keyword
MENU ▼
Read by QxMD icon Read
search

Seri

keyword
https://www.readbyqxmd.com/read/29793211/synthesis-and-evaluation-of-novel-triazolyl-quinoline-derivatives-as-potential-antileishmanial-agents
#1
Akanksha Upadhyay, Pragati Kushwaha, Sampa Gupta, Ranga Prasad Dodda, Karthik Ramalingam, Ruchir Kant, Neena Goyal, Koneni V Sashidhara
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover novel series of 25 compounds for the development of new antileishmanial agents. A series of triazolyl 2-methyl-4-phenylquinoline-3-carboxylate derivatives has been synthesized via click chemistry inspired molecular hybridization approach and evaluated against Leishmania donovani. Most of the screened derivatives exhibited significant in vitro anti-leishmanial activity against promastigote (IC50 ranging from 2...
May 12, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29793210/polypharmacological-profile-of-1-2-dihydro-2-oxo-pyridine-3-carboxamides-in-the-endocannabinoid-system
#2
Andrea Chicca, Chiara Arena, Simone Bertini, Francesca Gado, Elena Ciaglia, Mario Abate, Maria Digiacomo, Margherita Lapillo, Giulio Poli, Maurizio Bifulco, Marco Macchia, Tiziano Tuccinardi, Jürg Gertsch, Clementina Manera
The endocannabinoid system (ECS) represents one of the major neuromodulatory systems involved in different physiological and pathological processes. Multi-target compounds exert their activities by acting via multiple mechanisms of action and represent a promising pharmacological modulation of the ECS. In this work we report 4-substituted and 4,5-disubstituted 1,2-dihydro-2-oxo-pyridine-3-carboxamide derivatives with a broad spectrum of affinity and functional activity towards both cannabinoid receptors and additional effects on the main components of the ECS...
May 14, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29793143/oxidation-at-c-16-enhances-butyrylcholinesterase-inhibition-in-lupane-triterpenoids
#3
María Julia Castro, Victoria Richmond, María Belén Faraoni, Ana Paula Murray
A set of triterpenoids with different grades of oxidation in the lupane skeleton were prepared and evaluated as cholinesterase inhibitors. Allylic oxidation with selenium oxide and Jones's oxidation were employed to obtain mono-, di- and tri-oxolupanes, starting from calenduladiol (1) and lupeol (3). All the derivatives showed a selective inhibition of butyrylcholinesterase over acetylcholinesterase (BChE vs. AChE). A kinetic study proved that compounds 2 and 9, the more potent inhibitors of the series, act as competitive inhibitors...
May 17, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29793142/synthesis-of-aryl-pyrazole-via-suzuki-coupling-reaction-in-vitro-mushroom-tyrosinase-enzyme-inhibition-assay-and-in-silico-comparative-molecular-docking-analysis-with-kojic-acid
#4
Pervaiz Ali Channar, Aamer Saeed, Fayaz Ali Larik, Bakhtawar Batool, Saima Kalsoom, M M Hasan, Mauricio F Erben, Hesham R El-Seedi, Musrat Ali, Zaman Ashraf
Aryl pyrazoles are well recognized class of heterocyclic compounds found in several commercially available drugs. Owing to their significance in medicinal chemistry, in this current account we have synthesized a series of suitably substituted aryl pyrazole by employing Suzuki cross-coupling reaction. All compounds were evaluated for inhibition of mushroom tyrosinase enzyme both in vitro and in silico. Compound 3f (IC50  = 1.568 ± 0.01 µM) showed relatively better potential compared to reference kojic acid (IC50  = 16...
April 30, 2018: Bioorganic Chemistry
https://www.readbyqxmd.com/read/29793070/intradialytic-blood-pressure-pattern-recognition-based-on-density-peak-clustering
#5
Feng Wang, Jing-Yi Zhou, Yu Tian, Yu Wang, Ping Zhang, Jiang-Hua Chen, Jing-Song Li
End-stage renal disease (ESRD) is the final stage of chronic kidney disease (CKD) and requires hemodialysis (HD) for survival. Intradialytic blood pressure (IBP) measurements are necessary to ensure patient safety during HD treatments and have critical clinical and prognostic significance. Studies on IBP measurements, especially IBP patterns, are limited. All related studies have been based on a priori knowledge and artificially classified IBP patterns. Therefore, the results were influenced by subjective concepts...
May 21, 2018: Journal of Biomedical Informatics
https://www.readbyqxmd.com/read/29792976/simultaneous-bilateral-ureteral-calculi-a-new-paradigm-for-management
#6
Kymora B Scotland, Scott G Hubosky, Ryuta Tanimoto, Robert Cooper, Kelly A Healy, Demetrius H Bagley
OBJECTIVES: To define the need for emergent intervention between patients with SBUC compared to unilateral ureteral calculi (UUC). Patients with simultaneous bilateral ureteral calculi (SBUC) represent a potential urological emergency due to possible anuria and/or electrolyte imbalance. While conventional practice mandates immediate intervention in these patients, little data exist to define the rate of these events. METHODS: Records of all patients with ureteral stones treated ureteroscopically over an 11-year period were reviewed to identify those with SBUC...
May 21, 2018: Urology
https://www.readbyqxmd.com/read/29792971/impact-of-active-surveillance-and-infection-control-measures-on-carbapenem-resistant-gram-negative-bacterial-colonization-and-infections-in-intensive-care
#7
T Karampatakis, K Tsergouli, E Iosifidis, C Antachopoulos, A Karapanagiotou, A Karyoti, N Gritsi-Gerogianni, A Tsakris, E Roilides
BACKGROUND: Carbapenem-resistant Gram-negative bacteria (CRGNB) infections constitute a global threat for critically ill patients and the outcome of their hospitalization. Early identification of CRGNB through rectal surveillance cultures and routine infection control measures including contact precautions, use of appropriate disinfectants, staff education on cleaning, and hand hygiene may reduce the dissemination of CRGNB. AIM: To assess the impact of enhanced infection control measures on CRGNB infections in a nine-bed polyvalent intensive care unit in a tertiary level hospital in an endemic area...
May 21, 2018: Journal of Hospital Infection
https://www.readbyqxmd.com/read/29792913/comparison-of-cerebral-ventricular-volumes-and-cortical-thicknesses-in-normal-rats-and-genetic-absence-epilepsy-gaers-a-developmental-study
#8
Özlem Kirazlı, Hüsniye Hacıoğlu Bay, Yusuf Özgür Çakmak, Filiz Onat, Safiye Çavdar
Ventricular enlargement and cortical atrophy have been associated with various central nervous system diseases. The aim of the present study was to measure the volumes of the lateral (LV) and third (3V) ventricles and to determine the cortical thickness for the motor (MCx), somatosensory (SSCx), visual (VCx) and auditory (AuCx) cortex and the striatum of Wistar rats, in a developmental series at 10, 20, 30, and 60 days postnatal, and to compare them with similar data from genetic absence epilepsy rats from Strasbourg (GAERS)...
May 21, 2018: International Journal of Developmental Neuroscience
https://www.readbyqxmd.com/read/29792895/pharmacogenomics-of-drug-induced-liver-injury-dili-molecular-biology-to-clinical-applications
#9
REVIEW
Kalaiyarasi Kaliyaperumal, Jane I Grove, Robin M Delahay, William J H Griffiths, Adam Duckworth, Guruprasad P Aithal
A number of drug-specific and host-related factors contribute to the development of drug-induced liver injury (DILI). Investigations focused on genetic susceptibility to DILI have advanced our understanding of the pathogenesis of this rare, yet potentially life-threatening adverse reaction. Candidate gene studies involving well-characterized patients with DILI and drug-exposed controls have identified single nucleotide polymorphisms (SNPs) affecting the metabolism and clearance of specific drugs and hence, influencing individual's susceptibility to DILI...
May 21, 2018: Journal of Hepatology
https://www.readbyqxmd.com/read/29792798/structural-analysis-of-phospholipid-using-hydrogen-abstraction-dissociation-and-oxygen-attachment-dissociation-in-tandem-mass-spectrometry
#10
Hidenori Takahashi, Yuji Shimabukuro, Daiki Asakawa, Shosei Yamauchi, Sadanori Sekiya, Shinichi Iwamoto, Motoi Wada, Koichi Tanaka
Gas-phase hydrogen radicals were introduced into a quadrupole ion trap containing singly charged phospholipids to obtain structural fragmentation patterns in tandem mass spectrometry (MS/MS). Saturated and unsaturated phosphatidylcholines were used as a model phospholipid, whose chain-length ranges between 16 and 24. The MS/MS spectrum yielded a continuous series of fragment ions with a mass differencesdifference of 14 Da, representing the saturated fatty acyl chains. The fragment ions corresponding to the double-bond position within a single fatty acyl chain showed thea characteristic mass difference of 12 Da...
May 24, 2018: Analytical Chemistry
https://www.readbyqxmd.com/read/29792797/determination-of-a-focused-mini-kinase-panel-for-early-identification-of-selective-kinase-inhibitors
#11
Scott D Bembenek, Gavin Hirst, Taraneh Mirzadegan
We analyzed an extensive data set of 3000 Janssen kinase inhibitors (spanning some 40 therapeutic projects) profiled at 414 kinases in the DiscoverX KINOMEscan to better understand the necessity of using such a full kinase panel versus simply profiling one's compound at a much smaller number of kinases, or mini kinase panel (MKP), to assess its selectivity. To this end, we generated a series of MKPs over a range of sizes, and of varying kinase membership using Monte Carlo simulations. By defining the kinase hit index (KHI), we quantified a compound's selectivity based on the number of kinases it hits...
May 24, 2018: Journal of Chemical Information and Modeling
https://www.readbyqxmd.com/read/29792729/90-kvp-low-tube-voltage-ct-pulmonary-angiography-in-combination-with-advanced-modelled-iterative-reconstruction-algorithm-effects-on-radiation-dose-image-quality-and-diagnostic-accuracy-for-the-detection-of-pulmonary-embolism
#12
Doris Leithner, Tatjana Gruber-Rouh, Martin Beeres, Julian L Wichmann, Scherwin Mahmoudi, Simon S Martin, Lukas Lenga, Moritz H Albrecht, Christian Booz, Thomas J Vogl, Jan-Erik Scholtz
OBJECTIVE: To evaluate low-tube-voltage 90-kVp computed tomography pulmonary angiography (CTPA) with advanced modelled iterative reconstruction algorithm (Admire) compared to 120-kVp equivalent dual-energy acquisition with regards to radiation exposure, image quality, and diagnostic accuracy for pulmonary embolism (PE) assessment. METHODS: CTPA studies of 40 patients with suspected PE (56.7 ± 16.3 years) performed on a third-generation 192-slice dual-source CT scanner were retrospectively included...
May 24, 2018: British Journal of Radiology
https://www.readbyqxmd.com/read/29792704/double-hydrogen-atom-exchange-reactions-of-hx-x-f-cl-br-i-with-ho2
#13
Rex T Skodje, Jonathan R Church
A novel double hydrogen atom exchange process, HX+H'O2H'X+HO2 for the halogen series X=F, Cl, Br, and I, is identified using theoretical methods. These concerted reactions are mediated through a stabilized five-member planar ring transition state structure. The transition state barrier for the double exchange process is found to be significantly lower than that for the abstraction reaction of a single hydrogen atom, . Density functional theory employing the M11 exchange functional is used to compute parameters of the potential energy surface and the rate coefficients are obtained using transition state theory with small curvature tunneling...
May 24, 2018: Journal of Physical Chemistry. A
https://www.readbyqxmd.com/read/29792699/water-soluble-ruthenium-ii-carbonyls-with-1-3-5-triaza-7-phosphoadamantane
#14
Federica Battistin, Gabriele Balducci, Barbara Milani, Enzo Alessio
As a continuation of our strategy for preparing new Ru(II) precursors with improved water solubility through the introduction of highly water-soluble 1,3,5-triaza-7-phosphoadamantane (PTA) supporting ligands in the coordination sphere, in this work, we address the largely unexplored preparation of Ru(II)-PTA carbonyls. Two complementary synthetic approaches were used: (1) the treatment of a series of neutral Ru(II)-CO-dmso compounds of general formula RuCl2 (CO) n (dmso)4- n ( n = 1-3, 1-5) with PTA; (2) the reaction of Ru(II)-PTA complexes with CO...
May 24, 2018: Inorganic Chemistry
https://www.readbyqxmd.com/read/29792695/bond-dissociation-energies-of-metallo-supramolecular-building-blocks-insight-from-fragmentation-of-selectively-self-assembled-heterometallic-metallo-supramolecular-aggregates
#15
Yvonne Lorenz, Albert Gutiérrez, Montserrat Ferrer, Marianne Engeser
A series of selectively self-assembled metallo-supramolecular square-like macrocycles with unsymmetric ditopic linkers and two different types of metal corners, i.e., {Pd(η3 -2-Me-C3 H4 )} and {M(dppp)} with dppp = 1,3-bis(diphenylphosphino)propane and M = Pd2+ or Pt2+ , have been studied in the gas phase using collision-induced dissociation. The aggregates show distinct fragmentation patterns determined by ligand length, i.e, aggregate size, and type of metal corner. Information on relative binding strength can be deduced...
May 24, 2018: Inorganic Chemistry
https://www.readbyqxmd.com/read/29792689/selectivity-within-a-family-of-bacterial-phosphothreonine-lyases
#16
Kaitlin A Chambers, Nile S Abularrage, Rebecca A Scheck
Phosphothreonine lyases are bacterial effector proteins secreted into host cells to facilitate the infection process. This enzyme family catalyzes an irreversible elimination reaction that converts phosphothreonine or phosphoserine to dehydrobutyrine or dehydroalanine, respectively. Herein we report a study of substrate selectivity for each of the four known phosphothreonine lyases. This was accomplished using a combination of mass spectrometry and enzyme kinetics assays for a series of phosphorylated peptides derived from the mitogen activated protein kinase (MAPK) activation loop...
May 24, 2018: Biochemistry
https://www.readbyqxmd.com/read/29792640/-serial-cases-of-troubleshooting-of-neuviz-ct
#17
Jiansheng Zhong
The article describes the specifi c examples of fault maintenance of the Neusoft NeuViz series CT, so as toprovide some maintenance references for coleagues.
September 2017: Zhongguo Yi Liao Qi Xie za Zhi, Chinese Journal of Medical Instrumentation
https://www.readbyqxmd.com/read/29792594/an-nmdar-positive-and-negative-allosteric-modulator-series-share-a-binding-site-and-are-interconverted-by-methyl-groups
#18
Riley Perszyk, Brooke M Katzman, Hirofumi Kusumoto, Steven A Kell, Matthew P Epplin, Yesim A Tahirovic, Rhonda L Moore, David Menaldino, Pieter Burger, Dennis C Liotta, Stephen F Traynelis
N-methyl-d-aspartate receptors (NMDARs) are an important receptor in the brain and have been implicated in multiple neurological disorders. Many non-selective NMDAR-targeting drugs are poorly tolerated, leading to efforts to target NMDAR subtypes to improve the therapeutic index. We describe here a series of negative allosteric NMDAR modulators with submaximal inhibition at saturating concentrations. Modest changes to the chemical structure interconvert negative and positive modulation. All modulators share the ability to enhance agonist potency and are use-dependent, requiring the binding of both agonists before modulators act with high potency...
May 24, 2018: ELife
https://www.readbyqxmd.com/read/29792569/the-relationship-between-suicidal-responses-and-traumatic-brain-injury-and-severe-insomnia-in-active-duty-veteran-and-civilian-populations
#19
Kelly A Soberay, Jetta E Hanson, Megan Dwyer, E Ashby Plant, Peter M Gutierrez
OBJECTIVE: This study examined how a positive traumatic brain injury (TBI) screening and insomnia severity relates to suicidal outcomes across active duty, veteran, and civilian samples. METHODS: Data were used from 3,993 participants from 19 studies. We conducted a series of analyses by group to identify which significantly differed on the variables of interest. RESULTS: TBI and insomnia each had independent relationships with outcomes over and above the impact of the other factor...
May 24, 2018: Archives of Suicide Research: Official Journal of the International Academy for Suicide Research
https://www.readbyqxmd.com/read/29792561/testimonial-psychotherapy-in-immigrant-survivors-of-intimate-partner-violence-a-case-series
#20
Pooja Lakshmin, Veronica Slootsky, Peter B Polatin, James L Griffith
Testimonial psychotherapy is a therapeutic ritual for facilitating the recovery of survivors of human rights violations that focuses on sharing the trauma narrative. Originally developed in Chile as a method for collecting evidence during legal proceedings, testimonial therapy has been widely applied transculturally as a unique treatment modality for populations that are not amenable to traditional Western psychotherapy. In this case report, we first review the literature on testimonial therapy to this date...
January 1, 2018: Transcultural Psychiatry
keyword
keyword
51405
1
2
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"