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Hyun-Jeong Ryu, Seung-Ju Yang, Gee-Hyung Lee, Young-Dae Gong
A 2-amido benzo[d]imidazole library has been constructed on solid-phase synthesis. The key step of this solid-phase synthesis involves the preparation of polymer-bound 2-amino benzo[d]imidazole resin through desulfurative cyclization of thiourea resin by using DMC and DIPEA in DCM, and the resin is then functionalized by acylation at the 2-amine position, to afford 2-amido benzo[d]imidazole resin. In the case of 2-amido benzo[d]imidazole resin having p-I, and m-NO2, the resin was further functionalized by Suzuki/Sonogashira-coupling (p-I), and was reduced to primary amine (m-NO2), followed by acylation...
March 20, 2018: ACS Combinatorial Science
Maja Cindrić, Mihaela Perić, Marijeta Kralj, Irena Martin-Kleiner, Marie-Hélène David-Cordonnier, Hana Čipčić Paljetak, Mario Matijašić, Donatella Verbanac, Grace Karminski-Zamola, Marijana Hranjec
Novel nitro (3a-3f)- and amino (4a-4f and 5a-5f)-substituted 2-benzimidazolyl and 2-benzothiazolyl benzo[b]thieno-2-carboxamides were designed and synthesized as potential antibacterial agents. The antibacterial activity of these compounds has been evaluated against Gram-positive (Staphylococcus aureus and Enterococcus faecalis) and Gram-negative bacteria (Escherichia coli and Moraxella catarrhalis). The most promising antibacterial activity was observed for the nitro- and amino-substituted benzimidazole derivatives 3a, 4a, 5a and 5b with MICs 2-8 [Formula: see text]...
March 20, 2018: Molecular Diversity
Gong Jin, Jing Sun, Yuan Yuan, Dan-Dan He, Chao-Guo Yan
Triethylamine-promoted cycloaddition reactions of N-phenacyl and N-alkoxycarbonylmethylbenzothiazolium bromides with aromatic aldehydes and malononitrile (ethyl cyanoacetate, pivaloylacetonitrile) in ethanol afforded functionalized tetrahydrobenzo[d]pyrrolo[2,1-b]thiazoles in good yields and various diastereoselectivity. The oxidation reaction of the functionalized tetrahydrobenzo[d]pyrrolo[2,1-b]thiazoles with DDQ in different solvents resulted in diverse benzothiazole derivatives and benzo[d]pyrrolo[2,1-b]thiazoles...
March 19, 2018: Molecular Diversity
Zhen Ma, Huisheng Zhuang
Benzo[a]pyrene (BaP), a type of polycyclic aromatic hydrocarbon, is widely distributed in the environment. In this study, BaP immunogen and coating antigen were respectively prepared by different methods, and the specific antibody targeting the BaP analyte was obtained. Moreover, gold nanoparticles modified with the specific polyclonal antibody and thiol-capped DNA were prepared as biological probes. Based on the work above, an ultrasensitive biological probe enhanced real-time immuno-polymerase chain reaction (BP-rt-iPCR) assay was developed to detect BaP in several environmental samples...
March 15, 2018: Acta Biochimica et Biophysica Sinica
Jennifer J Trowell, Frank A P C Gobas, Margo M Moore, Christopher J Kennedy
Determining the biotransformation potential of commercial chemicals is critical for estimating their persistence in the aquatic environment. In vitro systems are becoming increasingly important as screening methods for assessing the potential for chemical metabolism. Depletion rate constants (kd ) for several organic chemicals with high octanol-water partition coefficient (Kow ) values (9-methylanthracene, benzo(a)pyrene, chrysene, and PCB-153) in rainbow trout hepatocytes were determined to estimate biotransformation rate constants (kMET ) that were used in fish bioconcentration factor (BCF) models...
March 17, 2018: Archives of Environmental Contamination and Toxicology
ChuanYang Cai, ShuangYu Yu, XinYue Li, Yu Liu, Shu Tao, WenXin Liu
Two typical types of electronic waste (E-waste) were selected to investigate the emission characteristics of polycyclic aromatic hydrocarbons (PAHs) during pyrolytic processing, including emission factor, compositional profile, size distribution and gas-particle partitioning. The mean emission factors (EFs) of total PAHs were measured to be 2.77 ± 1.41 μg/g and 23.65 ± 14.52 μg/g for printed wiring boards and plastic casings, respectively, lower than those for coal combustion and biomass burning...
March 9, 2018: Journal of Hazardous Materials
Mako Funada, Takeshi Nakano, Hiroshi Moriwaki
A novel clean-up technology to remove polycyclic aromatic hydrocarbons (PAHs) from solid samples by magnetic separation using a composite containing iron powder as a magnetic material and activated carbon as an adsorbent in the freeze-dried calcium alginate matrix (Fe-AC-alg) has been developed. The Fe-AC-alg powder (50 mg), mixed with 1.0 g of glass beads having 12 kinds of adsorbed PAHs, was shaken without adding solvents at 300 rpm. After shaking, the Fe-AC-alg powder was separated using a permanent magnet...
March 8, 2018: Journal of Hazardous Materials
Jana Tomc, Katja Kološa, Bojana Žegura, Urška Kamenšek, Barbara Breznik, Tamara Lah Turnšek, Metka Filipič
The problem of the currently used routine genotoxicity tests is relatively low predictivity of in vitro tests for in vivo genotoxicity and carcinogenicity. An important reason is considered to be inadequate expression of xenobiotic-metabolizing enzymes in indicator cell lines. The aim of our study was to generate metabolically active differentiated hepatic progenies (hDHP) from human adipose tissue-derived mesenchymal stem cells (hASC) for genotoxicity testing. hDHP, generated using a three-step hepatic differentiation procedure, expressed hepatic properties such as glycogen storage and albumin secretion...
March 16, 2018: Archives of Toxicology
Tiantian Wang, Shiyang Dong, Xiaodong Chen, Kun Qian, Huayu Wang, Hexiu Quan, Zhongli Zhang, Yueming Zuo, Liping Huang, Dongxun Li, Ming Yang, Shilin Yang, Yi Jin, Zengtao Wang
A series of (E)-3-(benzo[d][1,3]dioxol-5-ylmethylene)pyrrolidin-2-one derivatives were designed, synthesized, and evaluated for their anticonvulsant activities. In the preliminary screening, compounds 5, 6a-6f and 6h-6i showed promising anticonvulsant activities in MES model, while 6f and 6g represented protection against seizures at doses of 100 mg/kg and 0.5 h in scPTZ model. The most active compound 6d had a high-degree protection against the MES-induced seizures with ED50 value of 4.3 mg/kg and TD50 value of 160...
March 6, 2018: Bioorganic & Medicinal Chemistry Letters
G Vázquez-Gómez, L Rocha-Zavaleta, M Rodríguez-Sosa, P Petrosyan, J Rubio-Lightbourn
Benzo[a]pyrene (B[a]P), the most extensively studied carcinogen in cigarette smoke, has been regarded as a critical mediator of lung cancer. It is known that B[a]P-mediated Aryl hydrocarbon Receptor (AhR) activation stimulates the mitogen activated protein kinases (MAPK) signaling cascade in different cell models. MAPK pathway disturbances drive alterations in cellular processes, such as differentiation, proliferation, and apoptosis, and the disturbances may also modify the AhR pathway itself. However, MAPK involvement in B[a]P metabolic activation and toxicity in lung tissues is not well understood...
March 12, 2018: Toxicology Letters
Kyeongjun Lee, Chowee Park, Yeonsoo Oh, Heesoon Lee, Jungsook Cho
Excitotoxicity and oxidative stress play vital roles in the development of neurodegenerative disorders including Alzheimer's disease (AD). In the present study, we investigated the effect of N -((3,4-dihydro-2H-benzo[h]chromen-2-yl)methyl)-4-methoxyaniline (BL-M) on excitotoxic neuronal cell damage in primary cultured rat cortical cells, and compared to that of memantine, a non-competitive N -methyl-d-aspartate (NMDA) receptor antagonist clinically used to treat AD. We found that BL-M inhibited glutamate- or N -methyl-d-aspartate (NMDA)-induced excitotoxic cell damage...
March 15, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Raghavendra Achary, In-A Jung, Hyeon-Kyu Lee
A tandem process, involving Rh(III)-catalyzed oxidative C-H olefination of enantiomerically enriched 4-aryl-benzo-1,3-sulfamidates and subsequent intramolecular aza-Michael cyclization has been developed. The reaction produces trans-benzosulfamidate-fused-1,3-disubstituted isoindolines as major products, in which the configurational integrity of the stereogenic center in the starting material is preserved. Further transformations of the benzosulfamidate-fused-1,3-disubstituted isoindolines are described.
March 15, 2018: Journal of Organic Chemistry
Qiuping Xiang, Yan Zhang, Jiaguo Li, Xiaoqian Xue, Chao Wang, Ming Song, Cheng Zhang, Rui Wang, Chenchang Li, Chun Wu, Yulai Zhou, Xiaohong Yang, Guohui Li, Ke Ding, Yong Xu
Prostate cancer is a commonly diagnosed cancer and a leading cause of cancer-related deaths. The bromodomain and extra terminal domain (BET) family proteins have emerged as potential therapeutic targets for the treatment of castration-resistant prostate cancer. A series of 2,2-dimethyl-2 H -benzo[ b ][1,4]oxazin-3(4 H )-one derivatives were designed and synthesized as selective bromodomain containing protein 4 (BRD4) inhibitors. The compounds potently inhibit BRD4(1) with nanomolar IC50 values and exhibit high selectivity over most non-BET subfamily members...
March 8, 2018: ACS Medicinal Chemistry Letters
Yuan Wang, Zhuang Liu, Han-Yu Peng, Fan He, Lei Zhang, Yousef Faraj, Wei Wang, Xiao-Jie Ju, Rui Xie, Liang-Yin Chu
A simple device, which is equipped with a non-woven fabric filter medium on which immobilized with ion-recognizable smart hollow microgels, is developed for facile detection of trace lead(II) ions (Pb2+). The ion-recognizable smart microgels are made of poly(N-isopropylacrylamide-co-benzo-18-crown-6-acrylamide) (PNB), in which the 18-crown-6 groups act as the sensors of Pb2+ and the N-isopropylacrylamide groups act as the actuators. The PNB hollow microgels can isothermally change from a shrunk state to a swollen state in response to recognizing Pb2+ in the aqueous environment due to the electrostatic repulsion among the charged 18-crown-6/Pb2+ complex groups and the enhancement of hydrophilicity of the microgels...
March 14, 2018: Chemphyschem: a European Journal of Chemical Physics and Physical Chemistry
Katsuaki Kobayashi, Take-Aki Koizumi, Debashis Ghosh, Takashi Kajiwara, Susumu Kitagawa, Koji Tanaka
A RhCp* (Cp* = pentamethylcyclopentadienyl) complex bearing an NAD+ /NADH-functionalized ligand, [RhCp*(pbn)Cl]Cl ([1]Cl, pbn = (2-(2-pyridyl)benzo[b]-1,5-naphthyridine)), was synthesized. The cyclic voltammogram of [1]Cl in CH3 CN shows two reversible redox waves at E1/2 = -0.58 and -1.53 V (vs. the saturated calomel electrode (SCE)), which correspond to the RhIII /RhI and pbn/pbn˙- redox couples, respectively. The addition of acetic acid to the solution afforded the proton-coupled two-electron reduction of [1]Cl at -0...
March 14, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
Ondrej Benek, Lukas Hroch, Laura Aitken, Frank Gunn-Moore, Lucie Vinklarova, Kamil Kuca, Daniel I Perez, Concepcion Perez, Ana Martinez, Zdenek Fisar, Kamil Musilek
Several neurodegenerative disorders including Alzheimer's disease (AD) have been connected with deregulation of casein kinase 1 (CK1) activity. Inhibition of CK1 therefore presents a potential therapeutic strategy against such pathologies. Recently, novel class of CK1-specific inhibitors with N-(benzo[d]thiazol-2-yl)-2-phenylacetamide structural scaffold has been discovered. 1-(benzo[d]thiazol-2-yl)-3-phenylureas, on the other hand, are known inhibitors amyloid-beta binding alcohol dehydrogenase (ABAD), an enzyme also involved in pathophysiology of AD...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
Phealay May, Patricia Bremond, Christophe Sauzet, Philippe Piccerelle, Frédérique Grimaldi, Serge Champion, Pierre-Henri Villard
(1) Objective: Highlight the in vitro effects of 3T3-L1 cell exposure to polychlorinated biphenyls (PCB118 and 153) or benzo(a)pyrene (BaP) alone or as a cocktail on adipogenesis (ADG) by focusing on changes in lipid metabolism and inflammatory-related genes expression (INFG) and ADG-related genes expression (ADGG); (2) Results: Treatment from the early stage of cell differentiation by BaP alone or in combination with PCBs decreased the expression of some of the ADGG ( PPARγ Glut-4 , FAS , Lipin-1a , Leptin , and Adiponectin )...
March 13, 2018: International Journal of Molecular Sciences
Ruijie Liu, Youfeng Zhang, Jun Wang, Qiqi Pan, Yingqi Luo, Yujie Sun, Qingzhe Jin, Xingguo Wang
Contamination sources of polycyclic aromatic hydrocarbons (PAHs) in the raw material, oil production and storage processes of wood-pressed rapeseed oil were investigated in this study. The results showed that benzo[a]pyrene (BaP) and PAH4 (sum of BaP, benzo[a]fluoranthene, benzo[b]fluoranthene and chrysene) were unevenly distributed in the kernel (0.56-0.98 and 2.84-8.64 μg/kg, respectively) and hull (1.53-3.17 and 13.49-22.31 μg/kg, respectively) of the rapeseed raw materials. The contents of BaP and PAH4 continuously increased during the process of wood-pressed rapeseed oil, ranging from 2...
March 14, 2018: Food Additives & Contaminants. Part A, Chemistry, Analysis, Control, Exposure & Risk Assessment
Kohei Takamoto, Shohei Yoshioka, Hiromichi Fujioka, Mitsuhiro Arisawa
A palladium-catalyzed hydroxycyclization reaction of 1,7-enynes to afford seven-membered silacycles (1 H-benzo[ b]silepine skeletons) is developed. This is the first example of both seven-membered ring construction from enynes using a palladium catalyst and hydroxycyclization of enynes to give seven-membered silacycles.
March 12, 2018: Organic Letters
Hideaki Komiyama, Takahiro To, Seiichi Furukawa, Yu Hidaka, Woong Shin, Takahiro Ichikawa, Ryota Arai, Takuma Yasuda
Solution-processed organic solar cells (OSCs) based on narrow-bandgap small molecules hold great promise as next-generation energy-converting devices. In this paper, we focus on a family of A-π-D-π-A-type small molecules, namely, BDT-nT-ID (n = 1-4) oligomers, consisting of benzo[1,2-b:4,5-b']dithiophene (BDT) as the central electron-donating (D) core, 1,3-indandione (ID) as the terminal electron-accepting (A) units, and two regioregular oligo(3-hexylthiophene)s (nT) with different numbers of thiophene rings as the π-bridging units, and elucidate their structure-property-function relationships...
March 12, 2018: ACS Applied Materials & Interfaces
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