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https://www.readbyqxmd.com/read/28222571/the-edurep-approach-plus-manual-therapy-for-the-management-of-insertional-achilles-tendinopathy-a-case-report
#1
Francesco Sartorio, Anna Zanetta, Giorgio Ferriero, Elisabetta Bravini, Stefano Vercelli
BACKGROUND: Insertional Achilles tendinopathy (IAT) is a challenging overuse disorder. The aim of this case report was to study the feasibility of a comprehensive rehabilitative approach according to the Education, Unloading, Reloading, and Prevention (EdUReP) framework combined with Instrument-Augmented Soft Tissue Mobilization (I-ASTM). METHODS: An active 51-year-old man patient with chronic IAT was studied. Clinical assessment battery was composed by visual analogue scale for pain during the Achilles tendon palpation test, passive straight leg raise test, single leg hop test, Patient-Specific Functional Scale, and Foot and Ankle Ability Measure...
February 21, 2017: Journal of Sports Medicine and Physical Fitness
https://www.readbyqxmd.com/read/28222397/a-novel-approach-towards-design-synthesis-and-evaluation-of-some-schiff-base-analogues-of-2-aminopyridine-and-2-aminobezothiazole-against-hepatocellular-carcinoma
#2
Shinu Chacko, Subir Samanta
Hepatocellular carcinoma is the most common primary malignancy of the liver with poor prognosis. In this study novel, Schiff's bases of 2-aminopyridine (SSSC-26 to 31) and 2-aminobenzothiazole (SSSC-32 to 37) were designed, synthesised and evaluated for antioxidant potential using DPPH method, and anti-hepatocellular carcinoma property using diethylnitrosamine (DEN) induced hepatocellular carcinoma rat model. The in-silico pharmacokinetic, rule of five and toxicity studies reveals that all the leads have an excellent intrinsic quality and sufficient structural features necessary for an oral activity...
February 18, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28222318/design-synthesis-biological-evaluation-and-molecular-modeling-study-of-novel-macrocyclic-bisbibenzyl-analogues-as-antitubulin-agents
#3
Bin Sun, Lin Li, Qing-Wen Hu, Hong-Bo Zheng, Hui Tang, Huan-Min Niu, Hui-Qing Yuan, Hong-Xiang Lou
A series of macrocyclic bisbibenzyls with novel skeletons was designed, synthesized, and evaluated for antiproliferative activity against five anthropic cancer cell lines. Among these novel molecules, compound 47 displayed excellent anticancer activity against HeLa, k562, HCC1428, HT29 and PC-3/Doc cell lines, with IC50 values ranging from of 1.51 μM-5.51 μM, which were more potent than the parent compound, marchantin C. Compounds 44 and 55 with novel bisbibenzyl skeletons also exhibited significantly improved antiproliferative potency...
February 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28222315/allylic-isothiouronium-salts-the-discovery-of-a-novel-class-of-thiourea-analogues-with-antitumor-activity
#4
Misael Ferreira, Laura Sartori Assunção, Adny Henrique Silva, Fabíola Branco Filippin-Monteiro, Tânia Beatriz Creczynski-Pasa, Marcus Mandolesi Sá
A series of 28 aryl- and alkyl-substituted isothiouronium salts were readily synthesized in high yields through the reaction of allylic bromides with thiourea, N-monosubstituted thioureas or thiosemicarbazide. The S-allylic isothiouronium salts substituted with aliphatic groups were found to be the most effective against leukemia cells. These compounds combine high antitumor activity and low toxicity toward non-tumoral cells, with selectivity index higher than 20 in some cases. Furthermore, the selected isothiouronium salts induced G2/M cell cycle arrest and cell death, possibly by apoptosis...
February 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28222044/endocrine-system-on-chip-for-a-diabetes-treatment-model
#5
Dao Thi Thuy Nguyen, Danny van Noort, In-Kyung Jeong, Sungsu Park
The endocrine system is a collection of glands producing hormones which, among others, regulates metabolism, growth and development. One important group of endocrine diseases is diabetes, which is caused by a deficiency or diminished effectiveness of endogenous insulin. By using a microfluidic perfused 3D cell-culture chip, we developed an 'endocrine system on chip' to potentially be able to screen drugs for the treatment of diabetes by measuring insulin release over time. Insulin-secreting β-cells are located in the pancreas, while L-cells, located in the small intestines, stimulate insulin secretion...
February 21, 2017: Biofabrication
https://www.readbyqxmd.com/read/28221724/novel-pieces-for-the-emerging-picture-of-sulfoximines-in-drug-discovery-synthesis-and-evaluation-of-sulfoximine-analogues-of-marketed-drugs-and-advanced-clinical-candidates
#6
Ulrich Lücking, Juan Alberto Sirvent
Sulfoximines have gained considerable recognition as an important structural motif in drug discovery of late. In particular, the clinical kinase inhibitors for the treatment of cancer, roniciclib (pan-CDK inhibitor), BAY 1143572 (PTEFb inhibitor), and AZD 6738 (ATR inhibitor), have recently drawn considerable attention. Whilst the interest in this underrepresented functional group in drug discovery is clearly on the rise, there remains an incomplete understanding of the medicinal chemistry relevant properties of sulfoximines...
February 21, 2017: ChemMedChem
https://www.readbyqxmd.com/read/28221697/solution-processable-hyperbranched-conjugated-polymer-nanoparticles-based-on-c3h-symmetric-benzotrithiophene-for-polymer-solar-cells
#7
Xiaofu Wu, Zijian Zhang, Hao Hang, Yonghong Chen, Yuxiang Xu, Hui Tong, Lixiang Wang
The development of photovoltaic polymers based on C3h -symmetric benzotrithiophene (C3h -BTT), an analogue of the well-known benzodithiophene (BDT) donor unit, has been severely limited due to difficult processability. Here the authors report the preparation of solution-processable C3h -BTT-based hyperbranched conjugated polymer nanoparticles (BTT-HCPNs) with tunable particle sizes via Stille miniemulsion polymerization. Compared with the corresponding star-shaped small molecule (C3h -BTT core with three diketopyrrolopyrrole arms, BTT-3DPP) with a wide bandgap (1...
February 21, 2017: Macromolecular Rapid Communications
https://www.readbyqxmd.com/read/28221388/synthesis-of-c6-modified-%C3%AE-c-galcer-analogues-as-mouse-and-human-inkt-cell-agonists
#8
Joren Guillaume, Toshiyuki Seki, Tine Decruy, Koen Venken, Dirk Elewaut, Moriya Tsuji, Serge Van Calenbergh
α-GalCer analogues that combine known Th1 polarizing C6''-modifications with a C-glycosidic linkage were synthesized. We employed a protecting group strategy that allowed the preparation of both saturated and unsaturated derivatives with variable C6''-substituents. Selected analogues demonstrate promising activity in mice. Interestingly, the introduction of a 6''-O-pyridinylcarbamoyl substituent to α-C-GalCer restores its antigenicity in human iNKT cells.
February 21, 2017: Organic & Biomolecular Chemistry
https://www.readbyqxmd.com/read/28221351/imaging-quantum-stereodynamics-through-fraunhofer-scattering-of-no-radicals-with-rare-gas-atoms
#9
Jolijn Onvlee, Sean D S Gordon, Sjoerd N Vogels, Thomas Auth, Tijs Karman, Bethan Nichols, Ad van der Avoird, Gerrit C Groenenboom, Mark Brouard, Sebastiaan Y T van de Meerakker
Stereodynamics describes how the vector properties of molecules, such as the directions in which they move and the axes about which they rotate, affect the probabilities (or cross-sections) of specific processes or transitions that occur on collision. The main aspects of stereodynamics in inelastic atom-molecule collisions can often be understood from classical considerations, in which the particles are represented by billiard-ball-like hard objects. In a quantum picture, however, the collision is described in terms of matter waves, which can also scatter into the region of the geometrical shadow of the object and reveal detailed information on the pure quantum-mechanical contribution to the stereodynamics...
March 2017: Nature Chemistry
https://www.readbyqxmd.com/read/28221207/aprotinin-vs-tranexamic-acid-in-isolated-coronary-artery-bypass-surgery-a-large-multicentre-observational-study
#10
Elsa Deloge, Julien Amour, Sophie Provenchère, Bertrand Rozec, Bruno Scherrer, Alexandre Ouattara
BACKGROUND: Aprotinin appears to be more efficacious than lysine analogues to reduce bleeding and transfusion of blood products in high-transfusion-risk cardiac surgical patients. However, in isolated coronary artery bypass graft (CABG) surgery, the results from head-to-head trials remain less conclusive. OBJECTIVE: Our objective was to compare the efficacies and safety of aprotinin and tranexamic acid (TXA) in patients undergoing isolated on-pump CABG. DESIGN: A large multicentre before-and-after study pooling individual data from published trials and unpublished data from three other databases...
February 17, 2017: European Journal of Anaesthesiology
https://www.readbyqxmd.com/read/28221031/%C3%AF-conjugated-discrete-oligomers-containing-planar-and-nonplanar-aromatic-motifs
#11
Ji Li, Anamaria Terec, Yue Wang, Hrishikesh Joshi, Yunpeng Lu, Handong Sun, Mihaiela C Stuparu
A new family of π-conjugated oligomers featuring a nonplanar polycyclic aromatic hydrocarbon, corannulene, and a planar aromatic unit, thiophene, is synthesized through an iterative metal-catalyzed coupling protocol. The two structural motifs are connected through an acetylene linkage. In the shorter oligomers, a thiophene unit is attached to one or two corannulenes. In the higher analogues, two, three, and four thiophene units are placed in an alternating fashion with three, four, and five corannulene units, respectively...
February 21, 2017: Journal of the American Chemical Society
https://www.readbyqxmd.com/read/28220975/thermodynamic-stability-of-heterodimetallic-lnln-complexes-synthesis-and-dft-studies
#12
Guillem Aromi, Joan González-Fabra, Nuno A G Bandeira, Veronica Velasco, Leoní A Barrios, David Aguilà, Simon J Teat, Olivier Roubeau, Carles Bo
The solid state and solution configuration of the heterodimetallic complexes, (Hpy)[CeEr(HL)3(NO3)(py)(H2O)] (1), (Hpy)[PrSm(HL)3(NO3)(py)(H2O)] (2) and (Hpy)2[LaYb(HL)3(NO3)(H2O)](NO3) (3), where H3L is 6-(3-oxo-3-(2-hydroxyphenyl)propionyl)pyridine-2-carboxylic acid, are analysed experimentally and through DFT calculations. Complexes 2 and 3 are described here for the first time, by means of single crystal X-ray diffraction and mass spectrometry. The theoretical study is also extended to the [LaCe], [LaLu] and [CeGd] analogues...
February 21, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28220966/nhc-based-tri-organyl-zn-alkyl-cations-synthesis-structure-isomerization-for-improved-stability-and-use-in-co2-functionalization
#13
Samuel Dagorne
Tri-organyl and tri-coordinate N-heterocyclic carbene Zn-NHC alkyl cations (nNHC)2Zn-Me+ (nNHC = C2-bonded-IMes/-IDipp; 3+ and 4+) were first synthesized and structurally characterized via ionization of the corresponding neutral precursors (NHC)ZnMe2 with [Ph3C][B(C6F5)4] in the presence of 1 equiv. of free NHC. Cations 3+-5+ are the first Zn cations of the type Zn(C)(C')(C'')+ (C, C', C'' = σ-donor carbyl ligand). While cation (nIMes)2Zn-Me+ (3+) is stable, its sterically congested analogue (nIDipp)2Zn-Me+ (4+) readily undergoes a nNHC-to-aNHC isomerization in the presence of THF or IDipp to afford the more thermodynamically stable (aDipp)(nIDipp)Zn-Me+ (aIDipp = C5-bonded IDipp, 5+), reflecting the adaptable-to-sterics coordination chemistry of these cations for improved stability...
February 21, 2017: Chemistry: a European Journal
https://www.readbyqxmd.com/read/28220920/tetradecanuclearity-in-3d-4f-chemistry-relaxation-and-magnetocaloric-effects-in-niln-species
#14
Angelos B Canaj, Dimitris A Kalofolias, Milosz Siczek, Tadeusz Lis, Robbie McNab, Giulia Lorusso, Ross Inglis, Marco Evangelisti, Constantinos J Milios
The employment of 2-amino-isobutyric acid, Haib, and 2-hydroxy-1-naphthaldehyde, Hnaphth, in Ni(II)/Ln(III) chemistry has led to the isolation and characterization of two new isostructural 3d-4f tetradecanuclear [NiLn] clusters (Ln = Gd(III), Dy(III)), with the Dy analogue displaying temperature and frequency dependent out-of-phase signals, and the Gd analogue showing interesting magnetocaloric properties.
February 21, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28220918/cadmium-complexes-bearing-me2-n-e-o-e-s-se-organochalcogenoalkoxides-and-their-zinc-and-mercury-analogues
#15
Alexandra Pop, Clément Bellini, Răzvan Şuteu, Vincent Dorcet, Thierry Roisnel, Jean-François Carpentier, Anca Silvestru, Yann Sarazin
Heteroleptic zinc and cadmium complexes of the type [{(Me2)N^E^O(R2)}M-Nu]n (M = Zn, Cd; E = S, Se; R = CH3, CF3; Nu = N(SiMe3)2, I, Cl; n = 1-2) were prepared by reacting the alcohol proteo-ligands {(Me2)N^E^O(R2)}H with [M(N(SiMe3)2)2] (M = Zn, Cd) or [XMN(SiMe3)2] (M = Zn, X = Cl; M = Cd, X = I) in an equimolar ratio. These group 12 metal complexes were characterised in solution by multinuclear NMR spectroscopy and their solid-state structures were determined by X-ray diffractometry. The ligands {(Me2)N^E^O((CH3)2)}(-) bearing CH3 groups in α position to the alkoxide behave as κ(2)-O,E-bidentate moieties (E = S, Se) and form centro-symmetric dinuclear O-bridged heteroleptic alkoxo-amido complexes both with zinc and cadmium, with four-coordinate metal centres resting in tetrahedral environments...
February 21, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28220917/ditopic-receptors-containing-urea-groups-for-solvent-extraction-of-cu-ii-salts
#16
Israel Carreira-Barral, Marta Mato-Iglesias, Andrés de Blas, Carlos Platas-Iglesias, Peter A Tasker, David Esteban-Gómez
The ditopic receptor L3 [1-(2-((7-(4-(tert-butyl)benzyl)-1,4,7,10-tetraazacyclododecan-1-yl)methyl)phenyl)-3-(3-nitrophenyl)urea] containing a macrocyclic cyclen unit for Cu(ii)-coordination and a urea moiety for anion binding was designed for recognition of metal salts. The X-ray structure of [CuL3(SO4)] shows that the sulfate anion is involved in cooperative binding via coordination to the metal ion and hydrogen-bonding to the urea unit. This behaviour is similar to that observed for the related receptor L1 [1-(2-((bis(pyridin-2-ylmethyl)amino)methyl)phenyl)-3-(3-nitrophenyl)urea], which forms a dimeric [CuL1(μ-SO4)]2 structure in the solid state...
February 21, 2017: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/28220857/samhd1-enhances-nucleoside-analogue-efficacy-against-hiv-1-in-myeloid-cells
#17
Paula Ordonez, Simone Kunzelmann, Harriet C T Groom, Melvyn W Yap, Simon Weising, Chris Meier, Kate N Bishop, Ian A Taylor, Jonathan P Stoye
SAMHD1 is an intracellular enzyme that specifically degrades deoxynucleoside triphosphates into component nucleoside and inorganic triphosphate. In myeloid-derived dendritic cells and macrophages as well as resting T-cells, SAMHD1 blocks HIV-1 infection through this dNTP triphosphohydrolase activity by reducing the cellular dNTP pool to a level that cannot support productive reverse transcription. We now show that, in addition to this direct effect on virus replication, manipulating cellular SAMHD1 activity can significantly enhance or decrease the anti-HIV-1 efficacy of nucleotide analogue reverse transcription inhibitors presumably as a result of modulating dNTP pools that compete for recruitment by viral polymerases...
February 21, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28220597/a-new-option-for-definitive-burn-wound-closure%C3%A2-%C3%A2-pair-matching-type-of-retrospective-case-control-study-of-hand-burns-in-the-hospitalised-patients-group-in-the-dr-stanislaw-sakiel-centre-for-burn-treatment-between-2009-and-2015
#18
Justyna Glik, Marek Kawecki, Diana Kitala, Agnieszka Klama-Baryła, Wojciech Łabuś, Marek Grabowski, Agata Durdzińska, Mariusz Nowak, Marcelina Misiuga, Aleksandra Kasperczyk
Nearly 80% of all burns include the hands of affected individuals. Skin grafting is the gold standard in burns treatment, but in the case of the burn wound bed, it may require the necessity of utilising skin substitutes to facilitate closure. The aim of this study is to assess the impact of a porcine-derived wound dressing (Oasis™) for application to hand burns compared to a synthetic dressing (Suprathel™). Comparative assessments were made, including the time to heal, quality of healing and pain intensity...
February 21, 2017: International Wound Journal
https://www.readbyqxmd.com/read/28220592/turkish-validation-of-the-urethral-stricture-surgery-specific-patient-reported-outcome-measure-uss-prom-with-supplemental-assessment-of-erectile-function-and-morbidity-due-to-oral-graft-harvesting
#19
Fikret Fatih Önol, Ahmet Bindayi, Ahmet Tahra, Ismail Basibuyuk, Sinasi Yavuz Onol
AIMS: We validated a Turkish language version of the urethral stricture surgery specific patient-reported outcome measure (USS-PROM) in men undergoing anterior urethroplasty. We also investigated changes in erectile function (EF) and quality of life (QoL) due to oral mucosa graft (OMG) harvesting. METHODS: The USS-PROM captures lower urinary tract symptoms (LUTS), health related QoL (HRQoL) with EQ-5D visual analogue scale (EQ-VAS). To evaluate EF and OMG morbidity, we used International Index of Erectile Function (IIEF-5) and a self-completed questionnaire, respectively...
February 21, 2017: Neurourology and Urodynamics
https://www.readbyqxmd.com/read/28220557/aza-amino-acid-scanning-of-chromobox-homolog-7-cbx7-ligands
#20
Mariam Traoré, Michael Gignac, Ngoc-Duc Doan, Fraser Hof, William D Lubell
An aza-amino acid scan of peptide inhibitors of the chromobox homolog 7 (CBX7) was performed to study the conformational requirements for affinity to the methyllysine reader protein. Twelve azapeptide analogues were prepared using three different approaches employing respectively N-(Fmoc)aza-amino acid chlorides and submonomer azapeptide synthesis to install systematically aza-residues at the first four residues of the peptide, as well as to provide aza-lysine residues possessing saturated and unsaturated side chains...
February 21, 2017: Journal of Peptide Science: An Official Publication of the European Peptide Society
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