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https://www.readbyqxmd.com/read/28651259/new-biguanides-as-anti-diabetic-agents-part-i-synthesis-and-evaluation-of-1-substituted-biguanide-derivatives-as-anti-diabetic-agents-of-type-ii-diabetes-insulin-resistant
#1
Samir Y Abbas, Wahid M Basyouni, Khairy A M El-Bayouk, Wael M Tohamy, Hanan F Aly, Azza Arafa, Mahmoud S Soliman
New 1-substituted-biguanide hydrochloride salts were synthesized via reacting benzo[1,3-d]dioxol-5-amine, phenylhydrazine, N,N-dimethylhydrazinecarboxamide, benzohydrazide and 2-phenyl acetohydrazide with dicyandiamide in acidic medium. Structures of the obtained biguanide salts were characterized by spectroscopic tools. The synthesized compounds were screened for their anti-diabetic activity with standard metformin drug. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives significantly decreased the elevated blood glucose level...
June 26, 2017: Drug Research
https://www.readbyqxmd.com/read/28651000/assessing-the-impact-of-benzo-a-pyrene-on-marine-mussels-application-of-a-novel-targeted-low-density-microarray-complementing-classical-biomarker-responses
#2
Mohamed Banni, Susanna Sforzini, Volker M Arlt, Audrey Barranger, Lorna J Dallas, Caterina Oliveri, Yann Aminot, Beniamina Pacchioni, Caterina Millino, Gerolamo Lanfranchi, James W Readman, Michael N Moore, Aldo Viarengo, Awadhesh N Jha
Despite the increasing use of mussels in environmental monitoring and ecotoxicological studies, their genomes and gene functions have not been thoroughly explored. Several cDNA microarrays were recently proposed for Mytilus spp., but putatively identified partial transcripts have rendered the generation of robust transcriptional responses difficult in terms of pathway identification. We developed a new low density oligonucleotide microarray with 465 probes covering the same number of genes. Target genes were selected to cover most of the well-known biological processes in the stress response documented over the last decade in bivalve species at the cellular and tissue levels...
2017: PloS One
https://www.readbyqxmd.com/read/28649092/aryl-hydrocarbon-receptor-ahr-is-a-potential-tumour-suppressor-in-pituitary-adenomas
#3
Robert Formosa, Joseph Borg, Josanne Vassallo
Pituitary adenomas (PA) represent the largest group of intracranial neoplasms, yet the molecular mechanisms driving this disease remain largely unknown. The aim of this study was to use high-throughput screening to identify molecular pathways that may be playing a significant and consistent role in PA. RNA profiling using microarrays on eight local PAs identified the aryl hydrocarbon receptor (AHR) signalling pathway as a key canonical pathway down-regulated in all PA types. This was confirmed by qPCR in 31 tumours...
June 25, 2017: Endocrine-related Cancer
https://www.readbyqxmd.com/read/28641227/presence-distribution-and-risk-assessment-of-polycyclic-aromatic-hydrocarbons-in-rice-wheat-continuous-cropping-soils-close-to-five-industrial-parks-of-suzhou-china
#4
Yong Li, Ling Long, Jing Ge, Li-Xuan Yang, Jin-Jin Cheng, Ling-Xiang Sun, Changying Lu, Xiang-Yang Yu
Polycyclic aromatic hydrocarbons (PAHs) accumulated in agricultural soils are likely to threaten human health and ecosystem though the food chain, therefore, it is worth to pay more attention to soil contamination by PAHs. In this study, the presence, distribution and risk assessment of 16 priority PAHs in rice-wheat continuous cropping soils close to industrial parks of Suzhou were firstly investigated. The concentrations of the total PAHs ranged from 125.99 ng/g to 796.65 ng/g with an average of 352.94 ng/g...
June 15, 2017: Chemosphere
https://www.readbyqxmd.com/read/28639390/design-synthesis-and-biological-evaluation-of-a-new-class-of-benzo-b-furan-derivatives-as-antiproliferative-agents-with-in-silico-predicted-antitubulin-activity
#5
Antonino Lauria, Carla Gentile, Francesco Mingoia, Antonio Palumbo Piccionello, Roberta Bartolotta, Riccardo Delisi, Silvestre Buscemi, Annamaria Martorana
A new series of 3-benzoylamino-5-(1H-imidazol-4-yl)methylaminobenzo[b]furans were synthesized and screened as antitumor agents. As a general trend, tested compounds showed concentration-dependent antiproliferative activity against HeLa and MCF-7 cancer cell lines, exhibiting GI50 values in the low micromolar range. In most cases, insertion of a methyl substituent on the imidazole moiety improved the antiproliferative activity. Therefore, methyl-imidazolyl-benzo[b]furans compounds were tested in cell cycle perturbation experiments, producing cell cycle arrest with proapoptotic effects...
June 22, 2017: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/28639072/a-synthesis-of-functionalized-arylthio-acrylates-benzo-b-1-4-thiazines-and-benzo-4-5-thiazolo-3-2-a-azepines-from-2-methylbenzothiazole-and-acetylenic-esters-in-aqueous-media
#6
Issa Yavari, Kiyana Ghafouri, Nooshin Zahedi, Mohammad Reza Halvagar
Alkyl (Z)-3-((2-(N-((E)-3-methoxy-3-oxoprop-1-en-1-yl)acetamido)phenyl)thio)acrylates are obtained from the reaction between 2-methylbenzothiazole and alkyl propiolates in 70% aqueous alcohol, in moderate yields. When dialkyl acetylenedicarboxylates were used under similar conditions, tetra-alkyl 9,10-dihydrobenzo[4,5]thiazolo[3,2-a]azepine-7,8,9,10-tetracarboxylates, together with dialkyl 4-acetyl-3,4-dihydro-2H-benzo[b][1,4]thiazine-2,3-dicarboxylates were obtained in about 4:1 ratios. The stereochemistry of these products has been confirmed by X-ray diffraction...
June 20, 2017: Molecular Diversity
https://www.readbyqxmd.com/read/28638767/novel-5-benzo-b-thiophen-3-yl-pyridine-3-carbaldehyde-btpa-functionalization-framework-for-modulating-fullerene-electronics
#7
Suru V John, Christian C De Filippo, Simone Silvestrini, Michele Maggini, Emmanuel Iwuoha
Through a cycloaddition reaction, fullerene (C60) was derivatized with a novel organic compound 5-(benzo[b]thiophen-3-yl)pyridine-3-carbaldehyde to form the processable and stable 3-(benzo[b]thiophene-3yl)-5-fullero-1-methylpyrrolidinepyridine (BTFP) compound. BTFP exhibits close similarities to phenyl-C61-butyric-acid-methyl-ester (PCBM) in terms of first reduction potential values (-0.62 and -0.61 V vs. Ag/AgCl, for BTFP and PCBM, respectively) and lowest occupied molecular orbital (LUMO) energy level values (3...
June 2017: ChemistryOpen
https://www.readbyqxmd.com/read/28638659/2-4-chloro-phen-yl-selan-yl-3-4-di-hydro-2h-benzo-h-chromene-5-6-dione-crystal-structure-and-hirshfeld-analysis
#8
Julio Zukerman-Schpector, Karinne E Prado, Luccas L Name, Rodrigo Cella, Mukesh M Jotani, Edward R T Tiekink
The title organoselenium compound, C19H13ClO3Se {systematic name: 2-[(4-chloro-phen-yl)selan-yl]-2H,3H,4H,5H,6H-naphtho-[1,2-b]pyran-5,6-dione}, has the substituted 2-pyranyl ring in a half-chair conformation with the methyl-ene-C atom bound to the methine-C atom being the flap atom. The dihedral angle between the two aromatic regions of the mol-ecule is 9.96 (9)° and indicates a step-like conformation. An intra-molecular Se⋯O inter-action of 2.8122 (13) Å is noted. In the crystal, π-π contacts between naphthyl rings [inter-centroid distance = 3...
June 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28638658/different-intra-and-inter-molecular-hydrogen-bonding-patterns-in-3s-4as-8as-2-2r-3s-3-2-5-x2-benzamido-2-2-5-x2-benzo-yloxy-4-phenyl-butyl-n-tert-butyldeca-hydro-iso-quinoline-3-carboxamides-x-h-or-cl-compounds-with-moderate-aspartyl-protease-inhibition-activity
#9
Wilson Cunico, Maria de Lourdes G Ferreira, James L Wardell, William T A Harrison
The crystal structures of (3S,4aS,8aS)-2-[(2R,3S)-3-benzamido-2-benzo-yloxy-4-phenyl-but-yl]-N-tert-butyldeca-hydro-iso-quinoline-3-carboxamide, C38H47N3O4, (I), and (3S,4aS,8aS)-2-[(2R,3S)-3-(2,5-di-chloro-benzamido)-2-(2,5-di-chloro-benzo-yloxy)-4-phenyl-but-yl]-N-tert-butyldeca-hydro-iso-quinoline-3-carboxamide, C38H43Cl4N3O4, (II), are described. Despite their chemical similarity, they adopt different conformations in the solid state: (I) features a bifurcated intra-molecular N-H⋯(N,O) hydrogen bond from the tert-butylamide NH group to the piperidine N atom and the benzoate O atom, whereas (II) has an intra-molecular N-H⋯O link from the benzamide NH group to the tert-butyl-amide O atom...
June 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28638622/the-synergistic-use-of-plant-and-isolated-bacteria-to-clean-up-polycyclic-aromatic-hydrocarbons-from-contaminated-soil
#10
S Eskandary, A Tahmourespour, M Hoodaji, A Abdollahi
BACKGROUND: Biological methods of polycyclic aromatic hydrocarbons (PAH) contamination elimination typically involve the transformation of contaminants to non-toxic materials by microorganisms and plants and appear to be the most effective methods available. METHODS: In this study, Bacillus licheniformis and Bacillus mojavensis isolated from oil-contaminated soils were inoculated onto Festuca arundinacea seeds before planting in the pot and 3 weeks after planting by syringe injection into the rhizospheric zone in order to study the elimination of PAHs from Festuca's rhizosphere in the greenhouse...
2017: Journal of Environmental Health Science & Engineering
https://www.readbyqxmd.com/read/28637389/occurrence-of-polycyclic-aromatic-hydrocarbons-in-various-types-of-raw-oilseeds-from-different-regions-of-china
#11
Yun-Qi Wen, Yu-Lan Liu, Li-Li Xu, Wen-Xiu Yu, Yu-Xiang Ma
95 samples of 18 types of oilseeds used for edible oil production were collected from different origins of China. The occurrence of polycyclic aromatic hydrocarbons (PAHs) in these oilseeds was presented after the analysis by using a simplified GC-MS method. The results indicated that some of these oilseeds were not found of Indeno[1,2,3-cd]pyrene, Dibenz[a,h]anthracene and Benzo[ghi]perylene. Naphthalene and Phenanthrene had higher concentration than other individual PAH in the same sample. The range of BaP, PAH4 and PAH16 concentration in these 95 samples were 0...
June 21, 2017: Food Additives & Contaminants. Part B, Surveillance
https://www.readbyqxmd.com/read/28634338/coumarin-benzimidazole-hybrids-as-a-potent-antimicrobial-agent-synthesis-and-biological-elevation
#12
L Ravithej Singh, Srinivasa Rao Avula, Sneha Raj, Akanksha Srivastava, Gopala Reddy Palnati, C K M Tripathi, Mukesh Pasupuleti, Koneni V Sashidhara
Molecular hybridization approach is an emerging tool in drug discovery for designing new pharmacophores with biological activity. A novel, new series of coumarin-benzimidazole hybrids were designed, synthesized and evaluated for their broad spectrum antimicrobial activity. Among all the synthesized molecules, compound (E)-3-(2-1H-benzo[d]imidazol-1-yl)-1-((4-chlorobenzyl)oxy)imino)ethyl)-2H-chromen-2-one showed the most promising broad spectrum antibacterial activity against Pseudomonas aeruginosa, Staphylococcus aureus, Bacillus subtilis and Proteus vulgaris...
June 21, 2017: Journal of Antibiotics
https://www.readbyqxmd.com/read/28629854/inhibition-of-organic-anion-transporter-oat-activity-by-cigarette-smoke-condensate
#13
Katia Sayyed, Marc Le Vee, Ziad Abdel-Razzak, Olivier Fardel
Cigarette smoke condensate (CSC) has previously been shown to impair activity and expression of hepatic drug transporters. In the present study, we provided evidence that CSC also hinders activity of organic anion transporters (OATs), notably expressed at the kidney level. CSC thus cis-inhibited OAT substrate uptake in OAT1- and OAT3-transfected HEK293 cells, in a concentration-dependent manner (IC50=72.1μg/mL for OAT1 inhibition and IC50=27.3μg/mL for OAT3 inhibition). By contrast, OAT4 as well as the renal organic cation transporter (OCT) 2 were less sensitive to the inhibitory effect of CSC (IC50=351...
June 16, 2017: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/28626943/bending-curling-rolling-and-salient-behaviors-of-molecular-crystals-driven-by-2-2-cycloaddition-of-styrylbenzoxazole-derivative
#14
Haoran Wang, Peng Chen, Zhu Wu, Jinyu Zhao, Jingbo Sun, Ran Lu
We report interesting photomechanical behaviors of the dynamic molecular crystals of (E)-2-(2,4-dichlorostyryl)benzo[d]oxazole (BOACl24). The first photosalient effect of the crystal based on metal-free olefin driven by photodimerization is observed. Moreover, the needle-like crystals of BOACl24 exhibit a reversible bending away from UV light source. The nanofibers curl easily under UV irradiation in organogel, in which the photo-induced rolling of small slice undergoes. It suggests that the rapid release of the accumulated strain during photodimerization may lead to photosalient effect, and the bending or curling happens when the strain is released more uniformly...
June 19, 2017: Angewandte Chemie
https://www.readbyqxmd.com/read/28626137/novel-palm-fatty-acid-functionalized-magnetite-nanoparticles-for-magnetic-solid-phase-extraction-of-trace-polycyclic-aromatic-hydrocarbons-from-environmental-samples
#15
Siti Khalijah Mahmad Rozi, Hamid Rashidi Nodeh, Muhammad Afzal Kamboh, Ninie Suhana Abdul Manan, Sharifah Mohamad
A novel adsorbent, palm fatty acid coated magnetic Fe3O4 nanoparticles (MNP-FA) was successfully synthesized with immobilization of the palm fatty acid onto the surface of MNPs. The successful synthesis of MNP-FA was further confirmed by X-Ray diffraction (XRD), transmission electron microscopy (TEM), Fourier transform infrared spectroscopy (FT-IR) and Energy dispersive X-Ray spectroscopy (EDX) analyses and water contact angle (WCA) measurement. This newly synthesized MNP-FA was applied as magnetic solid phase extraction (MSPE) adsorbent for the enrichment of polycyclic aromatic hydrocarbons (PAHs), namely fluoranthene (FLT), pyrene (Pyr), chrysene (Cry) and benzo(a)pyrene (BaP) from environmental samples prior to High Performance Liquid Chromatography- Diode Array Detector (HPLC-DAD) analysis...
June 13, 2017: Journal of Oleo Science
https://www.readbyqxmd.com/read/28616976/synthesis-and-herbicidal-activity-of-pyrido-2-3-d-pyrimidine-2-4-dione-benzoxazinone-hybrids-as-protoporphyrinogen-oxidase-inhibitors
#16
Da-Wei Wang, Qian Li, Kai Wen, Ismail Ismail, Dan-Dan Liu, Cong-Wei Niu, Xin Wen, Guang-Fu Yang, Zhen Xi
To search for new protoporphyrinogen oxidase (PPO, EC 1.3.3.4) inhibitors with improved bioactivity, a series of novel pyrido[2,3-d]pyrimidine-2,4-dione-benzoxazinone hybrids, 9-13, were designed and synthesized. Several compounds with improved tobacco PPO (mtPPO)-inhibiting and promising herbicidal activities were found. Among them, the most potent compound, 3-(7-fluoro-3-oxo-4-(prop-2-yn-1-yl)-3,4-dihydro-2H-benzo[b][1,4] oxazin-6-yl)-1-methylpyrido[2,3-d]pyrimidine-2,4(1H,3H)-dione, 11q, with a Ki value of 0...
June 26, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28616736/geographic-variations-in-female-breast-cancer-incidence-in-relation-to-ambient-air-emissions-of-polycyclic-aromatic-hydrocarbons
#17
Courtney Large, Yudan Wei
A significant geographic variation of breast cancer incidence exists, with incidence rates being much higher in industrialized regions. The objective of the current study was to assess the role of environmental factors such as exposure to ambient air pollution, specifically carcinogenic polycyclic aromatic hydrocarbons (PAHs) that may be playing in the geographic variations in breast cancer incidence. Female breast cancer incidence and ambient air emissions of PAHs were examined in the northeastern and southeastern regions of the USA by analyzing data from the Surveillance, Epidemiology, and End Results (SEER) Program and the State Cancer Profiles of the National Cancer Institute and from the Environmental Protection Agency...
June 14, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28616140/photochromic-benzo-b-phosphole-oxide-with-excellent-thermal-irreversibility-and-fatigue-resistance-in-the-thin-film-solid-state-via-direct-attachment-of-dithienyl-units-to-the-weakly-aromatic-heterocycle
#18
Nathan Man-Wai Wu, Hok-Lai Wong, Vivian Wing-Wah Yam
A novel photochromic benzo[b]phosphole oxide has been demonstrated to display photochromic properties with excellent fatigue resistance and thermal irreversibility in polymethylmethacrylate (PMMA) thin film under ambient conditions. The remarkable photochromic behaviour can be achieved by rational molecular design, in which the weakly aromatic phosphole oxide is directly incorporated into the photo-responsive dithienylethene units. Photopatterning via photoinduced colouration and decolouration has been performed to demonstrate the repeatable and distinct transformation between the bistable states, making it a promising candidate with photoswitching properties for optoelectronic applications...
February 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28615927/p-tsa-promoted-syntheses-of-5h-benzo-h-thiazolo-2-3-b-quinazoline-and-indeno-1-2-d-thiazolo-3-2-a-pyrimidine-analogs-molecular-modeling-and-in-vitro-antitumor-activity-against-hepatocellular-carcinoma
#19
Amit K Keshari, Ashok K Singh, Vinit Raj, Amit Rai, Prakruti Trivedi, Balaram Ghosh, Umesh Kumar, Atul Rawat, Dinesh Kumar, Sudipta Saha
In our efforts to address the rising incidence of hepatocellular carcinoma (HCC), we have made a commitment to the synthesis of novel molecules to combat Hep-G2 cells. A facile and highly efficient one-pot, multicomponent reaction has been successfully devised utilizing a p-toluenesulfonic acid (p-TSA)-catalyzed domino Knoevenagel/Michael/intramolecular cyclization approach for the synthesis of novel 5H-benzo[h]thiazolo[2,3-b]quinazoline and indeno[1,2-d] thiazolo[3,2-a]pyrimidine analogs bearing a bridgehead nitrogen atom...
2017: Drug Design, Development and Therapy
https://www.readbyqxmd.com/read/28615111/synthesis-and-antitumor-activities-of-1-2-3-triazines-and-their-benzo-and-heterofused-derivatives
#20
Stella Cascioferro, Barbara Parrino, Virginia Spanò, Anna Carbone, Alessandra Montalbano, Paola Barraja, Patrizia Diana, Girolamo Cirrincione
1,2,3-Triazines are a class of biologically active compounds that exhibit a broad spectrum of activities, including antibacterial, antifungal, antiviral, antiproliferative, analgesic and anti-inflammatory properties. This review, which covers the literature from the end of last century to 2016, treats, through a comprehensive, systematic approach, the 1,2,3-triazine and related benzo- and hetero-fused derivatives possessing antitumor activity. Their efficacy, combined with a simple synthesis confers to these molecules a great potential as scaffold for the development of antitumor compounds...
June 11, 2017: European Journal of Medicinal Chemistry
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