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agents halogénés

Xia Liu, Xin Zhao, Fushun Liang, Baoyi Ren
An efficient halogenation of electron-deficient (hetero)arenes is described. The reaction utilizes common t-BuONa as a catalyst (for iodination) or a promoter (for bromination and chlorination), and perfluorobutyl iodide, CBr4 or CCl4 as the readily-available halogenating agents, respectively. The protocol features broad scope, high efficiency, mild conditions and gram scalability. An ionic pathway involving halogen bond formation and halophilic attack is proposed. The utility of the resulting iodinated heteroarenes is demonstrated in visible light-mediated Caryl-Caryl cross-coupling reaction...
January 17, 2018: Organic & Biomolecular Chemistry
Peng-Hui Li, Hong Jiang, Wen-Jin Zhang, Yong-Lian Li, Min-Cong Zhao, Wei Zhou, Lan-Yue Zhang, Ya-Dong Tang, Chang-Zhi Dong, Zhi-Shu Huang, Hui-Xiong Chen, Zhi-Yun Du
Novel topoisomerase II (Topo II) inhibitors have gained considerable interest for the development of anticancer agents. In this study, a series of carbazole derivatives containing chalcone analogs (CDCAs) were synthesized and investigated for their Topo II inhibition and cytotoxic activities. The results from Topo II mediated DNA relaxation assay showed that CDCAs could significantly inhibit the activity of Topo II, and the structure-activity relationship indicated the halogen substituent in phenyl ring play an important role in the activity...
January 6, 2018: European Journal of Medicinal Chemistry
Sujin Park, Eun Hye Kim, Jinwoo Kim, Seong Hwan Kim, Ikyon Kim
A new chemical space was explored based on an indolizine-chalcone hybrid, which was readily accessible by base-mediated aldol condensation of indolizine bearing a 7-acetyl group with various (hetero)aromatic aldehydes. Their anticancer effect was evaluated, revealing that indolizine-chalcone hybrids with 3,5-dimethoxyphenyl group (4h) or the halogen at the meta position (4j and 4l) could have the potential to induce the caspase-dependent apoptosis of human lymphoma cells.
December 19, 2017: European Journal of Medicinal Chemistry
Xianyi Mei, Xiaoli Yan, Hui Zhang, Mingjia Yu, Guangqing Shen, Linjun Zhou, Zixin Deng, Chun Lei, Xudong Qu
Anthrabenzoxocinones (ABXs) including (-)-ABXs and (+)-ABXs are a group of bacterial FabF-specific inhibitors with potent antimicrobial activity of resistant strains. Optimization of their chemical structures is a promising method to develop potent antibiotics. Through biosynthetic investigation, we herein identified and characterized two highly promiscuous enzymes involved in the (-)-ABX structural modification. The promiscuous halogenase and methyltransferase can respectively introduce halogen-modifications into various positions of the ABX scaffolds and methylation to highly diverse substrates...
December 11, 2017: ACS Chemical Biology
Izabela Szczuka, Andrzej Gamian, Grzegorz Terlecki
3-Bromopyruvate (3-BrPA) is an halogenated analogue of pyruvic acid known for over four decades as an alkylating agent reacting with thiol groups of many proteins. It enters animal cells like a lactate: via monocarboxylic acid transporters. Increasing interest in this compound, in recent times, is mainly due to hopes associated with its anticancer action. It is based on the impairment of energy metabolism of tumor cells by inhibiting enzymes in the glycolysis pathway (hexokinase II, glyceraldehyde 3-phosphate dehydrogenase, phosphoglycerate kinase) and the oxidative phosphorylation (succinate dehydrogenase)...
December 8, 2017: Postȩpy Higieny i Medycyny Doświadczalnej
Yali Wang, Situ Xue, Ruolan Li, Zhihui Zheng, Hong Yi, Zhuorong Li
A series of chalcone derivatives bearing benzamide or benzenesulfonamide moieties were synthesized and evaluated for their anti-tumor effect on HCT116, MCF7 and 143B cell lines in vitro. SAR analysis showed that compounds bearing a benzenesulfonamide group had greater potency than those bearing a benzamide group. It was also shown that compounds with a mono-methyl or mono-halogen group at the 3-position on the terminal phenyl ring were more effective than those with trifluoromethyl or methoxy groups. Compound 8e exhibited the most potent anti-tumor activities against HCT116, MCF7 and 143B cell lines, with IC50 values of 0...
September 18, 2017: Bioorganic & Medicinal Chemistry
Tugce Ipek, Mariana Petronela Hanga, Andreas Hartwig, James Wolffsohn, Clare O'Donnell
PURPOSE: Cataract surgery can lead to the temporary development or worsening of dry eye symptoms. Contributing factors may include corneal incisions, agents used before, during or after surgery, light from the operating microscope, disruption of ocular surface tissues and inflammatory processes. The purpose of this study was to observe the effect of light exposure on conjunctival fibroblasts in order to determine whether light has an effect on wound healing closure, assuming that operating microscopes might have an effect on the ocular surface...
December 7, 2017: Contact Lens & Anterior Eye: the Journal of the British Contact Lens Association
Kristina Pavić, Ivana Perković, Šárka Pospíšilová, Marta Machado, Diana Fontinha, Miguel Prudêncio, Josef Jampilek, Aidan Coffey, Lorraine Endersen, Hrvoje Rimac, Branka Zorc
Four series of primaquine (PQ) derivatives were screened for antitubercular and antiplasmodial activity: amides 1a-k, ureas 2a-s, semicarbazides 3a-c and bis-ureas 4a-u. Antimycobacterial activity of PQ derivatives against Mycobacterium tuberculosis (MTB), M. avium complex (MAC) and M. avium subsp. paratuberculosis (MAP) were evaluated in vitro and compared with PQ and the standard antitubercular drugs. In general, the PQ derivatives showed higher potency than the parent compound. Most of the compounds of series 1 and 2 showed high activity against MAP, comparable or even higher than the relevant drug ciprofloxacin, and weak or no activity against MTB and MAC...
December 2, 2017: European Journal of Medicinal Chemistry
Seul Ki Yeon, Ji Won Choi, Jong-Hyun Park, Ye Rim Lee, Hyeon Jeong Kim, Su Jeong Shin, Bo Ko Jang, Siwon Kim, Yong-Sun Bahn, Gyoonhee Han, Yong Sup Lee, Ae Nim Pae, Ki Duk Park
Benzyloxyphenyl moiety is a common structure of highly potent, selective and reversible inhibitors of monoamine oxidase B (MAO-B), safinamide and sembragiline. We synthesized 4-(benzyloxy)phenyl and biphenyl-4-yl derivatives including halogen substituents on the terminal aryl unit. In addition, we modified the carbon linker between amine group and the biaryl linked unit. Among synthesized compounds, 12c exhibited the most potent and selective MAO-B inhibitory effect (hMAO-B IC50: 8.9 nM; >10,000-fold selectivity over MAO-A) as a competitive inhibitor...
November 24, 2017: Bioorganic & Medicinal Chemistry
Brian M Cawrse, Rena S Lapidus, Brandon Cooper, Eun Yong Choi, Katherine L Seley-Radtke
Halogenated pyrrolo[3,2-d]pyrimidine analogues have shown anti-proliferative activity in recent studies, with cell accumulation occurring in the G2/M stage without apoptosis. However, the mechanism of action and pharmacokinetic (PK) profile of these compounds has yet to be determined. In order to investigate the PK profile of these compounds, a series of halogenated pyrrolo[3,2-d]pyrimidine compounds was synthesized and first tested for activity in various cancer cell lines, as well as in a mouse model. EC50 values ranged from 0...
November 28, 2017: ChemMedChem
M Ramirez Aliaga, J J Escalona Belmonte, Alicia Ramirez-Fernandez, M Rubio Navarro, J Cruz Manas
The implementation of cardioprotective strategies involving pre-, intra-, and postoperative interventions is key during cardiac surgery requiring extracorporeal circulation (ECC). The primary goal of this study was to review the physiopathology of and protection strategies against myocardial damage secondary to ECC during cardiac surgery. The administration of halogenated anesthetics for cardiac anesthesia is commonplace due to their well-known cardioprotective effects and their capacity to ensure hypnosis...
November 16, 2017: Current Vascular Pharmacology
Dinesh Giri Goswami, Rajesh Agarwal, Neera Tewari-Singh
Phosgene Oxime (CX, Cl2CNOH), a halogenated oxime, is a potent chemical weapon that causes immediate acute injury and systemic effects. CX, grouped together with vesicating agents, is an urticant or nettle agent with highly volatile, reactive, corrosive, and irritating vapor, and has considerably different chemical properties and toxicity compared to other vesicants. CX is absorbed quickly through clothing with faster cutaneous penetration compared to other vesicating agents causing instantaneous and severe damage...
November 12, 2017: Toxicology Letters
B J A Palanca, M S Avidan, G A Mashour
Sevoflurane, a volatile anaesthetic agent well-tolerated for inhalation induction, provides a useful opportunity to elucidate the processes whereby halogenated ethers disrupt consciousness and cognition. Multiple molecular targets of sevoflurane have been identified, complementing imaging and electrophysiologic markers for the mechanistically obscure progression from wakefulness to unconsciousness. Recent investigations have more precisely detailed scalp EEG activity during this transition, with practical clinical implications...
October 1, 2017: British Journal of Anaesthesia
Lu Xiao, Yishi Wu, Jianwei Chen, Zhenyi Yu, Yanping Liu, Jiannian Yao, Hongbing Fu
The development of metal-free organic room temperature phosphorescence (RTP) materials has attracted increasing attention because of their applications in sensors, biolabeling (imaging) agents and anticounterfeiting technology, but remains extremely challenging owing to the restricted spin-flip intersystem crossing (ISC) followed by low-yield phosphorescence that cannot compete with nonradiative relaxation processes. Here, we report a facile strategy to realize highly efficient RTP by doping iodo difluoroboron dibenzoylmethane (I-BF2dbm-R) derivatives into a rigid crystalline 4-iodobenzonitrile (Iph-C≡N) matrix...
November 7, 2017: Journal of Physical Chemistry. A
Keum Hwa Lee, Jae Hyon Park, Dong Hyun Kim, Jimin Hwang, Goeun Lee, Jae Seok Hyun, Sung Taik Heo, Ji Hoon Choi, Minwoo Kim, Minhye Kim, Seong Il Kim, Michael Eisenhut, Andreas Kronbichler, Jae Il Shin
Henoch-Schönlein Purpura (HSP, IgA vasculitis) is an immunoglobulin A (IgA) mediated disorder characterized by systemic vasculitis with variable presentation, frequently affecting the skin, mucous membrane, joints, kidneys, and rarely lungs and the central nervous system. Interestingly, enhanced production of interleukin-8 (IL-8) levels are found during active disease and increased levels have been reported in supernatants from human umbilical venous endothelial cells after stimulation with sera from patients affected by HSP...
October 2017: Medical Hypotheses
Manabu Aoki, Hironori Hayashi, Kalapala Venkateswara Rao, Debananda Das, Nobuyo Higashi-Kuwata, Haydar Bulut, Hiromi Aoki-Ogata, Yuki Takamatsu, Ravikiran S Yedidi, David A Davis, Shin-Ichiro Hattori, Noriko Nishida, Kazuya Hasegawa, Nobutoki Takamune, Prasanth R Nyalapatla, Heather L Osswald, Hirofumi Jono, Hideyuki Saito, Robert Yarchoan, Shogo Misumi, Arun K Ghosh, Hiroaki Mitsuya
Antiretroviral therapy for HIV-1 infection/AIDS has significantly extended the life expectancy of HIV-1-infected individuals and reduced HIV-1 transmission at very high rates. However, certain individuals who initially achieve viral suppression to undetectable levels may eventually suffer treatment failure mainly due to adverse effects and the emergence of drug-resistant HIV-1 variants. Here, we report GRL-142, a novel HIV-1 protease inhibitor containing an unprecedented 6-5-5-ring-fused crown-like tetrahydropyranofuran, which has extremely potent activity against all HIV-1 strains examined with IC50 values of attomolar-to-picomolar concentrations, virtually no effects on cellular growth, extremely high genetic barrier against the emergence of drug-resistant variants, and favorable intracellular and central nervous system penetration...
October 17, 2017: ELife
Giovanni Landoni, Juan Carlos Lopez-Delgado, Chiara Sartini, Simona Tamà, Alberto Zangrillo
Halogenated anesthetic agents (desflurane, isoflurane and sevoflurane) may have cardioprotective properties at therapeutic doses against myocardial intraoperative ischemia-reperfusion injury. Cardioprotection mechanisms are related to mitochondrial and anti-apoptotic signaling pathways. Experimental and human studies have proven that their use may reduce morbidity and mortality in the setting of cardiac surgery, including a reduction in myocardial infarct size and mechanical ventilation needs. On the contrary, total intra-venous propofol based anesthesia may be detrimental...
October 10, 2017: Current Vascular Pharmacology
Jaspreet K Aulakh, Tarlok S Lobana, Henna Sood, Daljit S Arora, Victoria A Smolinski, Courney E Duff, Jerry P Jasinski
The basic objective of this investigation is to explore potential metallo-organic antimicrobial agents based on silver-heterocyclic-2-thiones. In this respect, a series of silver(I) halide complexes with imidazolidine-2-thiones (L-NR, R=H, Me, Et, Pr(n), Bu(n), Ph), namely, mononuclear [AgX(L-NR)(PPh3)2] (X, R: Cl, Bu, 1; Br, Ph, 7); [AgX(L-NR)3] (Br, Bu, 5; Br, Pr(n), 8) and halogen bridged dinuclear [Ag2(μ-X)2(L-NR)2(PPh3)2] (Cl, Bu(n), 2; Cl, Ph, 3; Cl, Pr(n), 4; Br, Ph, 6) have been synthesized and characterized using modern techniques...
October 7, 2017: Journal of Inorganic Biochemistry
Francesco De Simone, Luigi Cassarà, Salvatore Sardo, Elena Scarparo, Omar Saleh, Caetano Nigro Neto, Alberto Zangrillo, Giovanni Landoni
CONTEXT: Myocardial injury during cardiac surgery on cardiopulmonary bypass (CPB) is a major determinant of morbidity and mortality. Preclinical and clinical evidence of dose- and time-related cardioprotective effects of volatile anesthetic drugs exist and their use during the whole surgery duration could improve perioperative cardiac protection. Even if administering volatile agents during CPB are relatively easy, technical problems, such as waste gas scavenging, may prevent safe and manageable administration of halogenated vapors during CPB...
October 2017: Annals of Cardiac Anaesthesia
Christ W Shapumba, Michael Knott, Petrina Kapewangolo
The antioxidant potential of various marine natural products is well documented. The aim of this study was to evaluate the antioxidant potential of a rare halogenated monoterpene, namely; 1E,3R,4S,5E,7Z-1-bromo-3,4,8-trichloro-7-(dichloromethyl)-3-methylocta-1,5,7-triene (1) for the first time. This compound was isolated from a Namibian red algal Plocamium species. The antioxidant activity of the compound was evaluated using a series of antioxidant assays, namely; 2,2-diphenyl-1-picryl-hydrazyl radical (DPPH), reducing power, nitric oxide (NO) and hydrogen peroxide (H2O2)...
September 2017: Journal of Food Science and Technology
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