High DR Research Articles

Chiral N,N'-dioxide-Sc(NTf2)3 complex-catalyzed asymmetric bromoamination of chalones with N-bromosuccinimide as both bromine and amide source.

The catalytic asymmetric bromoamination of chalcones with N-bromosuccinimide as both bromine and amide source was realized by using a chiral N,N'-dioxide-Sc(NTf2)3 complex as an efficient catalyst. The corresponding chiral bromoamination products were obtained in high yields with high dr and good ee values (up to 92% yield, 93 : 7 dr and 97% ee) under mild reaction conditions.

TB management by private practitioners – Is it bad everywhere?

IntroductionPoor prescribing practice is alleged to be one of the major factors fuelling the drug-resistant tuberculosis (DR TB) emergence. A study in Mumbai revealed the extent of inappropriate tuberculosis (TB) management practices of private practitioners and discussed that with the context of high DR TB. Kerala is rated among the well performing States in India as far as TB control is concerned with evidences for a lower level of TB transmission and DR TB. The current study was done in Kerala State to assess the prescribing practices of private sector doctors in the treatment of TB. MethodsSurvey questionnaire to write a standard prescription for treating TB was administered to private practitioners dealing with TB, who attended continuing medical education programme on TB at two major cities in Kerala. ResultsResponses from a total of 124 questionnaires were studied. None of them prescribed anti-TB regimen for less than 6 months. Only 7 (5.6%) prescribed a regimen without complete four drugs (H, R, Z, E) in the intensive phase. Out of the 81 doctors who prescribed private anti-TB regimen, 67 (82.7%) had of the opinion that not less than 80% of their patients complete the treatment for the prescribed duration. ConclusionThe current study reports a reasonable TB management practice among the private sector doctors from a State with a low prevalence of DR TB and compliments the argument that effective treatment of TB following the principles of standards for TB care can prevent the emergence of DR TB.

Evidence of Brain Inflammation in Patients with Human T-Lymphotropic Virus Type 1-Associated Myelopathy (HAM): A Pilot, Multimodal Imaging Study Using 11C-PBR28 PET, MR T1-Weighted, and Diffusion-Weighted Imaging.

Five subjects with HAM and 2 HTLV-1 asymptomatic carriers were studied. All underwent clinical neurologic assessment including cognitive function and objective measures of gait, quantification of HTLV-1 proviral load in peripheral blood mononuclear cells, and human leukocyte antigen-antigen D related expression on circulating CD8+ lymphocytes. 11C-PBR28 PET and MRI were performed on the same day. 11C-PBR28 PET total volume of distribution and distribution volume ratio (DVR) were estimated using 2-tissue-compartment modeling. MRI data were processed using tools from the FMRIB Software Library to estimate mean diffusivity (MD) and gray matter (GM) fraction changes. The results were compared with data from age-matched healthy volunteers. Across the whole brain, the total volume of distribution for the subjects with HAM (5.44 ± 0.84) was significantly greater than that of asymptomatic carriers (3.44 ± 0.80). The DVR of the thalamus in patients with severe and moderate HAM was higher than that in the healthy volunteers, suggesting increased translocator protein binding (z > 4.72). Subjects with more severe myelopathy and with high DR expression on CD8+ lymphocytes had increased DVR and MD (near-significant correlation found for the right thalamus MD: P = 0.06). On the T1-weighted MRI scans, the GM fraction of the brain stem was reduced in all HTLV-1-infected patients compared with controls (P < 0.001), whereas the thalamus GM fraction was decreased in patients with HAM and correlated with the disease severity. There was no correlation between neurocognitive function and these markers of central nervous system inflammation. This pilot study suggests that some patients with HAM have asymptomatic inflammation in the brain, which can be detected and monitored by 11C-PBR28 PET together with structural and diffusion-weighted MRI.

PC200. Drain Placement Confers No Benefit Following Carotid Endarterectomy in the Vascular Quality Initiative

While bleeding complications requiring a return to the operating room (OR) after carotid endarterectomy (CEA) are infrequent (1%), they are associated with an increased 30-day combined postoperative stroke or death rate. Drain placement (DR) after CEA varies among vascular surgeons, and there are limited data to support the practice. The goal of this study is to evaluate factors leading to DR and the effect of DR on postoperative outcomes, including return to OR for bleeding, stroke, and death. We identified 47,752 patients undergoing CEA using the VQI registry from 2011 to 2015. Demographic, preoperative and intraoperative factors between patients who underwent CEA with DR (n = 19,425) and without DR (n = 28,327) were compared. End points included return to the OR for bleeding, stroke, death, postoperative wound infection, and hospital length of stay. We then compared postoperative outcomes between groups using mixed-effect logistic regression models to control for correlation within center. Similar methods were used to show relationship between return to OR for bleeding and other variables. Subgroup analysis of patients with DR was compared among centers with high DR (>66.7% of cases), medium DR (33.3-66.7%), and low DR (<33.3%). Patients with DR were more likely to be on a preoperative P2Y12 antagonist (P2A; P < .001), have prior CEA/CAS (P < .001), use dextran (P < .001), have a concomitant procedure/CABG (P < .001), and less likely to use protamine (P < .001) compared to those without DR. DR did not prevent return to the OR for bleeding (P < .22). Re-exploration of the carotid artery after closure in the OR (P < .001), preoperative P2A (P < .001) and no protamine use (P < .001) were predictors for return to the OR for bleeding among those with DR. Of patients requiring return to the OR for bleeding, DR did not influence 30-day stroke (P = .82), 30-day mortality (P = .43), or 30-day combined stroke/mortality (P = .42) compared to those without DR. DR did not influence postoperative wound infection (P < .3). Hospital length of stay was increased in patients with DR (P < .001). Return to OR for bleeding (P = .24), wound infection (P = .16), and length of stay (P = .94) did not differ among the high, medium and low DR groups. DR after CEA does not reduce return to the OR for bleeding nor does it reduce perioperative stroke or death. Drain placement is associated with increased length of stay.

Ion-Tagged Prolinamide Organocatalysts for the Direct Aldol Reaction On-Water

A concise synthesis of two imidazolium ion-tagged prolinamide organocatalysts 3 and 4, varying in anionic component (CF3COO− and PF6 −, respectively) is presented. The latter could be classified as an ionic liquid with a melting point of 66.3 °C, and glass transition temperature of 14.5 °C. The efficiency of each catalyst was compared via a direct aldol reaction revealing a large contrast in catalytic performance, with the catalyst bearing the PF6 − anion being superior. The optimal conditions were determined to be an on-water reaction system, and substrate scoping gave a range of desired aldol products in high conversion (up to >99 %), dr (up to 98:2), and er (up to 96:4). The application of these catalysts to beta-nitrostyrene conjugate addition is also presented.

ENGARUH RANGE OF MOTION (ROM) PASIF TERHADAP KEKUATAN OTOT PADA PASIEN STROKE DENGAN PENURUNAN KESADARAN DI RUANG HCU IGD RSUD Dr. MOEWARDI DI SURAKARTA TAHUN 2012

AbstractIntroduction: Each year, approximately 15 million people worldwide have a stroke. In Indonesia based on the census of population and demography Indonesia (SKDI) in 2010 as many as 3.6 million per year with a prevalence of 8.3 per 1,000 population. Stroke is a neurological disease that appeared suddenly in a short time. One of the clinical manifestations of the most common is hemiparese. Complications hemiparese in muscles and joints is muscle atrophy and joint contractures. One treatment technique to prevent these complications is the Range Of Motion (ROM) passive exercise.Objective: (1) Identify the characteristics of stroke patients with loss of consciousness (2) Identify the muscle power stroke patients with loss of consciousness (3) to analyze the influence Range Of Motion (ROM) of the passive muscle strength in stroke patients with loss of consciousness. Method: This research is quasy experiment with design one-group pretestposttest design. The population in this study were 13 stroke patients with critical conditions in Space High Care Unit Hospital Dr Moewardi in Surakarta. Samples were taken by sampling saturated. Data were analyzed with the Wilcoxon or Z test using SPSS for windows 16 series.Result: (1) The muscle strength before passive ROM was 11 people (68.8%) is trace, 5 people (31.2%) is poor, and of zero muscle strength, fair, good, and normally does not exist. (2) Muscle strength stroke after passive ROM is 7 (43.8%) of respondents with poor muscle strength scale, 9 people (56.2%) fair, and scale of zero muscle strength, trace, good, and normally there is not exist(0%). (3) The results of the statistical Wilcoxon or Z test significance value (p) of 0000 which means that there are differences in muscle strength scale before and after passive Range Of Motion. (ROM) patients with loss of consciousness. Conclusion: Range Of Motion (ROM) is effective for improving muscle strength for stroke patients with loss of consciousness in H ospital Dr Moewardi Surakarta Keywords: Stroke, Hemiparese, Range Of Motion

Effects of exchangeable Ca:Mg ratio on the dispersion of soils some southern Nigeria soils.

Soil surface sealing and erosion which are the result of soil dispersion can be harmful or detrimental to soil, soil resources and also agricultural production thereby leading to great economic loss. Soil samples were collected at 0-30cm depth in eight locations in southern Nigeria. Dispersion behaviours of soil contents were studied at different Ca: Mg ratios. The range of values of properties determined are as follows; clay 10-22%, silt 1-18%, sand 64-89%, WDC 6-14%, WDS 1-16%, CDR 0.44-0.86%, DR 0.41-0.84%, ASC 2-18%, CEC 4-15.6cmolkg -1 , percentage base saturation 18-66%, available phosphorus 1.87-34.57mg/kg. The soils studied were acidic, low in nutrient level, showed high dispersion rate, high water- dispersible clay content and the textural class were loamy sand and sandy loam. The exchangeable Ca 2+ and Mg 2+ contents of the soils dominated the exchange complex. The cation exchange capacity (CEC) ranges between 4 and 15.6 cmol kg -1 . Values of percentage base saturation are between 18 and 66%. The available phosphorous ranges between 1.87-34.57 mg/kg. The distribution of Ca and Mg varied with the quantity of ratio of CaSO 4 and MgSO 4 added. The higher the proportion of Mg the higher the clay content while a lower Mg proportion had a lower clay content. Secondly, a higher Ca 2+ proportion resulted to smaller clay content while a lower Ca 2+ proportion led to a high clay content. From this study it was discovered that high Mg, silt and clay cause soil dispersion which will be detrimental to the soil. Also high CDR and DR are indicators of high soil dispersity. Therefore, monitoring dispersion in soil is important to avoid its negative impact on the soil. Management practices should be applied in the form of application of fertilizer and liming materials to the soil as higher concentration (Ca 2+ and Mg 2+ ) will be introduced to the soil which will bring about dispersion in the soil. Keywords : Dispersion, Ca: Mg ratio, dispersion ratio, clay dispersible ratio, dispersible silt.

Efficient Diastereo‐ and Enantioselective Synthesis of exo‐Nitroprolinates by 1,3‐Dipolar Cycloadditions Catalyzed by Chiral Phosphoramidite⋅Silver(I) Complexes

AbstractChiral complexes formed by privileged phosphoramidites and silver triflate or silver benzoate are excellent catalysts for the general 1,3‐dipolar cycloaddition between azomethine ylides generated from α‐amino acid‐derived imino esters and nitroalkenes affording with high dr the exo‐cycloadducts 4,5‐trans‐2,5‐cis‐4‐nitroprolinates in high ee at room temperature. In general, better results are obtained using silver rather than copper(II) complexes. In many cases the exo‐cycloadducts can be obtained in enantiomerically pure form just after simple recrystallization. The mechanism and the justification of the experimentally observed stereodiscrimination of the process are supported by DFT calculations. These enantiomerically enriched exo‐nitroprolinates can be used as reagents for the synthesis of nitropiperidines, by ester reduction and ring expansion, which are inhibitors of farnesyltransferase.magnified image

ChemInform Abstract: Desymmetrization of Cyclic Olefins via Asymmetric Heck Reaction and Hydroarylation.

An asymmetric Heck reaction allows desymmetrization of substituted cyclic olefins in high dr and ee. A bisphosphine oxide is uniquely stereoselective for this purpose. Desymmetrization of bicyclic olefins via hydroarylation can also be realized in high ee.

Diastereospecific Enolate Addition and Atom-Efficient Benzimidazole Synthesis for the Production of L/T Calcium Channel Blocker ACT-280778

A scalable access to 1 (ACT-280778), a potent L/T calcium channel blocker, has been developed. The synthesis, amenable to kilogram manufacturing, comprises 10 chemical steps from enantiomerically pure 5-phenylbicyclo[2.2.2]oct-5-en-2-one (3) and 1,4-dimethoxybenzene with a longest linear sequence of 7 steps. Key to the success of this fit-for-purpose approach are a robust and atom-efficient access to benzimidazole 4, the substrate-controlled diastereoselective enolate addition toward carboxylic acid 2 that was isolated by simple crystallization with high dr (>99:1), the convenient selective N-deacylation of intermediate 10, and the identification of a suitable solid form of 1 as the bis-maleate salt (1·2 C4H4O4). As an illustration of the robustness of this process, 14 kg of drug substance, suitable for human use, was produced with an overall yield of 38% over the longest linear sequence (7 steps).

N,N′‐Dioxide–Scandium(III)‐Catalyzed Asymmetric Michael Addition of β,γ‐Unsaturated Butenolides to α,β‐Unsaturated γ‐Keto Esters

AbstractA highly efficient N,N′‐dioxide–scandium(III) complex catalytic system has been developed for the asymmetric vinylogous Michael reaction of α‐angelica lactone and its derivatives to α,β‐unsaturated γ‐keto esters, affording the corresponding γ,γ‐disubstituted butenolide products in moderate to good yields (up to 93%) with high dr (up to &gt;19:1) and ee values (up to 97%) under mild reaction conditions.magnified image

DOα−β+ expression in favor of HLA-DR engagement in exosomes

The expression of DOβ and not DOα, in addition to the high intracellular DR, low DM levels and absence of surface DR expression in K562 and HL-60 cells introduce alternative regulatory pathways in DR trafficking and consequently the antigen presentation process. The present study attempted to define the naturally occurring DOα negative state and explain the role of DOβ in the intracellular DR accumulation in K562 and HL-60 cells. Despite the absence of DOα, the DOβ chain was detected in the endosomal compartments. The lack of DOα was found to be partially responsible for the absence of DR from the cell membrane since stable K562-DOα transfectants allowed expression of membrane DR. This expression could be significantly increased upon DM induction by IFN-γ, indicating that DM was another limiting factor for the migration of DR to the cell surface of K562 and HL-60 cells. Furthermore, intracellular DR co-localized with the exosome specific marker CD9, while culture supernatants were shown to contain exosome-engaged and exosome free DR activity as evaluated by SDS-page followed by western blot, ELISA and transmission electron microscopy analysis. These findings indicated that in DOα−β+ cells, DR molecules were programmed to secretion rather than surface expression. The presented results provide novel regulatory processes as to DR trafficking, avoiding expression to the cell surface.

Desymmetrization of cyclic olefins via asymmetric Heck reaction and hydroarylation

An asymmetric Heck reaction allows desymmetrization of substituted cyclic olefins in high dr and ee. A bisphosphine oxide is uniquely stereoselective for this purpose. Desymmetrization of bicyclic olefins via hydroarylation can also be realized in high ee.

Enhancing the performance of SBA-15-supported copper catalysts by chromium addition for the chemoselective hydrogenation of trans-cinnamaldehyde

SBA-15-supported copper–chromium mixed oxide nanoparticles (CuCr/SBA-15) were prepared by incipient wetness impregnation followed by mild drying at 25 °C and calcination. The Cu:Cr weight ratios were 1:1, 5:1, and 10:1, at a constant total loading of 5 wt%. Monocomponent SBA-15-supported Cu–oxide (Cu/SBA-15) and Cr–oxide (Cr/SBA-15) were prepared as reference samples. The materials were systematically characterized by XRD at low and high angles, N2 physisorption, DR UV-vis, FT-IR, and XPS spectroscopies, and TPR. XRD at low angles and N2 physisorption confirmed the preservation of the mesoporous structure of the SBA-15 support after impregnation and calcination. In the case of monocomponent samples, CuO appeared poorly dispersed, while the Cr species (Cr2O3, mono- and polychromates) appeared highly dispersed on the surface of the SBA-15 support. The progressive addition of chromium to copper had positive effects on the average crystallite size of CuO, which decreased from ∼28 nm (Cu/SBA-15) to ∼3 nm (CuCr/SBA-15; Cu:Cr = 1:1), and on reducibility, as well. Metallic active phases were obtained by reducing of the oxide phases under a hydrogen flow at 350 °C. By comparison to the monometallic catalysts, the reduced CuCr/SBA-15 materials were active in the hydrogenation of cinnamaldehyde and chemoselective towards cinnammyl alcohol (>50 mol%). The activity can be correlated with the particle size of copper, whereas the high selectivity to unsaturated alcohol can be associated with the presence of dual Cu0–Crn+ sites.

120-P

Aim To investigate changing protocol for HLA typings on related Bone Marrow (BM) Donors. Current protocol: Recipient typed at low res with ABDRDQ kit. Siblings typed at low res with ABDR kit. Matched Donor at low prompts BM program to select donor for further testing which initially includes high res DR for Recipient & Donor. If matched, low res C & high res A, B & C performed for matching pair. Methods DNA extraction using manual salting-out extraction kit by Qiagen. PCR-SSP using low & high resolution primer kits by One Lambda & Olerup. Results Typing performed on Recip: A ∗ 01,29,B ∗ 57,56,DRB1 ∗ 07,01,B4 ∗ ,DQB1 ∗ 02,05. Typings on 3 sibs all resulted in matches at low res ABDR. Donor selection made by BM program, we proceeded with high DR typing to confirm match. Confirmed DRB1 ∗ 07:01, 01:02, followed by low C typing: results C ∗ 06,16. Performed high res A, B & C for Recipient & Donor. Questioned likelihood of 4 sibs matching at all loci. Unlikely frequency, prompted (outside protocol) high DR on other 2 siblings. Two sibs matched at high DRB1. For education, we confirmed original typings & then low C & DQ to see if all sibs matched. We discovered 1 sib had antigen MM at DQ. Conclusions Overall, we concluded that the ultimate benefit would have been discovering DQ MM initially that would otherwise have been missed. Now, reconsidering approach to related BM Donors.

Phenomics of rice early vigour and drought response: Are sugar related and morphogenetic traits relevant?

BackgroundEarly vigour (biomass accumulation) is a useful but complex trait in rainfed rice (Oryza sativa L). Little is known on trade-offs with drought tolerance. This study explored the relevance of (sugar) metabolic and morphogenetic traits to describe the genetic diversity of rice early vigour and its phenotypic plasticity under drought conditions. A greenhouse experiment was conducted to characterize on a panel of 43 rice genotypes plant morphogenesis and sugar concentration in expanded (source) and expanding (sink) leaves.ResultsAcross genotypes in control treatment, leaf starch concentration was negatively correlated with organogenetic development rate (DR, defined as leaf appearance rate on main stem). Genotypes with small leaves had high DR and tiller number but low leaf starch concentration. Under drought, vigorous genotypes showed stronger growth reduction. Starch concentration decreased in source leaves, by contrast with soluble sugars and with that observed in sink leaves. Accordingly, genotypes were grouped in three clusters differing in constitutive vigour, starch storage and growth maintenance under drought showing a trade off between constitutive vigour and drought tolerance.ConclusionsIt was therefore suggested that non structural carbohydrates, particularly starch, were relevant markers of early vigour. Their relevance as markers of growth maintenance under drought needs to be further explored. Results are discussed regarding novel process based traits to be introduced in the GRiSP (Global Rice Science Partnership) phenotyping network.Electronic supplementary materialThe online version of this article (doi:10.1186/1939-8433-5-22) contains supplementary material, which is available to authorized users.

Developmental Dynamics and Early Growth Vigour in Rice 2. Modelling Genetic Diversity Using Ecomeristem

AbstractEarly vigour is an important objective in rice breeding. A previous study reported strong positive effects of development rate (DR, 1/phyllochron) on early growth vigour in two rice panels. This study provided a model‐based analysis of DR effects on rice early vigour and underlying source–sink processes during exponential growth, using Ecomeristem model. Relevant model parameters were fitted to panel observations, and their effect on early vigour was quantified. A sensitivity analysis was performed to quantify the impact of model parameters on simulation outputs. The simulated behaviour of a population of virtual genotypes defined by the combination of model parameter values was compared with that of diversity panel. Finally, a simulation experiment was conducted to analyse source–sink adjustments constituting early vigour across a range of DR. Parameters governing structural development, particularly DR, had greater impact on vigour than parameters for resource acquisition. High DR was associated with rapid dry weight accumulation and low transitory carbohydrate reserves in both real and virtual populations. Genotypic DR is thus a major driver of early vigour in rice under stress‐free conditions. To evaluate traits contributing to vigour, the capacity of crop models to simulate interactions between structural development and resource acquisition must be improved.

Intramolecular Ester Enolate–Imine Cyclization Reactions for the Asymmetric Synthesis of Polycyclic β-Lactams and Cyclic β-Amino Acid Derivatives

Enolates of chiral N-(α-methyl-p-methoxybenzyl)-ω-imino-esters undergo intramolecular cyclization reactions to afford (syn)-aza-anions of β-amino esters in high dr that cyclize to afford N-(α-methyl-p-methoxybenzyl)-β-lactams that can be readily deprotected to afford their corresponding cyclic NH-β-lactams, β-amino esters, or β-amino acids.

Ratio of size of recipient and donor areas in treatment of vitiligo by autologous cultured melanocyte transplantation

Autologous melanocytes can be expanded in vitro, allowing the treatment of large lesions of vitiligo in one session. Theoretically, this procedure could provide a higher donor/recipient size ratio (DR ratio) compared with that in noncultured cell transplantation (with a DR ratio < 1 : 10). However, the exact DR ratio obtained from this procedure has not been reported. To study whether transplantation of cultured pure melanocytes at a high DR ratio is as efficient as that at a low DR ratio. One hundred and two patients with vitiligo were treated by transplantation of cultured pure melanocytes and were divided into two groups: a low DR ratio group, including patients with DR ratio ≤ 1 : 10 (mean 1 : 8, 35 cases) and a high DR ratio group with DR ratio > 1 : 10 (mean 1 : 27, 67 cases). The extent of repigmentation between these two groups was compared. There was no significant difference in repigmentation between the low DR ratio group (mean ± SD 77·4 ± 22·5%) and the high DR ratio group (77·6 ± 24·8%). Multiple regression analysis showed that even after adjustment for age, sex, type of vitiligo and transplanted cell density, there was no significant correlation between the extent of repigmentation and the DR ratio, indicating that patients treated with high DR ratio obtained a satisfactory result and showed no difference from the low DR ratio group. Various surgical procedures for the treatment of vitiligo which involve melanocyte transplantation or skin grafts have different inherent DR ratios. Transplantation of cultured pure melanocytes is an expensive and complicated procedure; however, it provides the highest DR ratio (> 1 : 10 and up to 1 : 60). Surgeons can select one of these methods for the treatment of vitiligo based on their experience and skill, on the size of lesions, and the availability of laboratory support.

Aneuploidy screening: a position statement from a committee on behalf of the Board of the International Society for Prenatal Diagnosis, January 2011

Aneuploidy screening: a position statement from a committee on behalf of the Board of the International Society for Prenatal Diagnosis, January 2011