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1.
Acta Crystallogr B Struct Sci Cryst Eng Mater ; 79(Pt 6): 462-472, 2023 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-37820013

RESUMEN

The structure of (R)-rasagiline mesylate [(R)-RasH+·Mes-], an active pharmaceutical ingredient used to treat Parkinson's disease, is presented. The structure was determined from laboratory and synchrotron powder diffraction data, refined using the Rietveld method, and validated and optimized using dispersion-corrected DFT calculations. The unit-cell parameters obtained in both experiments are in good agreement and the refinement with both datasets converged to good agreement factors. The final parameters obtained from laboratory data were a = 5.4905 (8), b = 6.536 (2), c = 38.953 (3) Å, V = 1398.0 (4) Å3 and from synchrotron powder data were a = 5.487530 (10) Å, b = 6.528939 (12) Å, c = 38.94313 (9) Å, V = 1395.245 (5) Å3 with Z = 4 and space group P212121. Preferred orientation was properly accounted for using the synchrotron radiation data, leading to a March-Dollase parameter of 1.140 (1) instead of the 0.642 (1) value obtained from laboratory data. In the structure, (R)-RasH+ moieties form layers parallel to the ab plane connected by mesylate ions through N-H...O and C-H...O hydrogen bonds. These layers stack along the c axis and are further connected by C-H...π interactions. Hirshfeld surface analysis and fingerprint plot calculations indicate that the main interactions are: H...H (50.9%), H...C/C...H (27.1%) and H...O/O...H (21.1%).

2.
Sci Total Environ ; 898: 165632, 2023 Nov 10.
Artículo en Inglés | MEDLINE | ID: mdl-37467976

RESUMEN

Anthropogenic and natural sources contribute to chemical mixtures in air, water, and soil, posing potential risks to the environment and human health. To understand the interplay between element profiles in the human body, geographical location, and associated economic activities, we carried out an observational analytic cross-sectional study. The study recruited 199 participants from three municipalities, two of which had gold-mining as their primary economic activity, while the other was dedicated to agricultural and other local activities not related to mining. The concentrations of a total of 30 elements in human hair samples and 21 elements in environmental soil samples were measured using various spectrometry techniques. Unsupervised clustering analysis using Self-Organizing Maps was applied to human hair samples to analyze element concentrations. Distinct clusters of individuals were identified based on their hair element profiles, which were mapped to geographical location and economic activities. While higher levels of heavy metals (Ag, As, Hg, and Pb) were observed in individuals engaged in mining activities in certain clusters, individuals in agricultural areas show higher concentrations of elements found in pesticides (Ba and Sr). However, the elemental composition of hair is influenced not only by the anthropogenic activities but also by the inherent geological context where people live. Our findings highlight the significance of accounting for environmental factors when evaluating human health risks, as the intricate mixture of elements can yield valuable insights for targeted health interventions.

3.
Artículo en Inglés | MEDLINE | ID: mdl-36767692

RESUMEN

The exposure to chemical mixtures is a problem of concern in developing countries and it is well known that the kidney is the major target organ for toxic elements. This cross-sectional study aimed to estimate the individual and composite mixture effect of a large number of chemical elements on kidney function in gold-mining and surrounding non-mining populations in northeast Colombia. We measured concentrations of 36 chemical elements in hair as indicators of chronic exposure from 199 adult participants. We estimated the effect of exposure to mixtures of chemical elements on estimated glomerular filtration rate (eGFR) using weighted quantile sum regression (WQS). The WQS index of the mixture was associated with reduced eGFR (Coefficient -2.42; 95%CI: -4.69, -0.16) being Be, Cd, Pb, As, and Mn, the principal contributors of the toxic mixture. Mining activities and Hg concentration were not associated with decreased kidney function. Our results suggest that complex mixtures of chemical elements, mainly heavy metals, act as nephrotoxic in these populations and therefore the analysis of chemical element mixtures is a better approach to identify environmental and occupational chemical risks for kidney damage.


Asunto(s)
Metales Pesados , Adulto , Humanos , Colombia , Estudios Transversales , Metales Pesados/análisis , Oro , Riñón/química , Monitoreo del Ambiente/métodos
4.
Acta Crystallogr E Crystallogr Commun ; 78(Pt 2): 140-148, 2022 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-35145740

RESUMEN

The structure of racemic (RS)-trichlorme-thia-zide [systematic name: (RS)-6-chloro-3-(di-chloro-meth-yl)-1,1-dioxo-3,4-di-hydro-2H-1λ6,2,4-benzo-thia-di-azine-7-sulfonamide], C8H8Cl3N3O4S2 (RS-TCMZ), a diuretic drug used in the treatment of oedema and hypertension, was determined from laboratory X-ray powder diffraction data using DASH [David et al. (2006 ▸). J. Appl. Cryst. 39, 910-915.], refined by the Rietveld method with TOPAS-Academic [Coelho (2018 ▸). J. Appl. Cryst. 51, 210-218], and optimized using DFT-D calculations. The extended structure consists of head-to-tail dimers connected by π-π inter-actions which, in turn, are connected by C-Cl⋯π inter-actions. They form chains propagating along [101], further connected by N-H⋯O hydrogen bonds to produce layers parallel to the ac plane that stack along the b-axis direction, connected by additional N-H⋯O hydrogen bonds. The Hirshfeld surface analysis indicates a major contribution of H⋯O and H⋯Cl inter-actions (32.2 and 21.7%, respectively). Energy framework calculations confirm the major contribution of electrostatic inter-actions (E elec) to the total energy (E tot). A comparison with the structure of S-TCMZ is also presented.

5.
Acta Crystallogr E Crystallogr Commun ; 77(Pt 3): 226-232, 2021 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-33953941

RESUMEN

The title heterocyclic compound, C20H27N, has been prepared in good yield (72%) via a BiCl3-catalyzed cationic Povarov reaction between N-propargyl-4-methyl-aniline and (±)-citronellal. The X-ray single-crystal study indicates that the structure consists of mol-ecules connected by C-H⋯π contacts to produce chains, which pack in a sandwich-herringbone fashion along the b-axis direction. Hirshfeld surface analysis indicates that H⋯H inter-actions dominate by contributing 79.1% to the total surface. Energy frameworks and DFT calculations indicate a major contribution of dispersive forces to the total inter-action energy.

6.
Mil Med ; 186(Suppl 1): 384-390, 2021 01 25.
Artículo en Inglés | MEDLINE | ID: mdl-33499490

RESUMEN

INTRODUCTION: Prolonged field care for junctional wounds is challenging and involves limb movement to facilitate transport. No studies to date have explored the efficacy of gauze products to limit rebleeding in these scenarios. MATERIALS AND METHODS: We randomly assigned 48 swine to QuikClot Combat Gauze, ChitoGauze, NuStat Tactical, or Kerlix treatment groups (12 each) and then inflicted a severe groin injury by utilizing a modified Kheirabadi model of a 6-mm femoral artery punch followed by unrestricted bleeding for 60 seconds. We reassessed rebleed following limb movement at 30 minutes of stabilization and 4 hours after stabilization. RESULTS: Swine treated with Combat Gauze proved to have the lowest incidence of rebleeding, and conversely, NuStat Tactical had the highest incidence of rebleeding at wounds after limb movement. Importantly, rebleeds occurred at a rate of 25%-58% across all swine treatment groups at 30 minutes postinjury and 0%-42% at 270 minutes postinjury demonstrating that limb movements universally challenge hemostatic junctional wounds. CONCLUSIONS: Our findings highlight the difficulty of controlling hemorrhage from junctional wounds with hemostatic gauze in the context of prolonged field care and casualty transport. Our research can guide selection of hemorrhage control gauze when patients have prolonged field extraction or difficult transport. Our data demonstrates the frequency of junctional wound rebleeding after movement and thus the importance of frequent patient reassessment.


Asunto(s)
Hemostáticos , Animales , Vendajes , Modelos Animales de Enfermedad , Arteria Femoral , Hemorragia/terapia , Técnicas Hemostáticas , Porcinos
7.
Case Rep Infect Dis ; 2020: 7601757, 2020.
Artículo en Inglés | MEDLINE | ID: mdl-32351746

RESUMEN

Cryptococcal meningitis is the most common form of infection caused by Cryptococcus yeast species, followed by pulmonary infection. It is an opportunistic infection seen in patients with impaired cell immunity, most frequently in HIV patients and solid organ transplant recipients; however, it can occur in patients with no apparent immunodeficiency. We describe the case of Cryptococcus neoformans meningitis in an immunocompetent patient with aseptic cerebrospinal fluid analysis which highlights the heterogeneity of this disease.

8.
Cureus ; 11(8): e5368, 2019 Aug 12.
Artículo en Inglés | MEDLINE | ID: mdl-31612096

RESUMEN

Human immunodeficiency virus (HIV) infection presents with a variety of conditions. We describe the case of a 33-year-old Hispanic male with IgA nephropathy and Henoch-Schonlein Purpura in the setting of HIV. The incidence of vasculitis associated with HIV infection is less than 1%. There are few cases reported of IgA nephropathy in the context of HIV. Henoch-Schonlein Purpura usually presents in children. We encountered a patient with rare illnesses while in the setting of immunodeficiency.

9.
Cureus ; 11(6): e4932, 2019 Jun 18.
Artículo en Inglés | MEDLINE | ID: mdl-31431838

RESUMEN

Systemic sclerosis (SS) is a chronic, connective tissue disorder that can affect the skin, subcutaneous tissues, and internal organs. There are two different categories of SS, limited cutaneous systemic sclerosis (LCSS) and diffuse cutaneous systemic sclerosis (DCSS). One of the most fearful situations faced in DCSS is scleroderma renal crisis (SRC). This is a rare but potentially life-threatening complication characterized by an acute, usually symptomatic, increase in blood pressure, rise in serum creatinine levels, oliguria, and thrombotic microangiopathic changes. Pulmonary involvement in the setting of SCR is an even more rare combination and usually can progress into acute hypoxic respiratory failure and lead to worse outcomes. We present herein a case of scleroderma renal crisis complicated with diffuse pulmonary hemorrhage.

10.
Bioorg Chem ; 90: 103034, 2019 09.
Artículo en Inglés | MEDLINE | ID: mdl-31280015

RESUMEN

The chalcone and bis-chalcone derivatives have been synthesized under sonication conditions via Claisen-Schmidt condensation with KOH in ethanol at room temperature (20-89%). The structures were established on the basis of NMR, IR, Single-crystal XRD, and MS. The best compound 3u had inhibitory activity (IC50 = 7.50 µM). The synthesis, the antioxidative properties, chemical reactivity descriptors supported in Density Functional Theory (DFT), acetylcholinesterase (AChE) inhibition and their potential binding modes, and affinity were predicted by molecular docking of a number of morpholine-chalcones and quinoline-chalcone. A series of bis-chalcones are also reported. Molecular docking and an enzyme kinetic study on compound 3u suggested that it simultaneously binds to the catalytic active site (CAS) and peripheral anionic site (PAS) of AChE. Moreover, the pharmacokinetic profile of these compounds was investigated using a computational method.


Asunto(s)
Acetilcolinesterasa/metabolismo , Antioxidantes/química , Chalconas/química , Inhibidores de la Colinesterasa/química , Acetilcolinesterasa/química , Antioxidantes/síntesis química , Antioxidantes/metabolismo , Antioxidantes/farmacocinética , Dominio Catalítico , Chalconas/síntesis química , Chalconas/metabolismo , Chalconas/farmacocinética , Inhibidores de la Colinesterasa/síntesis química , Inhibidores de la Colinesterasa/metabolismo , Inhibidores de la Colinesterasa/farmacocinética , Pruebas de Enzimas , Humanos , Cinética , Simulación del Acoplamiento Molecular , Unión Proteica , Ondas Ultrasónicas
11.
Oxf Med Case Reports ; 2018(10): omy071, 2018 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-30263127

RESUMEN

Blastomycosis is a fungal infection caused by Blastomyces species. This infection is endemic to North America particularly states bordering the Mississippi, Ohio and St Lawrence Rivers, and the Great Lakes but also occurs worldwide. While the most common site of infection is the lung, it can also manifest in the bones, skin and central nervous system. Blastomycosis is a great masquerader and it can present in a manner difficult to distinguish from bacterial pneumonia, tuberculosis (TB), histoplasmosis or carcinoma. Here, we describe a 36-year-old male with disseminated blactomycosis infection who presented with right arm weakness. Initial diagnostic evaluation was cofounded by a previous concern for TB; however, broncho-alveolar lavage confirmed Blastomyces spp. Pulmonary and brain lesions markedly improved after Amphotericin and Itraconazole.

12.
J Environ Manage ; 196: 466-475, 2017 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-28342341

RESUMEN

In this work, NaY zeolite is explored as a possible "template" to obtain porous materials type ZTC from the adsorption of heavy crude oil in a water-oil model system (emulsion). In order to produce the adsorbents, a cationic surfactant is selected to facilitate the adsorption of the crude oil into the pores of the zeolite and to get the composite, which was activated with controlled thermal treatments (T: 700-800 °C and t: 0.5-1 h) in inert conditions (N2 gaseous). The starting materials, composite and porous carbons were characterized using structural/surface analysis techniques (API Gravity, SARA, IR, XRD, XRF, TGA, Langmuir isotherms, BET and SEM). The results showed that four types of mesoporous carbons were produced with specific surface areas between 70 ± 1 m2/g and 220 ± 3 m2/g, average pore volumes between 0.144 cm3/g and 0.40 cm3/g and average pore widths between 4.9 nm and 8.3 nm. The activation conditions of 800 °C and 1 h allowed to make the carbonaceous material with the best surface characteristics (220 ± 3 m2/g, 0.27 cm3/g, and 4.9 nm). Therefore, it is concluded that under assay conditions employed, the heavy crude oil, as a mixed model (water-oil), from an aqueous environment is a starting material suitable for preparation of "mesoporous" carbons.


Asunto(s)
Carbono , Petróleo , Zeolitas , Adsorción , Agua
13.
Acta Crystallogr E Crystallogr Commun ; 71(Pt 11): o882-3, 2015 Nov 01.
Artículo en Inglés | MEDLINE | ID: mdl-26594578

RESUMEN

In the title compound, C10H7FN2OS, the mean plane of the central amide fragment (r.m.s. deviation = 0.048 Å) makes dihedral angles of 35.28 (8) and 10.14 (12)° with those of the fluoro-benzene and thia-zole rings, respectively. The thia-zole S and amide O atoms lie to the same side of the mol-ecule. In the crystal, pairs of N-H⋯N hydrogen bonds connect the mol-ecules into inversion dimers with R 2 (2)(8) motifs, and weak C-H⋯O inter-actions connect the mol-ecules into C(6) [001] chains. Together, the N-H⋯N and C-H⋯O hydrogen bonds generate (100) sheets.

14.
Mil Med ; 180(11): 1189-95, 2015 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-26540712

RESUMEN

OBJECTIVE: Uncontrolled hemorrhage from junctional wounds that cannot be controlled by traditional tourniquets accounts for one in five preventable battlefield exsanguination deaths. Products for treating these wounds are costly and require special training. However, chemically treated gauze products are inexpensive, potentially effective, and require only minimal training. This study was designed to assess the efficacy of three hemostatic gauze products following brief training, using a consensus swine groin injury model. METHODS: After viewing a 15-minute PowerPoint presentation, without demonstration or practice, 24 U.S. Navy Corpsmen, most with little to no live tissue or hemostatic agent experience, applied one of three hemostatic agents: QuikClot Combat Gauze, Celox Trauma Gauze, or Hemcon ChitoGauze. Animals were resuscitated and monitored for 150 minutes to assess initial hemostasis, blood loss, rebleeding, and survival. Participants completed a survey before training and following testing. RESULTS: Products were similar in initial hemostasis, blood loss, and rebleeding. Twenty-three swine survived (96%). Ease of use and perceived efficacy of training ratings were high. Comfort level with application improved following training. CONCLUSIONS: Hemostatic gauze can potentially be effective for treating junctional wounds following minimal training, which has important implications for corpsmen, self-aid/buddy-aid, civilian providers, and Tactical Combat Casualty Care guidelines.


Asunto(s)
Biopolímeros , Consenso , Hemorragia/terapia , Técnicas Hemostáticas/instrumentación , Hemostáticos/uso terapéutico , Personal Militar/educación , Animales , Modelos Animales de Enfermedad , Femenino , Humanos , Masculino , Porcinos
15.
J Emerg Med ; 45(5): 686-94, 2013 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-23921173

RESUMEN

BACKGROUND: Tension pneumothorax accounts for 3%-4% of combat casualties and 10% of civilian chest trauma. Air entering a wound via a communicating pneumothorax rather than by the trachea can result in respiratory arrest and death. In such cases, the Committee on Tactical Combat Casualty Care advocates the use of unvented chest seals to prevent respiratory compromise. OBJECTIVE: A comparison of three commercially available vented chest seals was undertaken to evaluate the efficacy of tension pneumothorax prevention after seal application. METHODS: A surgical thoracostomy was created and sealed by placing a shortened 10-mL syringe barrel (with plunger in place) into the wound. Tension pneumothorax was achieved via air introduction through a Cordis to a maximum volume of 50 mL/kg. A 20% drop in mean arterial pressure or a 20% increase in heart rate confirmed hemodynamic compromise. After evacuation, one of three vented chest seals (HyFin(®), n = 8; Sentinel(®), n = 8, SAM(®), n = 8) was applied. Air was injected to a maximum of 50 mL/kg twice, followed by a 10% autologous blood infusion, and finally, a third 50 mL/kg air bolus. Survivors completed all three interventions, and a 15-min recovery period. RESULTS: The introduction of 29.0 (±11.5) mL/kg of air resulted in tension physiology. All three seals effectively evacuated air and blood. Hemodynamic compromise failed to develop with a chest seal in place. CONCLUSIONS: HyFin(®), SAM(®), and Sentinel(®) vented chest seals are equally effective in evacuating blood and air in a communicating pneumothorax model. All three prevented tension pneumothorax formation after penetrating thoracic trauma.


Asunto(s)
Ensayo de Materiales , Neumotórax/prevención & control , Animales , Presión Arterial , Modelos Animales de Enfermedad , Frecuencia Cardíaca , Apósitos Oclusivos , Neumotórax/fisiopatología , Estudios Prospectivos , Distribución Aleatoria , Porcinos , Toracostomía
16.
J Emerg Med ; 45(1): 78-85, 2013 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-23602144

RESUMEN

BACKGROUND: Principles of damage control resuscitation include minimizing intravenous fluid (IVF) administration while correcting perfusion pressure as quickly as possible. Recent studies have identified a potential advantage of vasopressin over catecholamines in traumatic shock. Terlipressin (TP) is a vasopressin analogue used to reverse certain shock etiologies in some European countries. STUDY OBJECTIVE: We evaluated three dosages of TP when combined with a limited colloid resuscitation strategy on mean arterial pressure (MAP) and lactatemia in a swine model of isolated hemorrhage. METHODS: Sixty anesthetized swine underwent intubation and severe hemorrhage. Subjects were randomized to one of four resuscitation groups: 4 mL/kg Hextend(®) (Hospira Inc, Lake Forest, IL) only, 3.75 µg/kg TP + Hextend, 7.5 µg/kg TP + Hextend, or 15 µg/kg TP + Hextend. MAP and heart rate were recorded every 5 min. Baseline and serial lactate values at 30-min intervals were recorded and compared. RESULTS: Subjects receiving 7.5 µg/kg TP had significantly higher MAPs at times t15 (p = 0.012), t20 (p = 0.004), t25 (p = 0.018), t30 (p = 0.032), t35 (p = 0.030), and t40 (p = 0.021). No statistically significant differences in lactate values between TP groups and controls were observed. CONCLUSION: Subjects receiving 7.5 µg/kg of TP demonstrated improved MAP within 10 min of administration. When combined with minimal IVF resuscitation, TP doses between 3.75 and 15 µg/kg do not elevate lactate levels in hemorrhaged swine.


Asunto(s)
Hemorragia/tratamiento farmacológico , Lipresina/análogos & derivados , Vasoconstrictores/administración & dosificación , Animales , Presión Arterial/efectos de los fármacos , Modelos Animales de Enfermedad , Fluidoterapia , Frecuencia Cardíaca/efectos de los fármacos , Hemorragia/terapia , Ácido Láctico/sangre , Lipresina/administración & dosificación , Porcinos , Terlipresina
17.
Univ. sci ; 16(2): 160-167, 2011. ilus, tab, graf
Artículo en Inglés | LILACS | ID: lil-619185

RESUMEN

Preparación simple de nuevas N-(6-metil-2-nitrofenil-1,2,3,4-tetrahidroquinolin-4-il) pirrolidin-2-onas y su análisis espectroscópico. Objetivos. Preparar nuevas moléculas N-(1,2,3,4-tetrahidroquinolin-4-il) 2-oxopirrolidínicas y caracterizarlas por métodos espectroscópicos. Materiales y métodos. Todos los reactivos usados son de Aldrich, grado comercial. La pureza de los productos y la composición de las mezclas de reacción fueron monitoreadas por cromatografía en capa fina sobre cromatoplacas de Silufol UV254 (0.25 mm). El aislamiento y purificación se realizó usando cromatografía en columna (SiO2), usando acetato de etilo. Resultados. La preparación de las nuevas N-(tetrahidroquinolin-4-il) pirrolidin-2-onas 4-nitrofenil (ó 2-nitrofenil) sustituidas en C-2 del anillo tetrahidroquinolínico, se realizóvía síntesis one-pot basada en la reacción de cicloadición imino Diels-Alder catalizada por BiCl3 entre toluidina, N-vinilpirrolidin-2-ona y 4-nitrobenzaldehído (3-nitrobenzaldehído). La estructura de los derivados pirrolidónicos fue confirmada por 1H RMN y 13C RMN, además de experimentos 2D RMN y difracción de rayos X de monocristal. Conclusiones. Una ruta eficiente, económica y rápida (reacción imino Diels-Alder multi-componente) fue empleada para la construcción de nuevas moléculas N-(tetrahidroquinolin-4-il) 2-oxopirrolidínicas, esqueleto muy atractivo y usado con estereoquímica bien definida...


Objectives. To prepare new N-(1,2,3,4-tetrahydroquinolin-4-yl) pyrrolidin-2-one molecules and to characterize them by spectroscopic methods. Materials and methods. All reagents were purchased from Aldrich, commercial grade. The purity of the products and the composition of the reaction mixtures were monitored by thin layer chromatography over Silufol UV254 chromatoplates (0.25 mm). Product isolation and purification were performed by column chromatography (SiO2) using ethyl acetate. Results. Preparation of new N-(2-nitrophenyl-1,2,3,4-tetrahydroquinolin-4-yl) pyrrolidin-2-ones has been achieved via the one-pot synthesis, based on a BiCl3-catalyzedimino Diels-Alder cycloaddition reaction of toluidine, N-vinylpyrrolidin-2-one and 4-nitro- or 3-nitrobenzaldehydes. The structure of the pyrrolidine derivatives was confirmed by 1H nmr and 13C nmr studies, in addition to inverse-detected 2D NMR experiments and monocrystal X-ray diffraction. Conclusions. An efficient, economic, and fast synthetic route (multi-component imino Diels-Alder reaction) was employed in the construction of several new tetrahydroquinoline derivatives, useful and attractive rigid skeleton with well-defined stereochemistry...


Preparação simples de novas N-(6-metil-2-nitrofenil-1,2,3,4-tetrahydroquinoline-4-il) pirrolidin-2-onas e sua análise espectroscópica. Objetivos. Preparar novas moléculas N-(1,2,3,4-tetrahydroquinoline-4-il) 2-oxopirrolidínicas e sua caracterização por espectroscopia. Materiais e métodos. Todos os reagentes utilizados são de Aldrich, de grau comercial. A pureza dos produtos e a composição das misturas de reação foram monitoradas por cromatografia em camada fina sobre cromatoplacas de Silufol UV254 (0,25 mm). O isolamento e purificação foi realizado utilizando cromatografia em coluna (SiO2), utilizando acetato de etila. Resultados. Preparação de novas N-(tetrahydroquinoline-4-il) pirrolidin-2-onas 4-nitrofenil (ou 2-nitrofenil) substituídas em C-2 do anel tetrahydroquinoline foi realizada através da síntese “one pot” baseada na reação de cicloadição imino Diels-Alder catalisada por BiCl3 entre toluidina, N-vinilpirrolidin-2-ona e 4 nitrobenzaldehyde (3 nitrobenzaldehyde). A estrutura dos derivados pirrolidónicos foi confirmada por 1H RMN y 13C RMN, experimentos 2D RMN, assim como difração de raios X e monocristais. Conclusões. Uma rota eficiente, econômica e rápida (reação imino Diels-Alder multi-componente) foi utilizada para a construção de novas moléculas N-(tetrahydroquinoline-4-il) 2-oxopirrolidínicas esqueleto muito atraente e usado com estereoquímica bem definida...


Asunto(s)
Composición de Medicamentos/clasificación , Composición de Medicamentos/métodos , Composición de Medicamentos
18.
Univ. sci ; 14(3): 216-224, sep.-dic. 2009. ilus, tab
Artículo en Español | LILACS-Express | LILACS | ID: lil-637330

RESUMEN

Objectives. To prepare new indolic molecules and characterize them by spectroscopic methods. Materials and methods: All reagents were purchased from Aldrich, commercial grade. The purity of the products and the composition of the reaction mixtures were monitored by thin layer chromatography over Silufol UV254 0.25 mm-thick chromatoplates. Product isolation and purification were performed by column chromatography (SiO2), using ethyl acetate-petroleum ether mixtures as eluents. Results. The synthesis of new N-aryl-N-(3-indolmethyl) acetamides based on first step iminization reaction of indol-3-carbaldehyde is accomplished. The structures of the C-3 substituted indoles were confirmed by ¹H-NMR and 13C-NMR studies supported by inverse-detected 2D NMR experiments and also through monocrystal X-ray diffraction. Conclusions. An efficient, economic, and fast synthetic route was designed to the construction of the N-aryl-N-(3-indolmethyl) acetamides, structural analogues of some alkaloids.


Objetivos: Preparar nuevas moléculas indólicas y caracterizarlas por los métodos espectroscópicos. Materiales y métodos. Todos los reactivos fueron adquiridos de Aldrich, de grado comercial. La pureza de los productos y composición de las mezclas de reacción fueron monitoreadas por la cromatografía en capa delgada, Silufol UV254 0.25 mm-grosor de cromatoplacas. El aislamiento y purificación de los productos fueron realizados por la cromatografía en columna (SiO2), usando mezclas de acetato de etilo y éter de petróleo como eluentes. Resultados. Se ha realizado la síntesis de nuevas N-aril-N-(3-indolmetil) acetamidas, basada en la reacción de iminización del indol-3-carbaldehído. Las estructuras de los indoles C-3 sustituidos fueron confirmadas por estudios de ¹H, 13C -RMN, experimentos de 2D RMN y también por difracción monocristal de Rayos X. Conclusiones. Se ha diseñado una nueva ruta de síntesis eficiente, económica y rápida para la construcción de las N-aril-N-(3-indolmetil) acetamidas, análogos estructurales de diversos alcaloides.


Objetivos. Preparar novas moléculas indólicas e caracterizar-las através de métodos espectroscópicos. Materiais e métodos. Todos os reagentes foram obtidos de Aldrich, de tipo comercial. A pureza dos produtos e a composição das misturas de reação foram monitoradas por cromatografia em camada fina, Silufol UV254 0,25 mm de espessura das cromatoplacas. O isolamento e a purificação dos produtos foram feitos através de cromatografia em coluna (SiO2), utilizando misturas de acetato de etila e éter de petróleo como eluente. Resultados. Realizou-se a síntese de novas N-aril-N-(3-indolmetil)acetamidas, baseada na reação de iminización do indol-3-carbaldeído. As estruturas dos indóis C-3 substituídos foram confirmadas por estudos de ¹H, 13C -RMN, experimentos de 2D RMN e também por difração monocristal dos Rayos X. Conclusões. Desenhou-se una nova rota de síntese eficiente, econômica e rápida para a construção das N-aril-N-(3-indolmetil) acetamidas, análogos estruturais de vários alcalóides.

19.
Acad Emerg Med ; 15(1): 74-81, 2008 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-18211317

RESUMEN

OBJECTIVES: Uncontrolled hemorrhage remains a leading cause of traumatic death. Several topical adjunct agents have been shown to be effective in controlling hemorrhage, and two, chitosan wafer dressing (HemCon [HC]) and zeolite powder dressing (QuikClot [QC]), are being utilized regularly on the battlefield. However, recent literature reviews have concluded that no ideal topical agent exists. The authors compared a new chitosan granule dressing (CELOX [CX]) to HC, QC and standard dressing in a lethal hemorrhagic groin injury. METHODS: A complex groin injury with transection of the femoral vessels and 3 minutes of uncontrolled hemorrhage was created in 48 swine. The animals were then randomized to four treatment groups (12 animals each). Group 1 included standard gauze dressing (SD); Group 2, CX; Group 3, HC; and Group 4, QC. Each agent was applied with 5 minutes of manual pressure followed by a standard field compression dressing. Hetastarch (500 mL) was infused over 30 minutes. Hemodynamic parameters were recorded over 180 minutes. Primary endpoints included rebleed and death. RESULTS: CX reduced rebleeding to 0% (p < 0.001), HC to 33% (95% CI = 19.7% to 46.3%, p = 0.038), and QC to 8% (95% CI = 3.3% to 15.7%, p = 0.001), compared to 83% (95% CI = 72.4% to 93.6%) for SD. CX improved survival to 100% compared to SD at 50% (95% CI = 35.9% to 64.2%, p = 0.018). Survival for HC (67%) (95% CI = 53.7% to 80.3%) and QC (92%; 95% CI = 84.3% to 99.7%) did not differ from SD. CONCLUSIONS: In this porcine model of uncontrolled hemorrhage, CX improved hemorrhage control and survival. CELOX is a viable alternative for the treatment of severe hemorrhage.


Asunto(s)
Vendajes , Hemorragia/tratamiento farmacológico , Hemostáticos/administración & dosificación , Animales , Presión Sanguínea , Temperatura Corporal , Quitosano/administración & dosificación , Modelos Animales de Enfermedad , Femenino , Ingle/lesiones , Hemorragia/etiología , Medicina Militar/instrumentación , Polvos , Distribución Aleatoria , Porcinos , Resultado del Tratamiento , Heridas y Lesiones/complicaciones , Zeolitas/administración & dosificación
20.
Acta Crystallogr C ; 63(Pt 4): o228-30, 2007 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-17413234

RESUMEN

The title compound, C(16)H(15)N(3), shows a hindrance effect between adjacent amino and methyl groups that leads to a structural distortion, which is reflected in the non-planarity of the quinoline entity and in the bond angles and distances. The crystal packing consists of chains along the b axis sustained by an intermolecular hydrogen bond between the amino group and the N atom of the pyridyl ring.


Asunto(s)
Aminas/química , Aminoquinolinas/química , Piridinas/química , Quinolinas/química , Conformación Molecular
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