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https://www.readbyqxmd.com/read/29456890/a-six-year-grazing-exclusion-changed-plant-species-diversity-of-a-stipa-breviflora-desert-steppe-community-northern-china
#1
Xing Wang, Xinguo Yang, Lei Wang, Lin Chen, Naiping Song, Junlong Gu, Yi Xue
Excluding grazers is one of most efficient ways to restore degraded grasslands in desert-steppe communities, but may negatively affect the recovery of plant species diversity. However, diversity differences between grazed and fenced grasslands in desert-steppe are poorly known. In a Stipa breviflora desert steppe community in Northern China, we established six plots to examine spatial patterns of plant species diversity under grazed and fenced conditions, respectively. We addressed three aspects of species diversity: (1) The logistic, exponential and power models were used to describe the species-area curve (SAR)...
2018: PeerJ
https://www.readbyqxmd.com/read/29456791/nonacidic-chemotype-possessing-n-acylated-piperidine-moiety-as-potent-farnesoid-x-receptor-fxr-antagonists
#2
Naoki Teno, Yukiko Yamashita, Yusuke Iguchi, Ko Fujimori, Mizuho Une, Tomoko Nishimaki-Mogami, Takie Hiramoto, Keigo Gohda
Farnesoid X receptor (FXR) plays a major role in the control of cholesterol metabolism. Antagonizing transcriptional activity of FXR is an effective means to treat the relevant metabolic syndrome. Some of antagonists so far have the charged functions; however, they may negatively affect the pharmacokinetics. We describe herein a structure-activity relationship (SAR) exploration of nonacidic FXR antagonist 6 focusing on two regions in the structure and biological evaluation of nonacidic 10 with the characteristic N -acylated piperidine group obtained from SAR studies...
February 8, 2018: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29456260/rf-safety-evaluation-of-a-breast-tissue-expander-device-for-mri-numerical-simulation-and-experiment
#3
Bu S Park, Amir Razjouyan, Leonardo M Angelone, Brent McCright, Sunder S Rajan
This study describes the MRI-related radio frequency (RF) safety evaluation of breast tissue expander devices to establish safety criteria. Numerical simulations and experimental measurements were performed at 64 MHz with a gel phantom containing a breast expander. Additionally, computational modeling was performed (64 and 128 MHz) with an adult female model, containing a virtually implanted breast tissue expander device for four imaging landmark positions. The presence of the breast tissue expander device led to significant alterations in specific absorption rate (SAR) and|B1 + |distributions...
October 2017: IEEE Transactions on Electromagnetic Compatibility
https://www.readbyqxmd.com/read/29456259/improvement-of-electromagnetic-field-distributions-using-high-dielectric-constant-hdc-materials-for-ctl-spine-mri-numerical-simulations-and-experiments
#4
Bu S Park, Brent McCright, Leonardo M Angelone, Amir Razjouyan, Sunder S Rajan
This study investigates the use of pads with high dielectric constant (HDC) materials to alter electromagnetic field distributions in patients during magnetic resonance imaging (MRI). The study was performed with numerical simulations and phantom measurements. An initial proof-of-concept and validation was performed using a phantom at 64 MHz, showing increases of up to 10% in electromagnetic field when using distilled water as the high dielectric material. Additionally, numerical simulations with computational models of human anatomy were performed at 128 MHz...
October 2017: IEEE Transactions on Electromagnetic Compatibility
https://www.readbyqxmd.com/read/29454915/synthesis-of-n-1-6-acetamido-5-phenylpyrimidin-4-yl-piperidin-3-yl-amide-derivatives-as-potential-inhibitors-for-mitotic-kinesin-spindle-protein
#5
P Muthuraja, M Himesh, S Prakash, U Venkatasubramanian, P Manisankar
Kinesin Spindle Protein (KSP) or Eg5 is an essential kinesin that is involved in spindle separation process during mitosis and also unregulated in certain cancer cells. Inhibitors of this enzyme have proved to be effective to block spindle separation followed by mitotic arrest and apoptosis of the cancer cells. Since this enzyme has two allosteric inhibitor binding sites, it's an excellent target for developing drugs for cancer chemotherapy. Many pyrimidine derivatives have been proved to be active against cancer and other enzymes...
February 10, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29454637/tools-to-study-pathogen-host-interactions-in-bats
#6
REVIEW
Arinjay Banerjee, Vikram Misra, Tony Schountz, Michelle L Baker
Bats are natural reservoirs for a variety of emerging viruses that cause significant disease in humans and domestic animals yet rarely cause clinical disease in bats. The co-evolutionary history of bats with viruses has been hypothesized to have shaped the bat-virus relationship, allowing both to exist in equilibrium. Progress in understanding bat-virus interactions and the isolation of bat-borne viruses has been accelerated in recent years by the development of susceptible bat cell lines. Viral sequences similar to severe acute respiratory syndrome coronavirus (SARS-CoV) have been detected in bats, and filoviruses such as Marburg virus have been isolated from bats, providing definitive evidence for the role of bats as the natural host reservoir...
February 15, 2018: Virus Research
https://www.readbyqxmd.com/read/29453796/using-a-hospital-admission-survey-to-estimate-the-burden-of-influenza-associated-severe-acute-respiratory-infection-in-one-province-of-cambodia-methods-used-and-lessons-learned
#7
Rebekah J Stewart, Sovann Ly, Borann Sar, Vanra Ieng, Seng Heng, Kheng Sim, Chiedza Machingaidze, Katherine Roguski, Erica Dueger, Ann Moen, Reiko Tsuyuoka, A Danielle Iuliano
BACKGROUND: Understanding the burden of influenza-associated severe acute respiratory infection (SARI) is important for setting national influenza surveillance and vaccine priorities. Estimating influenza-associated SARI rates requires hospital-based surveillance data and a population-based denominator, which can be challenging to determine. OBJECTIVES: We present an application of the World Health Organization's recently developed manual (WHO Manual) including hospital admission survey (HAS) methods for estimating the burden of influenza-associated SARI, with lessons learned to help others calculate similar estimates...
February 16, 2018: Influenza and Other Respiratory Viruses
https://www.readbyqxmd.com/read/29453389/toxicity-classification-of-oxide-nanomaterials-effects-of-data-gap-filling-and-pchem-score-based-screening-approaches
#8
My Kieu Ha, Tung Xuan Trinh, Jang Sik Choi, Desy Maulina, Hyung Gi Byun, Tae Hyun Yoon
Development of nanotoxicity prediction models is becoming increasingly important in the risk assessment of engineered nanomaterials. However, it has significant obstacles caused by the wide heterogeneities of published literature in terms of data completeness and quality. Here, we performed a meta-analysis of 216 published articles on oxide nanoparticles using 14 attributes of physicochemical, toxicological and quantum-mechanical properties. Particularly, to improve completeness and quality of the extracted dataset, we adapted two preprocessing approaches: data gap-filling and physicochemical property based scoring...
February 16, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29453190/testing-behavior-change-techniques-to-encourage-primary-care-physicians-to-access-cancer-screening-audit-and-feedback-reports-protocol-for-a-factorial-randomized-experiment-of-email-content
#9
Gratianne Vaisson, Holly O Witteman, Zachary Bouck, Caroline A Bravo, Laura Desveaux, Diego Llovet, Justin Presseau, Marianne Saragosa, Monica Taljaard, Shama Umar, Jeremy M Grimshaw, Jill Tinmouth, Noah M Ivers
BACKGROUND: Cancer Care Ontario's Screening Activity Report (SAR) is an online audit and feedback tool designed to help primary care physicians in Ontario, Canada, identify patients who are overdue for cancer screening or have abnormal results requiring follow-up. Use of the SAR is associated with increased screening rates. To encourage SAR use, Cancer Care Ontario sends monthly emails to registered primary care physicians announcing that updated data are available. However, analytics reveal that 50% of email recipients do not open the email and less than 7% click the embedded link to log in to their report...
February 16, 2018: JMIR Research Protocols
https://www.readbyqxmd.com/read/29452840/borrelidins-f-i-cytotoxic-and-cell-migration-inhibiting-agents-from-mangrove-derived-streptomyces-rochei-scsio-zj89
#10
Jianbin Sun, Junli Shao, Changli Sun, Yongxiang Song, Qinglian Li, Laichun Lu, Yunfeng Hu, Chun Gui, Hua Zhang, Jianhua Ju
Borrelidin A (1) is produced by several species of Streptomyces and within its bioactive scaffold, the vinylic nitrile moiety is essential for activity. We report herein newly discovered members of the borrelidin family, borrelidin F (2), borrelidin G (3), borrelidin H (4) and borrelidin I (5); all were isolated from Streptomyces rochei SCSIO ZJ89 originating from a mangrove-derived sediment sample. These structurally diverse metabolites enabled a number of new structure-activity relationships (SARs) to be identified, especially with respect to the different configurations at the C11-OH and C12-C15 double bonds for which the absolute configurations were determined using spectroscopic methods...
February 7, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29452839/development-of-selective-inhibitors-for-the-treatment-of-rheumatoid-arthritis-r-3-3-methyl-7h-pyrrolo-2-3-d-pyrimidin-4-yl-amino-pyrrolidin-1-yl-3-oxopropanenitrile-as-a-jak1-selective-inhibitor
#11
Chieyeon Chough, Misuk Joung, Sunmin Lee, Jaemin Lee, Jong Hoon Kim, B Moon Kim
A series of 3(R)-aminopyrrolidine derivatives were designed and synthesized for JAK1-selective inhibitors through the modification of tofacitinib's core structure, (3R,4R)-3-amino-4-methylpiperidine. From the new core structures, we selected (R)-N-methyl-N-(pyrrolidin-3-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine as a scaffold for further SAR studies. From biochemical enzyme assays and liver microsomal stability tests, (R)-3-(3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)-3-oxopropanenitrile (6) was chosen for further in vivo test through oral administration...
February 3, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29451794/-s-2-amino-3-5-methyl-3-hydroxyisoxazol-4-yl-propanoic-acid-ampa-and-kainate-receptor-ligands-further-exploration-of-bioisosteric-replacements-structural-and-biological-investigation
#12
Simone Brogi, Margherita Brindisi, Stefania Butini, Giridhar Uttam Kshirsagar, Samuele Maramai, Giulia Chemi, Sandra Gemma, Giuseppe Campiani, Ettore Novellino, Paolo Fiorenzani, Jessica Pinassi, Anna Maria Aloisi, Mikko Gynther, Raminta Venskutonyte, Liwei Han, Karla Frydenvang, Jette Sandholm Kastrup, Darryl S Pickering
Starting from 1-4 and 7 structural templates, analogues based on bioisosteric replacements (5a-c vs 1, 2 and 6 vs 7) were synthesized for completing the SAR analysis. Interesting binding properties at GluA2, GluK1 and GluK3 receptors were discovered. The requirements for GluK3 interaction were elucidated determining the X-ray structures of the GluK3-LBD with 2 and 5c and by computational studies. Antinociceptive potential was demonstrated for GluK1 partial agonist 3 and antagonist 7 (2 mg/kg ip).
February 16, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29451785/structure-function-evaluation-of-imidazopyridine-derivatives-selective-for-%C3%AE-subunit-containing-%C3%AE-aminobutyric-acid-type-a-gaba-a-receptors
#13
Kirsten Yakoub, Sascha Jung, Christian Sattler, Helen Damerow, Judith Weber, Annika Kretzschmann, Aylin S Cankaya, Markus Piel, Frank Rösch, Anne S Haugaard, Bente Frølund, Tanja Schirmeister, Hartmut Lüddens
Delta selective compounds 1 and 2 (DS1, compound 22; DS2, compound 16) were introduced as functionally selective modulators of δ-containing GABA receptors type A (GABAAR). In our hands [ 3 H]EBOB binding experiments with recombinant GABA A R using compound 22, showed no proof of δ-selectivity, though a minimally higher preference with respect to potency for α4β3δ and α6β2/3δ receptors. In order to delineate the structural determinant for δ-preference, we synthesized 25 derivatives of DS1 and DS2, and investigated their structure-activity relationship (SAR)...
February 16, 2018: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29448140/synthesis-and-structure-activity-relationships-of-asymmetric-dimeric-%C3%AE-carboline-derivatives-as-potential-antitumor-agents
#14
Liang Guo, Wei Chen, Rihui Cao, Wenxi Fan, Qin Ma, Jie Zhang, Bin Dai
A series of newly asymmetric dimeric β-carbolines with a spacer of 4-6 methylene units between the indole nitrogen and the harmine oxygen were synthesized. Structures of all the novel synthesized compounds were confirmed by their spectral and analytical studies. All of the synthesized compounds were screened for their in vitro cytotoxic activity against nine cancer cell lines. The results revealed that compounds 7c, 7o and 7s exhibited the highest cytotoxic activities with IC 50 values of less than 20 μM against the tumor cell lines tested...
February 7, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29447979/jatrophanes-as-promising-multidrug-resistance-modulators-advances-of-structure-activity-relationships
#15
Jun Li, Wen-Qiong Wang, Shuai Tang, Wei-Bin Song, Li-Jiang Xuan
The phytochemical study of Euphorbia helioscopia afforded euphornin (1) in a large amount. Alkaline hydrolysis of 1 using potassium carbonate yielded the main product monodeacetyleuphornin (2), whose structural modification at 14-OH gave rise to 21 acylated derivatives euphornoate A-U (3-23). Thus, a mini compound library of jatrophanes was established to screen for MDR modulators. Biological studies clearly demonstrated the effect of C-14 pattern modification in MDR reversal activity and several compounds with RF values over 300 fold at 20 μM (6, 16, 20, 22, 23) were thought to be promising MDR modulators...
February 12, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29446718/current-trends-and-future-directions-of-fluoroquinolones
#16
Hamada H H Mohammed, Gamal El-Din A A Abuo-Rahma, Samar H Abbas, El-Shimaa M N Abdelhafez
Fluoroquinolones represent an interesting synthetic class of antimicrobial agents with broad spectrum and potent activity. Since the discovery of nalidixic acid, the prototype of quinolones, several structural modifications to the quinolone nucleus have been carried out for improvement of potency, spectrum of activity, and to understand their structure activity relationship (SAR). The C-7 substituent was reported to have a major impact on the activity. Accordingly, Substitution at C-7 or its N-4-piperazinyl moiety was found to affect potency, bioavailability, and physicochemical properties...
February 14, 2018: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/29444267/safety-of-laser-interstitial-thermal-therapy-in-patients-with-pacemakers
#17
Sanjeet S Grewal, Krzysztof R Gorny, Christopher P Favazza, Robert E Watson, Timothy J Kaufmann, Jamie J Van Gompel
BACKGROUND AND IMPORTANCE: Laser interstitial thermal therapy (LiTT) has increasingly been used as a treatment option for medically refractory epilepsy, tumors, and radiation necrosis. The use of LiTT requires intraoperative magnetic resonance (MR) thermography. This can become an issue in patients with other implanted therapeutic devices such as pacemakers and vagal nerve stimulators due to concerns regarding increases in the specific absorption rate (SAR). This is a technical case report demonstrating a successfully and safely performed LiTT in a 1...
February 10, 2018: Operative Neurosurgery (Hagerstown, Md.)
https://www.readbyqxmd.com/read/29441933/synthesis-chemical-behavior-structure-elucidation-and-inos-inhibitory-activity-of-1-substituted-3-methylsulfanyl-5-6-7-8-tetrahydro-1-h-1-2-4-triazolo-1-2-a-pyridazines
#18
U Schulz, A Grossmann, F Wilde, M Freitag, C Lemmerhirt, C Schulzke, A Link, O Morgenstern
Novel slim and shapely sp3-rich nitrogen containing heterocyclic ring systems are sought-after platforms for the expansion of molecular diversity in lead discovery. The present work describes the synthesis and characterization of a series of derivatives of hitherto unknown 3-methylsulfanyl-5,6,7,8-tetrahydro-1H-[1,2,4]triazolo[1,2-a]pyridazines 2. This approach was guided by a computational study, aiming at an optimization of previously reported [1,2,4]triazolo[1,2-a]pyridazine-1-thiones 1 known to inhibit the inducible nitric oxide synthase (iNOS)...
July 3, 2017: Die Pharmazie
https://www.readbyqxmd.com/read/29440667/poleward-upgliding-siberian-atmospheric-rivers-over-sea-ice-heat-up-arctic-upper-air
#19
Kensuke K Komatsu, Vladimir A Alexeev, Irina A Repina, Yoshihiro Tachibana
We carried out upper air measurements with radiosondes during the summer over the Arctic Ocean from an icebreaker moving poleward from an ice-free region, through the ice edge, and into a region of thick ice. Rapid warming of the Arctic is a significant environmental issue that occurs not only at the surface but also throughout the troposphere. In addition to the widely accepted mechanisms responsible for the increase of tropospheric warming during the summer over the Arctic, we showed a new potential contributing process to the increase, based on our direct observations and supporting numerical simulations and statistical analyses using a long-term reanalysis dataset...
February 13, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29440212/scoping-review-on-the-use-of-socially-assistive-robot-technology-in-elderly-care
#20
Jordan Abdi, Ahmed Al-Hindawi, Tiffany Ng, Marcela P Vizcaychipi
OBJECTIVE: With an elderly population that is set to more than double by 2050 worldwide, there will be an increased demand for elderly care. This poses several impediments in the delivery of high-quality health and social care. Socially assistive robot (SAR) technology could assume new roles in health and social care to meet this higher demand. This review qualitatively examines the literature on the use of SAR in elderly care and aims to establish the roles this technology may play in the future...
February 12, 2018: BMJ Open
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