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https://www.readbyqxmd.com/read/28448900/dual-responsive-magnetic-composite-nanogels-for-thermo-chemotherapy
#1
S Indulekha, P Arunkumar, D Bahadur, R Srivastava
With the onset of hyperthermia and their advantage in increasing vascular perfusion and permeability in the cancer milieu, thermo-responsive polymers have become an attractive candidate for designing therapeutic nano-vehicles for targeted on-demand delivery of bioactive agents. For this purpose, we developed a dual (thermo- and pH-) responsive nanotherapeutic composite system rendering a combinational therapy of hyperthermia mediated drug delivery. This composite system comprises of magnetic chitosan-g-PNVCL (MCP) polymeric nanogels loaded with anticancer drug, Doxorubicin (DOX)...
April 19, 2017: Colloids and Surfaces. B, Biointerfaces
https://www.readbyqxmd.com/read/28448510/manure-and-tillage-use-in-remediation-of-eroded-land-and-impacts-on-soil-chemical-properties
#2
Maysoon M Mikha, Joseph G Benjamin, Merle F Vigil, David J Poss
Soil loss through wind and water erosion is an ongoing problem in semiarid regions. A thin layer of top soil loss over a hectare of cropland could be corresponding to tons of productive soil loss per hectare. The objectives of this study were to evaluate the influence of beef feedlot manure, tillage and legume grass mixtures on changes in soil quality and nutrient components. The study was initiated in 2006 on an eroded site near Akron, Colorado, on a Norka-Colby very-fine sandy loam (fine-silty, mixed, mesic, Aridic, Argiustolls)...
2017: PloS One
https://www.readbyqxmd.com/read/28446917/shoot-the-message-not-the-messenger-combating-pathogenic-virulence-in-plants-by-inhibiting-quorum-sensing-mediated-signaling-molecules
#3
REVIEW
Ganesh Alagarasan, Kumar S Aswathy
Immunity, virulence, biofilm formation, and survival in the host environment are regulated by the versatile nature of density dependent microbial cell signaling, also called quorum sensing (QS). The QS molecules can associate with host plant tissues and, at times, cause a change in its gene expression at the downstream level through inter-kingdom cross talking. Progress in controlling QS through fungicide/bactericide in pathogenic microscopic organisms has lead to a rise of antibiotic resistance pathogens. Here, we review the application of selective quorum quenching (QQ) endophytes to control phytopathogens that are shared by most, if not all, terrestrial plant species as well as aquatic plants...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28445411/discovery-of-farnesoid-x-receptor-antagonists-based-on-a-library-of-oleanolic-acid-3-o-esters-through-diverse-substituent-design-and-molecular-docking-methods
#4
Shao-Rong Wang, Tingting Xu, Kai Deng, Chi-Wai Wong, Jinsong Liu, Wei-Shuo Fang
The pentacyclic triterpene oleanolic acid (OA, 1) with known farnesoid X receptor (FXR) modulatory activity was modified at its C-3 position to find new FXR-interacting agents. A diverse substitution library of OA derivatives was constructed in silico through a 2D fingerprint similarity cluster strategy. With further docking analysis, four top-scored OA 3-O-ester derivatives were selected for synthesis. The bioassay results indicated that all four compounds 3 inhibited chenodeoxycholic acid (CDCA)-induced FXR transactivation in a concentration-dependent mode...
April 26, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28443517/1-3-4-oxadiazoles-as-telomerase-inhibitor-potential-anticancer-agents
#5
Shalini Bajaj, Partha Pratim Roy, Jagadish Singh
Cancer is a rapidly growing disease of current era which poses a major life threaten situation to human beings. Continuous research is going on in the direction to develop effective molecules for the treatment of the cancer. These efforts include searching of more active heterocyclic compounds possessing potential anti-cancer activity. The 1,3,4-Oxadiazole scaffold is a five member heterocyclic ring having versatile activities and created interest for synthetic organic and medicinal chemists for the designing of novel compounds having anti-cancer activity...
April 24, 2017: Anti-cancer Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/28443114/tadir1-2-a-wheat-ortholog-of-lipid-transfer-protein-atdir1-contributes-to-negative-regulation-of-wheat-resistance-against-puccinia-striiformis-f-sp-tritici
#6
Soyed M Ahmed, Peng Liu, Qinghe Xue, Changan Ji, Tuo Qi, Jia Guo, Jun Guo, Zhensheng Kang
Very few LTPs have been shown to act through plasma membrane receptors or to be involved in the hypersensitive response (HR). DIR1, a new type of plant LTP interacts with lipids in vitro, moves to distant tissues during systemic acquired resistance (SAR) and therefore is thought to be involved in long-distance signaling during SAR. However, the exact functions of DIR1 orthologs in cereal species under biotic and abiotic stresses have not been thoroughly defined. In this study, a novel wheat ortholog of the DIR1 gene, TaDIR1-2, was isolated from Suwon11, a Chinese cultivar of wheat and functionally characterized...
2017: Frontiers in Plant Science
https://www.readbyqxmd.com/read/28441993/randomized-placebo-controlled-study-of-cetirizine-and-loratadine-in-children-with-seasonal-allergic-rhinitis
#7
Anjuli S Nayak, William E Berger, Craig F LaForce, Eduardo R Urdaneta, Mitesh K Patel, Kathleen B Franklin, Mei-Miau Wu
BACKGROUND: Pharmacologic treatment is a mainstay of allergy therapy and many caregivers use over-the-counter antihistamines for the treatment of seasonal allergic rhinitis (SAR) symptoms in children. OBJECTIVE: To assess the efficacy and safety of cetirizine 10 mg syrup versus loratadine 10 mg syrup versus placebo syrup in a randomized double-blind study of children, ages 6-11 years, with SAR. METHODS: This randomized, double-blind, parallel-group, placebo-controlled study was conducted at 71 U...
May 1, 2017: Allergy and Asthma Proceedings:
https://www.readbyqxmd.com/read/28441580/the-computer-aided-discovery-of-novel-family-of-the-5-ht6-serotonin-receptor-ligands-among-derivatives-of-4-benzyl-1-3-5-triazine
#8
Dorota Łażewska, Rafał Kurczab, Małgorzata Więcek, Katarzyna Kamińska, Grzegorz Satała, Magdalena Jastrzębska-Więsek, Anna Partyka, Andrzej J Bojarski, Anna Wesołowska, Katarzyna Kieć-Kononowicz, Jadwiga Handzlik
The work describes a discovery of new chemical family of potent ligands for the 5-HT6 serotonin receptors. During the search for new histamine H4 receptor antagonists among 1,3,5-triazine derivatives, compound 2 (4-benzyl-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine) was found. Compound 2, weakly active for the H4 receptor but fitted in 3/4 of pharmacophore features of the 5-HT6R ligand, occurred to be a moderate 5-HT6R agent, useful as a lead structure for further modifications. A series of new derivatives (3-19) of the lead 2 was synthesized, evaluated in the radioligand binding assay (RBA) and explored in comprehensive molecular modelling, including both pharmacophore- and structure-based approaches with docking to the homology model of 5-HT6R...
April 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28441345/levels-and-distribution-of-pollutants-in-the-waters-of-an-aquatic-ecosystem-in-northern-mexico
#9
Jesús Manuel Ochoa-Rivero, Ana Victoria Reyes-Fierro, Ma Del Rosario Peralta-Pérez, Francisco Javier Zavala-Díaz de la Serna, Lourdes Ballinas-Casarrubias, Ivan Salmerón, Héctor Rubio-Arias, Beatriz A Rocha-Gutiérrez
The availability of good quality water resources is essential to ensure healthy crops and livestock. The objective of this study was to evaluate the level of pollution in Bustillos Lagoon in northern Mexico. Physical-chemical parameters like sodium, chloride, sulfate, electrical conductivity, nitrates, and the pesticide dichlorodiphenyltrichloroethane (DDT) were analyzed to determine the water quality available in the lagoon. Although DDT has been banned in several countries, it is still used for agricultural purposes in Mexico and its presence in this area had not been analyzed previously...
April 25, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28438710/a-purpose-built-neck-coil-for-black-blood-dante-prepared-carotid-artery-imaging-at-7t
#10
Konstantinos Papoutsis, Linqing Li, Jamie Near, Stephen Payne, Peter Jezzard
Atherosclerotic plaques in the bifurcation of the carotid arteries can pose a significant health risk due to possible plaque rupture and subsequent stroke. The assessment of plaques, and evaluation of the risk they pose, can be performed with Black-Blood (BB) vessel wall magnetic resonance imaging. However, resolution at standard clinical field strengths (up to 3T) is limited, hampering reliable assessment and diagnosis. The aim of this study was to investigate the benefits of 7T MRI using a BB application that has been successful at clinical field strengths...
April 21, 2017: Magnetic Resonance Imaging
https://www.readbyqxmd.com/read/28438633/structural-insights-into-the-interaction-of-coronavirus-papain-like-proteases-and-interferon-stimulated-gene-product-15-from-different-species
#11
Courtney M Daczkowski, John V Dzimianski, Jozlyn R Clasman, Octavia Goodwin, Andrew D Mesecar, Scott D Pegan
Severe Acute and Middle East Respiratory syndrome coronaviruses (SARS-CoV and MERS-CoV) encode multifunctional papain-like proteases (PLPs) that have the ability to process the viral polyprotein to facilitate RNA replication as well as antagonize the host innate-immune response. The latter function involves reversing post-translational modification of cellular proteins conjugated with either ubiquitin (Ub) or Ub-like interferon stimulated gene product 15 (ISG15). Ubiquitin is known to be highly conserved among eukaryotes but surprisingly ISG15 is highly divergent among animals...
April 21, 2017: Journal of Molecular Biology
https://www.readbyqxmd.com/read/28436655/investigating-the-antibacterial-activity-of-biphenylthiazoles-against-methicillin-and-vancomycin-resistant-staphylococcus-aureus-mrsa-and-vrsa
#12
Mohamed Hagras, Haroon Mohammad, Mohamed S Mandour, Youssef A Hegazy, Adel Ghiaty, Mohamed N Seleem, Abdelrahman S Mayhoub
Phenylthiazoles were reported previously as a new scaffold with antibacterial activity against an array of multidrug-resistant staphylococci. However, their promising antibacterial activity was hampered in large part by their short half-life due to excessive hepatic clearance. Close inspection of the structure-activity-relationships (SAR) of the phenylthiazoles revealed two important structural features necessary for antibacterial activity (a nitrogenous and a lipophilic component). Incorporating the nitrogenous part within a pyrimidine ring resulted in analogues with a prolonged half-life, while the biphenyl moiety revealed the most potent analogue 1b...
April 24, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28436164/synthesis-and-sar-study-of-novel-anticancer-protoflavone-derivatives-investigation-of-cytotoxicity-and-interaction-with-the-abcb1-and-abcg2-multidrug-efflux-transporters
#13
Balázs Dankó, Szilárd Tóth, Ana Martins, Vágvölgyi Máté, Norbert Kúsz, Joseph Molnár, Fang-Rong Chang, Yang-Chang Wu, Gergely Szakács, Attila Hunyadi
There is a constant need for new therapies against multidrug resistant (MDR) cancer. Natural compounds represent a promising class of novel anticancer agents. Recently, we have shown that protoflavones display activity in multidrug resistant cancer cell lines overexpressing the drug efflux pump P-glycoprotein. In the present study, 52 protoflavones, including 22 new derivatives were synthesized and tested against a panel of sensitive parental cells and their MDR derivatives obtained by transfection with the human ABCB1 or ABCG2 genes, or by adaptation to chemotherapeutics...
April 23, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28435885/phylogenomic-reconstruction-of-the-oomycete-phylogeny-derived-from-37-genomes
#14
Charley G P McCarthy, David A Fitzpatrick
The oomycetes are a class of microscopic, filamentous eukaryotes within the Stramenopiles-Alveolata-Rhizaria (SAR) supergroup which includes ecologically significant animal and plant pathogens, most infamously the causative agent of potato blight Phytophthora infestans. Single-gene and concatenated phylogenetic studies both of individual oomycete genera and of members of the larger class have resulted in conflicting conclusions concerning species phylogenies within the oomycetes, particularly for the large Phytophthora genus...
March 2017: MSphere
https://www.readbyqxmd.com/read/28435523/discovery-of-1-2-3-triazolo-4-5-d-pyrimidine-derivatives-as-novel-lsd1-inhibitors
#15
Zhong-Hua Li, Xue-Qi Liu, Peng-Fei Geng, Feng-Zhi Suo, Jin-Lian Ma, Bin Yu, Tao-Qian Zhao, Zhao-Qing Zhou, Chen-Xi Huang, Yi-Chao Zheng, Hong-Min Liu
Lysine specific demethylase 1 (LSD1) plays a pivotal role in regulating the lysine methylation. The aberrant overexpression of LSD1 has been reported to be involved in the progression of certain human malignant tumors. Abrogation of LSD1 with RNAi or small molecule inhibitors may lead to the inhibition of cancer proliferation and migration. Herein, a series of [1,2,3]triazolo[4,5-d]pyrimidine derivatives were synthesized and evaluated for their LSD1 inhibitory effects. The structure-activity relationship studies (SARs) were conducted by exploring three regions of this scaffold, leading to the discovery of compound 27 as potent LSD1 inhibitor (IC50 = 0...
April 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28434782/dimeric-isoxazolyl-1-4-dihydropyridines-have-enhanced-binding-at-the-multi-drug-resistance-transporter
#16
Scott A Steiger, Chun Li, Donald S Backos, Philip Reigan, N R Natale
A series of dimeric isoxazolyl-1,4-dihydropyridines (IDHPs) were prepared by click chemistry and examined for their ability to bind the multi-drug resistance transporter (MDR-1), a member of the ATP-binding cassette superfamily (ABC). Eight compounds in the present study exhibited single digit micromolar binding to this efflux transporter. One monomeric IDHP m-Br-1c, possessed submicromolar binding of 510nM at MDR-1. Three of the dimeric IDHPs possessed <1.5µM activity, and 4b and 4c were observed to have superior binding selectivity compared to their corresponding monomers verses the voltage gated calcium channel (VGCC)...
April 8, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28434764/novel-non-trimethoxylphenyl-piperlongumine-derivatives-selectively-kill-cancer-cells
#17
Youjun Zhang, Hao Ma, Yuelin Wu, Zhongli Wu, Zhengguang Yao, Wannian Zhang, Chunlin Zhuang, Zhenyuan Miao
Piperlongumine (PL) is a natural alkaloid with broad biological activities. Twelve analogues have been designed and synthesized with non-substituted benzyl rings or heterocycles in this work. Most of the compounds showed better anticancer activities than the parent PL without apparent toxicity in normal cells. Elevation of cellular ROS levels was one of the main anticancer mechanisms of these compounds. Cell apoptosis and cell cycle arrest for the best compound ZM90 were evaluated and similar mechanism of action with PL was demonstrated...
April 13, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28433681/n-aryl-n-ethyleneaminothioureas-effectively-inhibit-acetylcholinesterase-1-from-disease-transmitting-mosquitoes
#18
Sofie Knutsson, Tomas Kindahl, Cecilia Engdahl, Dariush Nikjoo, Nina Forsgren, Stanley Kitur, Fredrik Ekström, Luna Kamau, Anna Linusson
Vector control of disease-transmitting mosquitoes by insecticides has a central role in reducing the number of parasitic- and viral infection cases. The currently used insecticides are efficient, but safety concerns and the development of insecticide-resistant mosquito strains warrant the search for alternative compound classes for vector control. Here, we have designed and synthesized thiourea-based compounds as non-covalent inhibitors of acetylcholinesterase 1 (AChE1) from the mosquitoes Anopheles gambiae (An...
March 27, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28433680/organocatalyzed-and-mechanochemical-solvent-free-synthesis-of-novel-and-functionalized-bis-biphenyl-substituted-thiazolidinones-as-potent-tyrosinase-inhibitors-sar-and-molecular-modeling-studies
#19
Sadaf Mutahir, Muhammad Asim Khan, Islam Ullah Khan, Muhammad Yar, Muhammad Ashraf, Sidra Tariq, Ren-Long Ye, Bao-Jing Zhou
Eluding the involvement of solvents in organic synthesis and introducing environment friendly procedures can control environmental problems. A facile and an efficient solvent free mechanochemical method (grinding) is achieved to synthesize novel bis-biphenyl substituted thiazolidinones using non-toxic and cheap N-acetyl glycine (NAG). Organocatalytic condensation of a series of Schiff's bases bearing different substituents with thioglycolic acid produces a variety of thiazolidinones derivatives in good to excellent yield...
April 13, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28432813/targeting-on-poly-adp-ribose-polymerase-activity-with-dna-damaging-hybrid-lactam-steroid-alkylators-in-wild-type-and-brca1-mutated-ovarian-cancer-cells
#20
Dimitrios T Trafalis, Aikaterini Polonifi, Panayiotis Dalezis, Nikolaos Nikoleousakos, Sotirios Katsamakas, Vassiliki Sarli
Conjugated lactam-steroid alkylators (LSA), have been shown to exhibit superior activity at controlling cancer models and overlap drug resistance to conventional chemotherapy. Hybrid LSAs combine two active compounds in a single molecule and incorporate modified steroids bearing lactam moiety in one or more steroid rings functioning as vectors for cytotoxic agents. We first describe a novel class of LSAs that generate excellent anticancer activity against UWB1.289 and UWB1.289+BRCA1 human ovarian cancer cell lines...
April 22, 2017: Chemical Biology & Drug Design
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