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agents halogénés

Kehan Xu, Shaosheng He, Shichao Chen, Guoliang Qiu, Jingbo Shi, Xinhua Liu, Xiaoyu Wu, Jing Zhang, Wenjian Tang
To develop novel antibacterial agents, 2-sulfoether-4-quinolone scaffolds were synthesized by a free radical process and evaluated for their antibacterial abilities. Excellent activities against Gram-positive bacteria were observed, among which compounds 3m, 3n, 3p and 3t possessed the lowest MICs against both S. aureus and B. cereus (0.8 μM and 1.61 μM, respectively). The structure-activity relationship (SAR) showed that: (i) the antibacterial activity was related to the substituent, such as 2-SCH3  = 2-SCH2 CH3  > 2-S(=O)CH3  > 2-OH, 8-Br > 7-Br > 6-Br; (ii) -CF3 increased the antibacterial activity; (iii) the di-substituted group performed the better activity...
May 19, 2018: European Journal of Medicinal Chemistry
Napon Nilchan, Wanida Phetsang, Taechin Nowwarat, Soraya Chaturongakul, Chutima Jiarpinitnun
Incorporation of halogen atoms to drug molecule has been shown to improve its properties such as enhanced in membrane permeability and increased hydrophobic interactions to its target. To investigate the effect of halogen substitutions on the antibacterial activity of trimethoprim (TMP), we synthesized a series of halogen substituted TMP and tested for their antibacterial activities against global predominant methicillin resistant Staphylococcus aureus (MRSA) strains. Structure-activity relationship analysis suggested a trend in potency that correlated with the ability of the halogen atom to facilitate in hydrophobic interaction to saDHFR...
May 19, 2018: Bioorganic & Medicinal Chemistry
Kevin Muñoz Forti, Faviola Bernard, Gustavo Santiago-Collazo, Waldemar Garcia, Jose L Vera, Enrique Meléndez, Edu B Suarez-Martinez
Introduction: Bacterial antibiotic resistance is on rise despite advances in the development of new antibiotics. In an attempt to circumvent resistance, scientists are shifting focus from modifying existent antibiotics to identifying new antibiotic compounds. Aim: To assess the potential antibiotic effects of functionalised ferrocenecarboxylates para-substituted on the phenoxy pendant group to form: 4-fluorophenyl, 4-chlorophenyl, 4-bromophenyl, 4-iodophenyl and 4-(H-pyrrol-1-yl)phenyl...
February 2018: Journal of Clinical and Diagnostic Research: JCDR
Changliang Ren, Xin Ding, Arundhati Roy, Jie Shen, Shaoyuan Zhou, Feng Chen, Sam Fong Yau Li, Haisheng Ren, Yi Yan Yang, Huaqiang Zeng
Chloride-selective transmembrane carriers or channels might have possible uses in treating channelopathies or cancers. While chloride carriers have been extensively investigated, the corresponding chloride channels have remained limitedly studied. Moreover, all hitherto reported channel systems lack clearly definable and readily modifiable positions in their structures for the reliable construction and combinatorial optimization of their ion transport properties. As a result, the existing channels are limited by their large molecular weight, weak activity or low anion selectivity...
May 7, 2018: Chemical Science
Subhash Chander, Cheng-Run Tang, Ashok Penta, Ping Wang, Deepak P Bhagwat, Nicolas Vanthuyne, Muriel Albalat, Payal Patel, Sanskruti Sankpal, Yong-Tang Zheng, Murugesan Sankaranarayanan
In the current study, twenty-two compounds based upon 3-hydroxy-3-(2-oxo-2-phenylethyl)indolin-2-one nucleus were designed, synthesized and in vitro evaluated for HIV-1 RT inhibition and anti-HIV-1 activity. Compounds 3d, 5c and 5e demonstrated encouraging potency against RT enzyme as well as HIV-1 in low micromolar to nanomolar concentration with good to excellent safety index. Structure activity relationship studies revealed that halogens such as bromo or chloro at 5th the position of oxindole ring remarkably enhanced the potency against RT...
May 9, 2018: Bioorganic Chemistry
Chengzhe Gao, Shu Liu, Kevin J Edgar
Regioselective chlorination of cellulose is challenging due to its low reactivity, the small reactivity differences between cellulosic hydroxyl groups, and the high and diverse reactivity of most common chlorinating agents. Halogenation of cellulose affords useful precursors for subsequent nucleophilic substitution reactions, permitting incorporation of new functionality. Herein we report a simple and efficient pathway for preparation of 6-chloro-6-deoxycellulose esters and their derivatives. Cellulose acetate (degree of substitution (DS) 1...
August 1, 2018: Carbohydrate Polymers
Sara Gutiérrez, David Sucunza, Juan J Vaquero
A new method for the synthesis of γ-carbolines by a heterocyclization that involves α-indol-2-ylmethyl TosMIC derivatives and different electrophiles such as aldehydes, ketones, epoxides, aziridines, iminium salts and halogenating agents has been developed. This methodology has been successfully applied to the synthesis of several highly substituted γ-carbolines in a straightforward way under mild reaction conditions.
May 14, 2018: Journal of Organic Chemistry
Ting Zhou, Wei-Feng Song, You Shang, Shang-Long Yao, Sadis Matalon
Objective: Exposure to halogens, such as chlorine or bromine, results in environmental and occupational hazard to the lung and other organs. Chlorine is highly toxic by inhalation, leading to dyspnea, hypoxemia, airway obstruction, pneumonitis, pulmonary edema, and acute respiratory distress syndrome (ARDS). Although bromine is less reactive and oxidative than chlorine, inhalation also results in bronchospasm, airway hyperresponsiveness, ARDS, and even death. Both halogens have been shown to damage the systemic circulation and result in cardiac injury as well...
May 20, 2018: Chinese Medical Journal
Shigeyuki Kitamura
 The endocrine-disrupting activities of various environmental chemicals are metabolically activated. For example, diphenyls, styrene oligomers, chalcones, trans-stilbene and 2-nitrofluorene are not estrogens, but after incubation with liver microsomes, their metabolites show estrogenic activities. Thus, these chemicals are estrogenically activated by the cytochrome P450 system. In contrast, the antiandrogenic activity of fenthion, an organophosphorus insecticide, is abolished after metabolism to sulfoxide and sulfone derivatives...
2018: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
Viviana Teresa Orlandi, Eleonora Martegani, Fabrizio Bolognese
BACKGROUND: Pseudomonas aeruginosa is the etiological agent of systemic and skin infections that are often difficult to treat. Photodynamic therapy (PDT) and, more recently, phototherapy (PT), are emerging among antimicrobial treatments to be combined with antibiotics. Visible light, either alone or combined with a photosensitizer (PS), elicits photooxidative stress that induces microbial death. The response of bacteria to phototherapy seems to involve the antioxidant machinery. This study relies on the effects of detoxifying catalase A (KatA) in response to PDT and PT-induced photooxidative stress...
April 27, 2018: Photodiagnosis and Photodynamic Therapy
Mahima Bhat, Boja Poojary, Bhuvanesh Sukhlal Kalal, Purawarga Matada Gurubasavaraja Swamy, Senthamaraikannan Kabilan, Vasantha Kumar, Nooji Shruthi, Selvam Athavan Alias Anand, Vinitha Ramanath Pai
AIM: To synthesize a series of new thiazolidinone-pyrazole hybrids (5a-o) and assess their anticancer (in vitro and in vivo) and antimicrobial activities. RESULTS: The compounds 5h (against Ehrlich ascites carcinoma cells), 5e and 5i (against the human breast cancer [MDA-MB231] cell line) exhibited potent anticancer activity. All the compounds except 5g and 5e found to be less toxic for the human dermal fibroblast cells. The effective interactions of the compounds in silico with MDM2 exemplified their inhibitory potency...
April 30, 2018: Future Medicinal Chemistry
Ranjith Kumar Manoharan, Jin-Hyung Lee, Jintae Lee
Certain pathogenic bacteria and yeast form biofilms on biotic and abiotic surfaces including medical devices and implants. Hence, the development of antibiofilm coating materials becomes relevant. The virulence of those colonizing pathogens can be reduced by inhibiting biofilm formation rather than killing pathogens using excessive amounts of antimicrobials, which is touted as one of the main reasons for the development of drug resistance. Candida albicans is an opportunistic fungal pathogen, and the transition of yeast cells to hyphal cells is believed to be a crucial virulence factor...
April 15, 2018: Microbial Biotechnology
Chang-Hee Lee, Soo-Min Lee, Byul-Hana Min, Dong-Su Kim, Chul-Ho Jun
A new method for chlorination of alcohols and carboxylic acids, using α,α-dichlorodiphenylmethane as the chlorinating agent and FeCl3 as the catalyst, was developed. The method enables conversions of various alcohols and carboxylic acids to their corresponding alkyl and acyl chlorides in high yields under mild conditions. Particulary interesting is the observation that the respective alkyl bromides and iodides can be generated from alcohols when either LiBr or LiI are present in the reaction mixtures.
April 6, 2018: Organic Letters
Valerio Paolini, Francesco Petracchini, Monica Carnevale, Francesco Gallucci, Mattia Perilli, Giulio Esposito, Marco Segreto, Leandro Galanti Occulti, Davide Scaglione, Antonietta Ianniello, Massimiliano Frattoni
This study investigates the conversion of sewage sludge from wastewater treatment plants (WWTP) into biomethane for automotive fuel or grid injection. A prototype plant was monitored in Northern Italy, based on vacuum swing adsorption (VSA) on synthetic zeolite 13×: this biogas upgrading method is similar to pressure swing adsorption (PSA) and commonly used for other kinds of biomass. Measurements of biogas inlet, biomethane outlet and off-gas were performed including CH4 , CO2 , CO, H2 , O2 , N2 , HCl, HF, NH3 , H2 S and volatile organic compounds (VOCs)...
March 30, 2018: Journal of Environmental Management
Hossam Draz, Alexander A Goldberg, Emma S Tomlinson Guns, Ladan Fazli, Stephen Safe, J Thomas Sanderson
Prostate cancer is the second leading cause of cancer-related deaths in men in North America and there is an urgent need for development of more effective therapeutic treatments against this disease. We have recently shown that diindolylmethane (DIM) and several of its halogenated derivatives (ring-DIMs) induce death and protective autophagy in human prostate cancer cells. However, the in vivo efficacy of ring-DIMs and the use of autophagy inhibitors as adjuvant therapy have not yet been studied in vivo. The objective of this study was to determine these effects on tumor growth in nude CD-1 mice bearing bioluminescent androgen-independent PC-3 human prostate cancer cells...
April 2, 2018: Investigational New Drugs
Wei Zhang, Wei Wu, Yu Long, Fushan Wang, Jiantai Ma
The design of lower-cost alternative heterogeneous catalysts for the hydrogenation of halogenated nitrobenzenes using green method to synthesize the corresponding anilines is highly desirable. In this study, Ag was incorporated into the Co-MOFs during the growing process (Co-Ag(n)-MOFs), and then followed the carbothermal reduction process without any additional procedures, we synthesized a series of Co-Ag(n)@NCs. The self-supported catalysts exhibited excellent and stable catalytic performances for the chemoselective hydrogenation of halogenated nitrobenzenes without obvious dehalogenation...
March 19, 2018: Journal of Colloid and Interface Science
Xuefeng Guo, Chao Yu, Zhouyang Yin, Shouheng Sun, Christopher T Seto
Ni30 Pd70 nanoparticles supported on nitrogen-doped graphene (NG) acts as a catalyst for the hydrodehalogenation of halogenated aromatics under mild reaction conditions. It reduces mono- or dichloroarenes to the corresponding dehalogenated arenes in >90 % yield in 10 % aqueous isopropanol solvent at or below 50 °C within 5 h. Tests on a variety of substrates containing various functional groups show that the catalyst is selective for reduction of C-Cl and C-Br bonds. In addition, this catalyst completely hydrodehalogenates high-concentration solutions of dioxin, polychlorinated biphenyls, chloroaromatic constituents of the defoliant agent orange, and polybrominated diphenyl ethers in 12 h...
March 14, 2018: ChemSusChem
Rajesh B Patil, Euzebio G Barbosa, Jaiprakash N Sangshetti, Vishal P Zambre, Sanjay D Sawant
Dipeptidyl peptidase-IV (DPP-IV) inhibitors are promising antidiabetic agents. Currently, several DPP-IV inhibitors have been approved for therapeutic use in diabetes mellitus. Receptor-dependent 4D-QSAR is comparatively a new approach which uses molecular dynamics simulations to generate conformational ensemble profiles of compounds representing a dynamic state of compounds at a target's binding site. This work describes a receptor-dependent 4D-QSAR study on triazolopiperazine derivatives. QSARINS multiple linear regression method was adopted to generate 4D-QSAR models...
March 13, 2018: Molecular Diversity
Robin Schürmann, Stefanie Vogel, Kenny Ebel, Ilko Bald
High-energy radiation is used in combination with radiosensitizing therapeutics to treat cancer. The most common radiosensitizers are halogenated nucleosides and cisplatin derivatives, and recently also metal nanoparticles have been suggested as potential radiosensitizing agents. The radiosensitizing action of these compounds can at least partly be ascribed to an enhanced reactivity towards secondary low-energy electrons generated along the radiation track of the high-energy primary radiation, or to an additional emission of secondary reactive electrons close to the tumor tissue...
March 9, 2018: Chemistry: a European Journal
Okiemute Rosa Johnson-Ajinwo, Imran Ullah, Haddijatou Mbye, Alan Richardson, Paul Horrocks, Wen-Wu Li
Thymoquinone (TQ), 2-isopropyl-5-methyl-1,4-benzoquinone, a natural product isolated from Nigella sativa L., has previously been demonstrated to exhibit antiproliferative activity in vitro against a range of cancers as well as the human malarial parasite Plasmodium falciparum. We describe here the synthesis of a series of analogues of TQ that explore the potential for nitrogen-substitution to this scaffold, or reduction to a hydroquinone scaffold, in increasing the potency of this antiproliferative activity against ovarian cancer cell lines and P...
April 15, 2018: Bioorganic & Medicinal Chemistry Letters
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