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https://www.readbyqxmd.com/read/28650175/bioactive-peptide-natural-products-as-lead-structures-for-medicinal-use
#1
Tam Dang, Roderich D Süssmuth
The need for new drugs for the treatment of various diseases is enormous. From the previous century until the present, numerous peptide and peptide-derived natural products have been isolated from bacteria and fungi. Hence, microorganisms play a pivotal role as sources for novel drugs with an emphasis on anti-infective agents. Various disciplines from biology, chemistry, and medicine are involved in early stages of the search for peptide natural products including taxonomy, microbiology, bioanalytics, bioinformatics, and medicinal chemistry...
June 26, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28648932/federal-travel-restrictions-to-prevent-disease-transmission-in-the-united-states-an-analysis-of-requested-travel-restrictions
#2
M Robynne Jungerman, Laura A Vonnahme, Faith Washburn, Francisco Alvarado-Ramy
BACKGROUND: Individuals with certain communicable diseases may pose risks to the health of the traveling public; there has been documented transmission on commercial aircraft of tuberculosis (TB), measles, and severe acute respiratory syndrome (SARS). Federal public health travel restrictions (PHTR) prevent commercial air or international travel of persons with communicable diseases that pose a public health threat. METHODS: We described demographics and clinical characteristics of all cases considered for PHTR because of suspected or confirmed communicable disease from May 22, 2007, to December 31, 2015...
June 22, 2017: Travel Medicine and Infectious Disease
https://www.readbyqxmd.com/read/28648923/design-and-environmentally-benign-synthesis-of-novel-thiophene-appended-pyrazole-analogues-as-anti-inflammatory-and-radical-scavenging-agents-crystallographic-in-silico-modeling-docking-and-sar-characterization
#3
Malledevarapura Gurumurthy Prabhudeva, Srinivasan Bharath, Achutha Dileep Kumar, Shivalingegowda Naveen, Neratur Krishnappagowda Lokanath, Bantaganahalli Ningappa Mylarappa, Kariyappa Ajay Kumar
Oxidative-stress induces inflammatory diseases and infections caused by drug-resistant microbial strains are on the rise necessitating the discovery of novel small-molecules for intervention therapy. The current study presents an effective and new green protocol for the synthesis of thiophene-appended pyrazoles through 3+2 annulations method. Chalcones 3(a-g) were prepared from 5-chloro-2-acetylthiophene and aromatic aldehydes by Claisen-Schmidt approach. The reaction of chalcones 3(a-g) with phenylhydrazine hydrochlorides 4(a-b) in acetic acid (30%) medium and also with freshly prepared citrus extract medium under reflux conditions produced the thiophene appended pyrazoles 5(a-l) in moderate yields...
June 16, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28646790/the-effects-of-individual-biological-rhythm-differences-on-sleep-quality-daytime-sleepiness-and-dissociative-experiences
#4
Yavuz Selvi, Ali Kandeger, Murat Boysan, Nursel Akbaba, Ayca A Sayin, Emine Tekinarslan, Basak O Koc, Omer F Uygur, Vedat Sar
Individuals who differ markedly by sleep chronotype, i.e., morning-type or evening-type also differ on a number of psychological, behavioral, and biological variables. Among several other psychological functions, dissociation may also lead to disruption and alteration of consciousness, which may facilitate dream-like experiences. Our study was aimed at an inquiry into the effects of individual biological rhythm differences on sleep quality and daytime sleepiness in conjunction with dissociative experiences...
June 17, 2017: Psychiatry Research
https://www.readbyqxmd.com/read/28646757/discovery-and-structure-activity-relationship-studies-of-2-benzylidene-2-3-dihydro-1h-inden-1-one-and-benzofuran-3-2h-one-derivatives-as-a-novel-class-of-potential-therapeutics-for-inflammatory-bowel-disease
#5
Tara Man Kadayat, Suhrid Banskota, Pallavi Gurung, Ganesh Bist, Til Bahadur Thapa Magar, Aarajana Shrestha, Jung-Ae Kim, Eung-Seok Lee
To develop effective therapeutics for inflammatory bowel disease (IBD), 2-benzylidene-2,3-dihydro-1H-inden-1-one and benzofuran-3(2H)-one derivatives, were designed and synthesized and their structure-activity relationships (SAR) were investigated. Compounds 7, 25, 26, 32, 39, 41, 52, 54, and 55 showed potent inhibitory effect (>70%) on the TNF-α-induced adhesion of monocytes to colon epithelial cells, which is one of the hallmark events leading to IBD. Such inhibitory activity of the compounds correlated with their suppressive activities against the TNF-α-induced production of ROS; ICAM-1 and MCP-1 expression, critical molecules involved in monocyte-epithelial adhesion; and NF-κB transcriptional activity...
June 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28644809/structured-kernel-dictionary-learning-with-correlation-constraint-for-object-recognition
#6
Zhengjue Wang, Yinghua Wang, Hongwei Liu, Hao Zhang
In this paper, we propose a new discriminative non-linear dictionary learning approach, called correlation constrained structured kernel KSVD, for object recognition. The objective function for dictionary learning contains a reconstructive term and a discriminative term. In the reconstructive term, signals are implicitly non-linearly mapped into a space, where a structured kernel dictionary, each sub-dictionary of which lies in the span of the mapped signals from the corresponding class, is established. In the discriminative term, by analyzing the classification mechanism, the correlation constraint is proposed in kernel form, constraining the correlations between different discriminative codes, and restricting the coefficient vectors to be transformed into a feature space, where the features are highly correlated inner-class and nearly independent between-classes...
June 21, 2017: IEEE Transactions on Image Processing: a Publication of the IEEE Signal Processing Society
https://www.readbyqxmd.com/read/28644410/enhanced-antibacterial-activity-of-ent-labdane-derivatives-of-salvic-acid-7%C3%AE-hydroxy-8-17-ent-labden-15-oic-acid-effect-of-lipophilicity-and-the-hydrogen-bonding-role-in-bacterial-membrane-interaction
#7
Javier Echeverría, Alejandro Urzúa, Loreto Sanhueza, Marcela Wilkens
In the present study, the antibacterial activity of several ent-labdane derivatives of salvic acid (7α-hydroxy-8(17)-ent-labden-15-oic acid) was evaluated in vitro against the Gram-negative bacterium Escherichia coli and the Gram-positive bacteria Staphylococcus aureus and Bacillus cereus. For all of the compounds, the antibacterial activity was expressed as the minimum inhibitory concentration (MIC) in liquid media and minimum inhibitory amount (MIA) in solid media. Structure activity relationships (SAR) were employed to correlate the effect of the calculated lipophilicity parameters (logPow) on the inhibitory activity...
June 23, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28643204/host-factors-in-coronavirus-replication
#8
Adriaan H de Wilde, Eric J Snijder, Marjolein Kikkert, Martijn J van Hemert
Coronaviruses are pathogens with a serious impact on human and animal health. They mostly cause enteric or respiratory disease, which can be severe and life threatening, e.g., in the case of the zoonotic coronaviruses causing severe acute respiratory syndrome (SARS) and Middle East Respiratory Syndrome (MERS) in humans. Despite the economic and societal impact of such coronavirus infections, and the likelihood of future outbreaks of additional pathogenic coronaviruses, our options to prevent or treat coronavirus infections remain very limited...
June 23, 2017: Current Topics in Microbiology and Immunology
https://www.readbyqxmd.com/read/28642467/targeting-coronaviral-replication-and-cellular-jak2-mediated-dominant-nf-%C3%AE%C2%BAb-activation-for-comprehensive-and-ultimate-inhibition-of-coronaviral-activity
#9
Cheng-Wei Yang, Yue-Zhi Lee, Hsing-Yu Hsu, Chuan Shih, Yu-Sheng Chao, Hwan-You Chang, Shiow-Ju Lee
Tylophorine-based compounds exert broad spectral, potent inhibition of coronaviruses. NF-κB activation is a common pro-inflammatory response of host cells to viral infection. The aims of this study were to (i) find an effective combination treatment for coronaviral infections through targeting of the virus per se and cellular NF-κB activity; and (ii) to study the underling mechanisms. We found that tylophorine-based compounds target the TGEV viral RNA and effectively inhibit TGEV replication. NF-κB inhibition also leads to anti-TGEV replication...
June 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28642104/design-synthesis-and-sar-of-a-novel-series-of-heterocyclic-phenylpropanoic-acids-as-gpr120-agonists
#10
Xuqing Zhang, Chaozhong Cai, Michael Winters, Michele Wells, Mark Wall, James Lanter, Zhihua Sui, Jingyuan Ma, Aaron Novack, Imad Nashashibi, Yuanping Wang, Wen Yan, Arthur Suckow, Hong Hua, Austin Bell, Peter Haug, Wilma Clapper, Celia Jenkinson, Joseph Gunnet, James Leonard, William V Murray
A novel series of 5-membered heterocycle-containing phenylpropanoic acid derivatives was discovered as potent GPR120 agonists with low clearance, high oral bioavailability and in vivo antidiabetic activity in rodents.
June 12, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28642101/introduction-of-fluorine-to-phenyl-group-of-4-2-pyrimidinylamino-benzamides-leading-to-a-series-of-potent-hedgehog-signaling-pathway-inhibitors
#11
Minhang Xin, Liandi Zhang, Jun Wen, Han Shen, Xinge Zhao, Qiu Jin, Feng Tang
In present study, a novel series of fluorine containing 4-(2-pyrimidinylamino)benzamide analogues were designed and synthesized. The hedgehog (Hh) signaling inhibitory activities for these compounds were evaluated by a luciferase reporter method. The preliminary SAR was discussed and many compounds showed potent Hh signaling inhibitory activities. Compound 15h displayed the most potent inhibitory activity, with an IC50 of 0.050nM. This paper finds the introduction of fluorine to the 4-(2-pyrimidinylamino)benzamide scaffold can lead to a novel series of potent Hh signaling pathway inhibitors...
June 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28641156/mild-c-sp-3-h-functionalization-of-dihydrosanguinarine-and-dihydrochelerythrine-for-development-of-highly-cytotoxic-derivatives
#12
Adriana Romo-Pérez, Luis Demetrio Miranda, Alma D Chávez-Blanco, Alfonso Dueñas-González, María Del Rayo Camacho-Corona, Alejandrina Acosta-Huerta, Abraham García
A series of C(6)-substituted dihydrobenzo[c]phenanthridines were synthesized by mild copper-catalyzed C(sp(3))-H functionalization of dihydrosanguinarine (2) and dihydrochelerythrine (3) with certain nucleophiles selected to enhance cytotoxicity against human breast, colorectal, and prostate cancer cell lines. We also investigated the cytotoxicity of our previously reported C(6)-functionalized N-methyl-5,6-dihydrobenzo[c]phenanthridines 1a-1e to perform structure-activity relationship (SAR) studies. Among the target compounds, five β-aminomalonates (1a, 1b, 2a, 2b, and 3b), one α-aminophosphonate (2c), and one nitroalkyl derivative (2h) exhibited half maximal inhibitory concentration (IC50) values in the range of 0...
June 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28637397/ursolic-acid-derivatives-for-pharmaceutical-use-a-patent-review-2012-2016
#13
Hidayat Hussain, Ivan R Green, Iftikhar Ali, Ikhlas A Khan, Zulfiqar Ali, Abdullah M Al-Sadi, Ishtiaq Ahmed
Ursolic acid (UA), belongs to a group of pentacyclic triterpenoids and is known to possess some very interesting biological properties. Protocols have been developed in order to synthesize bioactive UA analogs which have resulted in numerous ursolic acid analogs being synthesized during the period 2012-2016. Ursolic acid and its analogues can be employed to treat various cancers, inflammatory diseases, diabetes, Parkinson's disease, Alzheimer's disease, hepatitis B, hepatitis C and AIDS to mention but a few...
June 21, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28636671/different-residues-in-the-sars-cov-spike-protein-determine-cleavage-and-activation-by-the-host-cell-protease-tmprss2
#14
Lennart Michel Reinke, Martin Spiegel, Teresa Plegge, Anika Hartleib, Inga Nehlmeier, Stefanie Gierer, Markus Hoffmann, Heike Hofmann-Winkler, Michael Winkler, Stefan Pöhlmann
The spike (S) protein of severe acute respiratory syndrome coronavirus (SARS-CoV) mediates viral entry into target cells. Cleavage and activation of SARS S by a host cell protease is essential for infectious viral entry and the responsible enzymes are potential targets for antiviral intervention. The type II transmembrane serine protease TMPRSS2 cleaves and activates SARS S in cell culture and potentially also in the infected host. Here, we investigated which determinants in SARS S control cleavage and activation by TMPRSS2...
2017: PloS One
https://www.readbyqxmd.com/read/28636590/host-and-viral-traits-predict-zoonotic-spillover-from-mammals
#15
Kevin J Olival, Parviez R Hosseini, Carlos Zambrana-Torrelio, Noam Ross, Tiffany L Bogich, Peter Daszak
The majority of human emerging infectious diseases are zoonotic, with viruses that originate in wild mammals of particular concern (for example, HIV, Ebola and SARS). Understanding patterns of viral diversity in wildlife and determinants of successful cross-species transmission, or spillover, are therefore key goals for pandemic surveillance programs. However, few analytical tools exist to identify which host species are likely to harbour the next human virus, or which viruses can cross species boundaries. Here we conduct a comprehensive analysis of mammalian host-virus relationships and show that both the total number of viruses that infect a given species and the proportion likely to be zoonotic are predictable...
June 21, 2017: Nature
https://www.readbyqxmd.com/read/28636361/a-machine-learning-assisted-approach-for-discovering-novel-inhibitors-targeting-bromodomain-containing-protein-4
#16
Jing Xing, Wenchao Lu, Rongfeng Liu, Yulan Wang, Yiqian Xie, Hao Zhang, Zhe Shi, Hao Jiang, Yu-Chih Liu, Kaixian Chen, Hualiang Jiang, Cheng Luo, Mingyue Zheng
Bromodomain-containing protein 4 (BRD4) is implicated in the pathogenesis of a number of different cancers, inflammatory diseases and heart failure. Much effort has been dedicated toward discovering novel scaffold BRD4 inhibitors (BRD4is) with different selectivity profiles and potential anti-resistance properties. Structure-based drug design (SBDD) and virtual screening (VS) are the most frequently used approaches. Here, we demonstrate a novel, structure-based VS approach that uses machine-learning algorithms trained on the priori structure and activity knowledge to predict the likelihood that a compound is a BRD4i based on its binding pattern with BRD4...
June 21, 2017: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/28635625/soil-moisture-content-estimation-based-on-sentinel-1-and-auxiliary-earth-observation-products-a-hydrological-approach
#17
Dimitrios D Alexakis, Filippos-Dimitrios K Mexis, Anthi-Eirini K Vozinaki, Ioannis N Daliakopoulos, Ioannis K Tsanis
A methodology for elaborating multi-temporal Sentinel-1 and Landsat 8 satellite images for estimating topsoil Soil Moisture Content (SMC) to support hydrological simulation studies is proposed. After pre-processing the remote sensing data, backscattering coefficient, Normalized Difference Vegetation Index (NDVI), thermal infrared temperature and incidence angle parameters are assessed for their potential to infer ground measurements of SMC, collected at the top 5 cm. A non-linear approach using Artificial Neural Networks (ANNs) is tested...
June 21, 2017: Sensors
https://www.readbyqxmd.com/read/28635519/the-elicitor-protein-ases-induces-a-sar-response-accompanied-by-systemic-microbursts-and-micro-hrs-in-fragaria-ananassa
#18
Verónica Hael Conrad, Silvia Marisa Perato, Marta Elena Arias, Martín Gustavo Martínez Zamora, Pía de Los Ángeles Di Peto, Gustavo Gabriel Martos, Atilio Pedro Castagnaro, Juan Carlos Diaz-Ricci, Nadia Regina Chalfoun
The elicitor AsES (Acremonium strictum Elicitor Subtilisin) is a 34 KDa subtilisin-like protein secreted by the opportunistic fungus Acremonium strictum. AsES activates the innate immunity and confers resistance against anthracnose and grey mold diseases in strawberry plants (Fragaria x ananassa Duch.) and the last disease also in Arabidopsis. In the present work, we show that upon AsES recognition, a cascade of defense responses is activated, including: calcium influx, biphasic oxidative burst (O2(.-) and H2O2), HR response, accumulation of autofluorescent compounds, cell wall reinforcement with callose and lignin deposition, salicylic acid accumulation, and expression of defense-related genes such as FaPR1, FaPG1, FaMYB30, FaRBOH-D, FaRBOH-F, FaCHI23 and FaFLS...
June 21, 2017: Molecular Plant-microbe Interactions: MPMI
https://www.readbyqxmd.com/read/28635286/utilization-of-an-active-site-mutant-receptor-for-the-identification-of-potent-and-selective-atypical-5-ht2c-receptor-agonists
#19
Joseph Carpenter, Ying Wang, Gang Wu, Jianxin Feng, Xiang-Yang Ye, Christian L Morales, Matthias Broekema, Karen A Rossi, Keith J Miller, Brian J Murphy, Ginger Yingzhe Wu, Sarah E Malmstrom, Anthony V Azzara, Philip M Sher, John M Fevig, Andrew Alt, Robert L Bertekap, Mary Jane Cullen, Timothy M Harper, Kimberly A Foster, Chiuwa Emily Luk, Qian Xiang, Mary F Grubb, Jeffrey A Robl, Dean A Wacker
Agonism of the 5-HT2C receptor represents one of the most well-studied and clinically-proven mechanisms for pharmacological weight reduction. Selectivity over the closely related 5-HT2A and 5-HT2B receptors is critical as their activation has been shown to lead to undesirable side-effects and major safety concerns. In this communication, we report the development of a new screening paradigm which utilizes an active site mutant D134A 5-HT2C receptor to identify atypical agonist structures. We additionally report the discovery and optimization of a novel class of non-basic heterocyclic amide agonists of 5-HT2C...
June 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28634338/coumarin-benzimidazole-hybrids-as-a-potent-antimicrobial-agent-synthesis-and-biological-elevation
#20
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
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