Read by QxMD icon Read


Beena Negi, Prija Poonan, Mohammad Fawad Ansari, Deepak Kumar, Sakshi Aggarwal, Ramandeep Singh, Amir Azam, Diwan S Rawat
A series of 22 novel metronidazole-triazole-styryl hybrids were synthesized and evaluated for their in vitro antiamoebic activity against HM1: IMSS strain of Entamoeba histolytica. Some of the hybrids were found to be more active (IC50  = 0.12-0.35 μM) than the reference drug metronidazole (IC50  = 1.79 μM). The most active compounds were found to be non-toxic (up to 50 μM) against the Vero cells showing a good safety profile of these hybrids. The docking and ADMET studies were also conducted to investigate the probable mode of action...
March 13, 2018: European Journal of Medicinal Chemistry
Cornelia Wiegand, Andrea Völpel, Andrea Ewald, Markko Remesch, Jan Kuever, Janine Bauer, Stefanie Griesheim, Carolin Hauser, Julian Thielmann, Silke Tonndorf-Martini, Bernd W Sigusch, Jürgen Weisser, Ralf Wyrwa, Peter Elsner, Uta-Christina Hipler, Martin Roth, Carolin Dewald, Claudia Lüdecke-Beyer, Jörg Bossert
Bactericidal materials gained interest in the health care sector as they are capable of preventing material surfaces from microbial colonization and subsequent spread of infections. However, commercialization of antimicrobial materials requires proof of their efficacy, which is usually done using in vitro methods. The ISO 22196 standard (Japanese test method JIS Z 2801) is a method for measuring the antibacterial activity of daily goods. As it was found reliable for testing the biocidal activity of antimicrobially active materials and surface coatings most of the laboratories participating in this study used this protocol...
2018: PloS One
Patrick Weber, Seyed A Nasseri, Bettina M Pabst, Ana Torvisco, Philipp Müller, Eduard Paschke, Marion Tschernutter, Werner Windischhofer, Stephen G Withers, Tanja M Wrodnigg, Arnold E Stütz
From 1,2;3,4-di- O -isopropylidene-d-galactopyranose, a preliminary series of highly functionalized amino(hydroxymethyl)cyclopentanes was easily available. These amine-containing basic carbasugars featuring the d- galacto configuration are potent inhibitors of the GH20 β-d-hexosaminidases probed and may bear potential as regulators of N -acetyl-d-hexosaminidase activities in vivo.
March 20, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
He Zhou, Hyoki Lee, Jessica Lee, Michael Schwenk, Bijan Najafi
Practical tools which can be quickly administered are needed for measuring subtle changes in cognitive-motor performance over time. Frailty together with cognitive impairment, or 'cognitive frailty', are shown to be strong and independent predictors of cognitive decline over time. We have developed an interactive instrumented trail-making task (iTMT) platform, which allows quantification of motor planning error (MPE) through a series of ankle reaching tasks. In this study, we examined the accuracy of MPE in identifying cognitive frailty in older adults...
March 20, 2018: Sensors
Quanwei Zhang, Qi Wang, Jishang Gong, Jiaxing Du, Yong Zhang, Xingxu Zhao
Insulin-like growth factor 2 (IGF2) recapitulates many of the activities of insulin and promotes differentiation of myoblasts and osteoblasts, which likely contribute to genetic variations of growth potential. However, little is known about the functions and signaling properties of IGF2 variants in yaks. The over-expression vector and knockdown sequence of yak IGF2 were transfected into yak fibroblasts, and the effects were detected by a series of assays. IGF2 expression in yak muscle tissues was significantly lower than that of other tissues...
March 20, 2018: Genes
Jin Liu, Yu Chen, Jing-Ya Li, Cheng Luo, Jia Li, Kai-Xian Chen, Xu-Wen Li, Yue-Wei Guo
Phidianidines A and B are two novel marine indole alkaloids bearing an uncommon 1,2,4-oxadiazole ring and exhibiting various biological activities. Our previous research showed that the synthesized phidianidine analogs had the potential to inhibit the activity of protein tyrosine phosphatase 1B (PTP1B), a validated target for Type II diabetes, which indicates that these analogs are worth further structural modification. Therefore, in this paper, a series of phidianidine derivatives were designed and rapidly synthesized with a function-oriented synthesis (FOS) strategy...
March 20, 2018: Marine Drugs
Ga Ram Kim, Ji Soo Choi, Boo-Kyung Han, Jeong Eon Lee, Seok Jin Nam, Eun Young Ko, Eun Sook Ko, Se Kyung Lee
Purpose To evaluate the value of preoperative axillary ultrasonography (US) for preventing unnecessary axillary lymph node dissection after sentinel lymph node (SLN) biopsy in a large series of patients with early-stage breast cancers treated with both breast-conserving surgery and SLN biopsy. Materials and Methods From March 2009 to February 2013, 1802 patients who underwent breast-conserving surgery for clinical T1-2/N0 cancers and SLN biopsy with or without axillary lymph node dissection were included. Preoperative axillary US results and clinical-pathologic variables were compared according to the status of non-SLN metastasis...
March 20, 2018: Radiology
Akira Murakami, Ayami Shibahashi, Ryota Iwasaki, Mifumi Kawabe, Mami Murakami, Hiroki Sakai, Takashi Mori
Inflammatory colorectal polyps (ICRP), which are more commonly recognized in miniature dachshunds, are thought to represent an immune-mediated disease. This retrospective case series describes six miniature dachshunds with refractory ICRP, who were treated with chlorambucil (CLB) combined with firocoxib or prednisolone. Improvement in clinical manifestations was seen in five of the six dogs by the end of the study period; four were treated with CLB/firocoxib and one with CLB/prednisolone. One dog had nonregenerative anemia after 23 mo of treatment with CLB, but whether there was a causative relationship was unclear...
March 20, 2018: Journal of the American Animal Hospital Association
Deng-Yuan Li, Zheng-Lu Huang, Pei-Nian Liu
The heterobicyclic core retained hydroarylation of oxa/azabenzonorbornadienes with quinoline N-oxides has been achieved under rhodium catalysis, giving quinoline N-oxide substituted heterobicyclic structures with excellent regioselectivity and in good yields. As the first example of the direct introduction of quinoline N-oxides onto heterobicyclic structures, the strained heterobicyclic core was well retained in the reaction. The products could be successfully transformed into a series of useful compounds, including epibatidine analogues...
March 20, 2018: Organic Letters
Sean Conroy, Nicholas D Kindon, Jacqueline Glenn, Leigh A Stoddart, Richard James Lewis, Stephen J Hill, Barrie Kellam, Michael John Stocks
The human P2Y2 receptor (hP2Y2R) is a G protein-coupled receptor that shows promise as a therapeutic target for many important conditions including anti-metastatic cancer therapy and more recently for the treatment of idiopathic pulmonary fibrosis. As such, there is a need for new hP2Y2R antagonists and molecular probes to study this receptor. Herein, we report the development of a new series of non-nucleotide hP2Y2R antagonists leading to the discovery of a series of fluorescent ligands containing different linkers and fluorophores based on the known, non-nucleotide hP2Y2R antagonist AR-C118925 (1)...
March 20, 2018: Journal of Medicinal Chemistry
Malcolm Spain, Joseph K-H Wong, Gayathri Nagalingam, James M Batten, Elinor Hortle, Stefan Oehlers, Xiao Fan Jiang, Hasini E Murage, Jack T Orford, Patrick Crisologo, James A Triccas, Peter J Rutledge, Matthew H Todd
We recently reported the discovery of non-toxic cyclam-derived compounds that are active against drug-resistant Mycobacterium tuberculosis. In this paper we report exploration of the structure-activity relationship for this class of compounds, identifying several simpler compounds with comparable activity. The most promising compound identified, possessing significantly improved water solubility, displayed high levels of bacterial clearance in an in vivo zebrafish embryo model, suggesting this compound series has promise for in vivo treatment of tuberculosis...
March 20, 2018: Journal of Medicinal Chemistry
Junghyun L Suh, Brian Watts, Jacob I Stuckey, Jacqueline L Norris-Drouin, Stephanie H Cholensky, Bradley M Dickson, Yi An, Sebastian Mathea, Eidarus Salah, Stefan Knapp, Abid Khan, Alexander T Adams, Brian D Strahl, Cari A Sagum, Mark T Bedford, Lindsey I James, Dmitri B Kireev, Stephen V Frye
Multivalent binding is an efficient means to enhance the affinity and specificity of chemical probes targeting multi-domain proteins in order to study their function and role in disease. While the theory of multivalent binding is straightforward, physical and structural characterization of bivalent binding encounters multiple technical difficulties. We present a case study where a combination of experimental techniques and computational simulations was used to comprehensively characterize the binding and structure-affinity relationships for a series of Bromosporine-based bivalent bromodomain ligands with a bivalent protein, Transcription Initiation Factor TFIID subunit 1 (TAF1)...
March 20, 2018: Biochemistry
Oğuz Ahmet Hasdemir, Serhat Tokgöz, Fulya Köybaşıoğlu, Harun Karabacak, Cüneyt Yücesoy, Gökşen İnanç İmamoğlu
BACKGROUND: Metaplastic carcinoma of the breast (MpBC) is defined as a group of heterogeneous malignant neoplasms that contain glandular and non-glandular components with mixed epithelial and mesenchymal differentiations. OBJECTIVES: The aim of this study was to research the clinical and pathological characteristics of MpBC determining its rank among all breast cancers. MATERIAL AND METHODS: Metaplastic carcinoma of the breast was found in 7 out of 1,164 patients who had been diagnosed with breast cancer within the period of 12 years in our hospital...
March 19, 2018: Advances in Clinical and Experimental Medicine: Official Organ Wroclaw Medical University
Shuangjian He, Xiaoyi Huang, Bin Yan, Jian Zhu, Nirong Bao, Jianning Zhao
To evaluate the biomechanical and clinical results of modified separate vertical wiring technique (SVW) for inferior pole patellar fracture repair we conducted a finite element biomechanical study using 2 fixation methods and evaluated a clinical series of eleven patients. The modified SVW technique was an effective, safe and simple method that can provide stable fixation for early exercise with excellent functional results in fixing inferior pole patella fractures.
April 2018: Journal of Orthopaedic Trauma
Joseph Christensen, Sean Spence, David Watson, Anjan Shah, Benjamin Maxson, Anthony Infante, Roy Sanders, Hassan R Mir
OBJECTIVE: To review the orthopaedic injuries from watercraft treated surgically at our institution and report the mechanisms, fractures, and complications encountered. DESIGN: Retrospective case series. SETTING: Level I trauma center. PATIENTS/PARTICIPANTS: There were 216 fractures from watercraft in 146 patients. Average age was 33 years (range 4-78 years), there were 68% males (99/146), and 16% of the injuries occurred in children...
April 2018: Journal of Orthopaedic Trauma
Santiago Mencía, Alba Palacios, Miriam García, Ana M Llorente, Olga Ordóñez, Blanca Toledo, Jesús López-Herce
OBJECTIVES: To analyze the effectiveness of inhaled sevoflurane in critically ill children with challenging sedation. DESIGN: Prospective case series. SETTING: Two PICUs of university hospitals in Spain. INTERVENTIONS: Prospective observational study and exploratory investigation conducted in two PICUs in Madrid, Spain, over a 6-year period. Children treated with inhaled sevoflurane due to difficult sedation were included...
March 19, 2018: Pediatric Critical Care Medicine
Rénuka S Birbal, Shugi Hsien, Vasiliki Zygoura, Jack S Parker, Lisanne Ham, Korine van Dijk, Isabel Dapena, Lamis Baydoun, Gerrit R J Melles
PURPOSE: To report the mid-term outcomes of hemi-Descemet membrane endothelial keratoplasty (hemi-DMEK) performed for Fuchs endothelial corneal dystrophy (FECD). METHODS: In this prospective, interventional case series, we evaluated clinical outcomes of 10 eyes from 10 patients who underwent hemi-DMEK for FECD. Main outcome measures were best-corrected visual acuity (BCVA), endothelial cell density (ECD), central pachymetry, and postoperative complications. RESULTS: At 1 year postoperatively, 7/7 eyes (excluding 2 eyes with low visual potential) reached a BCVA of ≥20/40 (≥0...
March 19, 2018: Cornea
Simone Zanella, Francesco Buccelletti, Francesco Franceschi, Claudio Ramponi, Federica Spagnolli, Gianpaolo Sacchetti, Giovanna Oliva
BACKGROUND: To evaluate the usefulness of Arnica compositum (AC) + Acidum nitricum (AN) + Hekla lava (HL) ointment in Emergency Medicine Department (EMD) as alternative non-pharmacological local treatment of patients with symptomatic calcific periarthritis of the shoulder (CPS) and to compare the effectiveness of this mixture against AC ointment alone. METHODS: A series of 41 consecutive patients (20 women, 19 men, median age 49 years, range 25-80 years) with non-traumatic painful unilateral CPS were randomly assigned to receive local treatment with AC+AN+HL ointment mixture (Group A, cases, N=21) or AC ointment alone (Group B, controls, N=20)...
March 19, 2018: Reviews on Recent Clinical Trials
Miran Brvar, Ming Yin Chan, Andrew H Dawson, Richard R Ribchester, Michael Eddleston
INTRODUCTION: Treatment of acute organophosphorus or carbamate insecticide self-poisoning is often ineffective, with tens of thousands of deaths occurring every year. Researchers have recommended the addition of magnesium sulfate or calcium channel blocking drugs to standard care to reduce acetylcholine release at cholinergic synapses. OBJECTIVE: We aimed to review systematically the evidence from preclinical studies in animals exposed to organophosphorus or carbamate insecticides concerning the efficacy of magnesium sulfate and calcium channel blocking drugs as therapy compared with placebo in reducing mortality or clinical features of poisoning...
March 20, 2018: Clinical Toxicology
Yohan Ko, Yechan Kim, Chanyong Lee, Youbin Kim, Yongseok Jun
Organometallic halide perovskite solar cells (PSCs) have unique photovoltaic properties for use in next-generation solar-energy harvesting systems. The highest efficiency PSCs reached 22.1% at a lab scale of <0.1 cm2 device area. Thus, scaling up is the next step toward commercialization, but the difficulty in controlling the quality of large-area perovskite thin films remains a fundamental challenge. It has also been frequently reported that the J-V hysteresis is intensified in PSCs with areas larger than 1 cm2 ...
March 20, 2018: ACS Applied Materials & Interfaces
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"