample preparation procedure followed by gas chromatography-mass spectrometry (GC-MS). Good analytical performances were obtained for all the target compounds. For the validation of the method, internal calibration (IC) and internal calibration with QuEChERS (ICQ) were compared...
October 14, 2016: Bulletin of Environmental Contamination and Toxicology
Marie N Hansen, Jon O Lundberg, Mariacristina Filice, Angela Fago, Nanna M G Christensen, Frank B Jensen
In mammals, treatment with low doses of nitrite have cytoprotective effects in ischemia/reperfusion events, due to nitric oxide formation and S-nitrosation of proteins. Interestingly, anoxia-tolerant lower vertebrates possess an intrinsic ability to increase intracellular [nitrite] during anoxia in tissues with high myoglobin and mitochondria contents, such as the heart. Here we test the hypothesis that red and white skeletal muscle develops different nitrite levels in crucian carp exposed to deep hypoxia and whether this correlates with myoglobin concentration...
October 14, 2016: Journal of Experimental Biology
Rajamani Nagarajan, Pankaj Gupta, Poonam Singh, Pinki Chakraborty
Given the fact that the literature describing the intercalation of organic molecules in monometallic LDH systems is scarce, the present investigation is aimed at the generation of ethylene glycol intercalated Fe(II)-Fe(III) LDH with the objective of enhancing the surface area for further catalytic applications of industrially important and environmentally harmful organics. The solvothermal reaction of FeCl3 with urea in an ethylene glycol medium yielded a brown colored powder which was characterized employing a wide range of analytical techniques including high resolution powder X-ray diffraction (PXRD), scanning electron microscopy, thermal analysis, X-ray photo electron spectroscopy (XPS), elemental (C, H, N and S) analysis, UV-visible, photoluminescence spectroscopy measurements, BET surface area and pore-size analysis...
October 14, 2016: Dalton Transactions: An International Journal of Inorganic Chemistry
Paula Regina Elias, Gleicekelly Silva Coelho, Viviane Flores Xavier, Policarpo Ademar Sales Junior, Alvaro José Romanha, Silvane Maria Fonseca Murta, Claudia Martins Carneiro, Nilton Soares Camilo, Flaviane Francisco Hilário, Jason Guy Taylor
A series of novel xylitan derivatives derived from xylitol were synthesized using operationally simple procedures. A xylitan acetonide was the key intermediate used to prepare benzoate, arylsulfonate esters and 1,2,3-triazole derivatives of xylitan. These compounds were evaluated for their in vitro anti-Trypanosoma cruzi activity against trypomastigote and amastigote forms of the parasite in T. cruzi-infected cell lineages. Benznidazole was used as positive control against T. cruzi and cytotoxicity was determined in mammalian L929 cells...
October 10, 2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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