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1.
Org Biomol Chem ; 2024 Apr 24.
Artigo em Inglês | MEDLINE | ID: mdl-38656328

RESUMO

Herein, we have showed the photophysical properties of favipiravir and its 6-substituted analogues. Also, we interpreted the origin of fluorescence of favipiravir and its 6-substituted analogues as a function of tautomerism modulation in ground and excited states. Favipiravir, the 6-fluorine derivative, showed the best photophysical profile, exhibiting a dominant emission wavelength of 430 nm, a high quantum yield (Q.Y.) of 1.0 and a long-lived state (10 ns). Its analogues also showed a maximum emission at 430 nm, but their Q.Y. values were 5-fold lower than that found for favipiravir, decreasing as a function of 6-substitution as follows: F > Cl > Br > I > H. Pyrazines bearing the least electronegative 6-substituent (X = Br, I, H) showed an extra lifetime, which was shorter (0.2-0.3 ns) and less abundant (>15%) than the main lifetime (10 ns, 85%). Further 2D excitation-emission matrix and solvent studies supported that these 3-hydroxy-2-pyrazinecarboxamides present two emissive states. The first of them (λem = 430 nm), which was the most abundant, most fluorescent and long-lived state, was characterized as "locally excited" (LE). Its fluorescence was favored with an increase of the hydrogen-donor nature of the solvent and for pyrazines having a high enolic characteristic. Thus, the high LE-fluorescence of these types of pyrazines depends on the keto-tautomerization of the ground state using a protic solvent and its feasible enol-tautomerization upon excitation. Finally, the second excited state (λem = 536 nm) was suggested as an excited-state intramolecular proton-transfer (ESIPT), and it was observed only, although discretely, for pyrazines bearing the least electronegative 6-substituent.

2.
Chemistry ; : e202400905, 2024 Mar 27.
Artigo em Inglês | MEDLINE | ID: mdl-38536766

RESUMO

Blue LEDs-irradiation of a mixture of N,N,N',N'-tetramethylethylenediamine (TMEDA) and perfluoroalkyl iodides (RF-I) - Electron Donor Acceptor (EDA)-complex - in the presence of triphenylamines (TPAs) in an aqueous solvent mixture afforded mono-perfluoroalkylated triphenylamines (RF-TPA) in good yields. These RF-TPA were further subjected to acetone-sensitized [6π]-electrocyclization at 315 nm-irradiation affording exclusively perfluoroalkylated endo-carbazole derivatives (RF-CBz) in quantitative yields. Mechanistic studies and photophysical properties of products are studied.

3.
Chemistry ; 30(8): e202303229, 2024 Feb 07.
Artigo em Inglês | MEDLINE | ID: mdl-38032158

RESUMO

Carbazole is a heterocyclic motif that can be found in a diverse array of natural and unnatural products displaying a wide range of biological and physiological properties. Furthermore, this heterocycle is part of electronic materials like photoconducting polymers and organic optoelectronic materials owing to its excellent photophysical characteristics. Consequently, the development of synthetic strategies for carbazole scaffolds holds potential significance in biological and material fields. In this regard, a variety of preparation methods has been developed to exploit their efficient and distinct formation of new C-C and C-heteroatom bonds under mild conditions and enabling broad substrate diversity and functional group tolerance. Therefore, this review focuses on the synthesis of a set of carbazole derivatives describing a variety of methodologies that involve direct irradiation, photosensitization, photoredox, electrochemical and thermal cyclization reactions.

4.
J Org Chem ; 88(7): 4405-4421, 2023 Apr 07.
Artigo em Inglês | MEDLINE | ID: mdl-36976299

RESUMO

The substituent and solvent effects on the spectroscopic behavior and on the photoinduced [6π]-electrocyclization reaction of substituted triphenylamine derivatives have been investigated. Direct irradiation of triphenylamines bearing electron-donor substituents in different solvents has provided for the first time the substituted exo/endo carbazole derivatives from modest to good yields, whereas triphenylamines bearing electron-withdrawing substituents did not provide the carbazoles due to the formation of charge transfer complexes (CTCs). A corollary of the experiments purports that the photoreaction is favored with weak electron-acceptor groups in polar solvents. The lowest-frequency absorption bands of the triarylamines (π,π* electronic transitions) displayed bathochromic shifts as the solvent polarity is increased. The fluorescence emission spectra of triarylamines bearing electron-donor substituents behave as mirror images of the lowest absorption bands, showing dependence on the solvent polarity. Conversely, triarylamines bearing formyl, acetyl, and nitro groups formed CTCs behaving as good fluorescence chromophores in polar solvents. Hammett correlations on the ΔE(0,0) energies of monosubstituted amines showed a bell-shape behavior where the ρ values depended on the solvent polarity. The physical quenching of the photoreaction of triarylamines has demonstrated for the first time that the triplet excited state is univocally the photoreactive state leading to exo/endo carbazole derivatives.

5.
J Stroke Cerebrovasc Dis ; 31(10): 106733, 2022 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-36030578

RESUMO

BACKGROUND: Stroke therapy has been transformed in recent years due to the availability of thrombolysis and mechanical thrombectomy (MT). Whether transferring the patient directly to a comprehensive stroke center (CSC, mothership model) is better than taking them to a primary stroke center (PSC) and then to a CSC for MT (drip and ship) is unclear but has important implications. We compared the performance of both models in a district of the Basque country, Spain. METHODS: This is a retrospective analysis of prospectively collected data of all acute ischemic stroke patients consecutively admitted to the Neurology Department of two institutions and eligible for MT over a 36-month period with anterior circulation large vessel occlusion (LVO). One center applied the mothership model and the other the drip-and-ship. The two models were compared in terms of mortality and functional status assessed by modified Rankin (mRS) scale at 90 days. As a surrogate of the effectiveness of the two models, all times pertinent to stroke therapy were recorded. RESULTS: A total of 187 patients were evaluated subjected to MT with the drip-and-ship model and 188 with mothership, with a median NIHSS of 15. Prior to MT, 17% of the drip-and-ship patients received thrombolysis and 26% in the mothership. Neither mortality rate nor mRS showed statistically significant differences 90 days after stroke. The time lapse from stroke to MT was optimal in both models; albeit being 10 minutes longer in the drip-and-ship model, it had no impact on patients' outcomes. CONCLUSIONS: Drip-and-ship and mothership models can provide optimal and similar results in acute stroke patients in terms of mortality and functional status at 90 days. Their coexistence may alleviate the burden of CSC thus facilitating the access of more stroke patients to advanced therapies in an equitable manner.


Assuntos
Isquemia Encefálica , AVC Isquêmico , Acidente Vascular Cerebral , Isquemia Encefálica/diagnóstico , Isquemia Encefálica/etiologia , Isquemia Encefálica/terapia , Humanos , Estudos Retrospectivos , Acidente Vascular Cerebral/diagnóstico , Acidente Vascular Cerebral/etiologia , Acidente Vascular Cerebral/terapia , Trombectomia , Terapia Trombolítica/efeitos adversos , Terapia Trombolítica/métodos , Resultado do Tratamento
6.
J Org Chem ; 87(20): 13439-13454, 2022 Oct 21.
Artigo em Inglês | MEDLINE | ID: mdl-35675160

RESUMO

Direct irradiation of mono-, di-, and trisubstituted triphenylamine derivatives in acetonitrile as solvent with light of 254 nm has been systematically investigated, revealing that the exo/endo carbazole derivatives were formed as the main photoproducts from modest to good yields for triphenylamines substituted with electron-donor and neutral substituents. The kinetic profiles of the photoreaction were also recorded, and the consumption rate constants (k) were measured. These kinetic parameters show dependence on the nature of the substituents, and linear Hammett correlations were carried out to showcase the substituent effect. On the other hand, the spectroscopic behavior of the electron-rich substituted triphenylamines has been analyzed, suggesting that the fluorescence emission spectra display a mirror image of the lower energy absorption bands, while for those amines bearing electron-acceptor groups the formation of charge-transfer complexes and their fluorescence emissions constitute the main deactivation pathway of the photoreaction.

7.
J Phys Chem B ; 125(32): 9268-9285, 2021 08 19.
Artigo em Inglês | MEDLINE | ID: mdl-34357778

RESUMO

Diverse models of intramolecular charge transfer (ICT) have been proposed for interpreting the origin of the charge-transfer (CT) state in donor-acceptor (D-A) dyes. However, a large variety of fused-heterocyclic dyes containing a pseudo-aromatic ring in the rigid structure have shown to be incompatible with them. To approximate a solution within the ICT concept, we reported a novel ICT model called partially aromatized intramolecular charge transfer (PAICT). PAICT involves the generation of a CT state from an ICT that occurred within a pre-excited D-A fused-heterocyclic structure possessing a pseudo-aromatic or unstable aromatic ring as the acceptor moiety. The model was proposed from the multiple-emissive mesomeric D-A N1-aryl-2-(trifluoromethyl)benzo[b][1,8]naphthyridin-4(1H)-one, whose excited mesomeric states, which are defined by the aromatic and pseudo-aromatic forms of the pyrindin-4(1H)-one ring, led to a common partial aromatized CT state upon excitation via PAICT. The latter was supported through theoretical calculations on the excited mesomeric states, one-dimensional (1D) and two-dimensional (2D) excitation-emission measurements in different solvents, and the detection of three excited states by lifetime measurements upon 370 nm excitation. The existence of mesomerism was supposed from: (i) two overlapping bands at 370-390 (or 400-420 nm) in UV-vis spectra, (ii) the direct interaction between the pyridinic nitrogen of one molecule and the carbonylic oxygen of the other found in the solid state and, (iii) the detection of three excited states by lifetime measurements. The PAICT opens new perspectives for interpreting the charge-transfer phenomenon in fused-heterocyclic dyes, in particular, those containing a pseudo-aromatic or unstable aromatic ring as an acceptor moiety.


Assuntos
Corantes/química , Solventes
8.
Medwave ; 21(5): e8210, 2021 Jun 25.
Artigo em Espanhol, Inglês | MEDLINE | ID: mdl-34214068

RESUMO

INTRODUCTION: Studies show a high prevalence of physical inactivity and sedentary behavior among university students. However, the relationship between physical activity and sedentary behavior in medical students is unknown. OBJECTIVES: To determine the prevalence of physical activity, sedentary behavior, and related factors among medical students at a public university. METHODS: We conducted an analytical cross-sectional study that included students from the first to the sixth year of medical school. We used the International Physical Activity Questionnaire (IPAQ). We analyzed study variables using Poisson regression, estimating crude and adjusted prevalence ratios. RESULTS: The final sample consisted of 513 students, of which 35% of women and 30.1% of all pre-clinical students had a low level of physical activity. Male sex and 20 to 24 age group were associated with a lower prevalence of low level of physical activity. Sedentary behavior was 60.9% among students under 20 years old and 55.5% among pre-clinical students. A lower prevalence of sedentary behavior was found in students over 25 years old, clinical students, and those with high levels of physical activity. CONCLUSION: Most medical students presented a moderate level of physical activity. We found a higher presence of low-level physical activity among females and pre-clinical students. We found that sedentary behavior was higher than reported in similar populations. The relationship between physical activity and lower sedentary behavior was significant only for students with a high-level physical activity.


INTRODUCCIÓN: Se ha reportado elevados porcentajes de inactividad física y sedentarismo en estudiantes universitarios. Sin embargo, el nivel de actividad física y su relación con el sedentarismo en estudiantes de medicina no es concluyente. OBJETIVOS: Determinar los niveles de actividad física y conducta sedentaria, así como factores relacionados a estas, en estudiantes de medicina humana de una universidad pública. MÉTODOS: Realizamos un estudio transversal analítico que incluyó a estudiantes de primer a sexto año académico de la carrera de medicina. Empleamos el cuestionario internacional de actividad física (IPAQ). Realizamos un análisis entre las variables de estudio mediante regresión de Poisson, que estimó razones de prevalencia crudas y ajustadas. RESULTADOS: La muestra fue de 513 estudiantes. Un 35% de mujeres y 30,1% de estudiantes de preclínica presentaron un nivel bajo de actividad física. El sexo masculino y el grupo de 20 a 24 años estuvieron asociados a una menor prevalencia de nivel bajo de actividad física. La conducta sedentaria fue 60,9% en el grupo menor de 20 años, y 55,5% entre estudiantes de preclínica. Los tres grupos en que se asoció una menor prevalencia de conducta sedentaria fueron el mayor a 25 años, los estudiantes de clínica, y los con nivel de actividad física alto. CONCLUSIONES: Los estudiantes de medicina presentaron principalmente un nivel moderado de actividad física. Hallamos una mayor presencia de actividad física baja entre estudiantes de sexo femenino y de preclínica. Encontramos un nivel de conducta sedentaria por encima de lo reportado en poblaciones similares. La relación entre nivel de actividad física y menor conducta sedentaria fue significativa solo para la categoría actividad física alta.


Assuntos
Exercício Físico , Comportamento Sedentário , Estudantes de Medicina/psicologia , Adulto , Estudos Transversais , Feminino , Humanos , Masculino , Peru/epidemiologia , Universidades , Adulto Jovem
10.
Neurol Sci ; 41(11): 3031-3038, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-32935157

RESUMO

BACKGROUND: COVID-19 disease affects the nervous system and led to an increase in neurological consults for patients at admission and through the period of hospitalization during the peak of the pandemic. METHODS: Patients with clinical and laboratory diagnosis of COVID-19 that required a neurologic consultation or those who presented with neurological problems on admission that led to a diagnosis of SARS-CoV-2 infection during a 2-month period at the peak of the pandemic were included in this study. Demographic and clinical variables were analyzed. RESULTS: Thirty-five patients were included. The presenting neurologic manifestations on admission led to the diagnosis of COVID-19 in 14 patients (40%). The most common reasons for consultation during the hospitalization period were stroke (11), encephalopathy (7), seizures (6), and neuropathies (5) followed by a miscellaneous of syncope (2), migraine (1), anosmia (1), critical illness myopathy (1), and exacerbation of residual dysarthria (1). The most common neurological disturbances were associated with severe disease except for neuropathies. Patients with encephalopathies and seizures had markedly increased D-dimer and ferritin values, even higher than stroke patients. RT-PCR was performed in 8 CSF samples and was negative in all of them. CONCLUSION: Neurological disturbances represent a significant and severe burden in COVID-19 patients, and they can be the presenting condition that leads to the diagnosis of the viral infection in a high percentage of patients. Evidence of direct viral mechanisms was scarce, but the pathogenesis of the diverse manifestations remains enigmatic.


Assuntos
Infecções por Coronavirus/complicações , Doenças do Sistema Nervoso/epidemiologia , Doenças do Sistema Nervoso/virologia , Pneumonia Viral/complicações , Adulto , Idoso , Idoso de 80 Anos ou mais , Betacoronavirus , Biomarcadores/sangue , Proteína C-Reativa/análise , COVID-19 , Infecções por Coronavirus/sangue , Estudos Transversais , Feminino , Ferritinas/sangue , Produtos de Degradação da Fibrina e do Fibrinogênio/análise , Hospitalização , Humanos , Incidência , Masculino , Pessoa de Meia-Idade , Doenças do Sistema Nervoso/sangue , Pandemias , Pneumonia Viral/sangue , Encaminhamento e Consulta , SARS-CoV-2 , Adulto Jovem
11.
ACS Omega ; 4(4): 6757-6768, 2019 Apr 30.
Artigo em Inglês | MEDLINE | ID: mdl-31459798

RESUMO

An efficient access toward novel tridentate ligands based on 1,7-dipyridinyl-substituted bis-pyrazolo[3,4-b:4',3'-e]pyridines (BPs) and their usefulness as fluorescent probes for cation detection is reported. The synthesis proceeds by a three-step sequence starting from 2-chloropyridine (1), all reactions were performed using microwave radiation under solvent-free conditions, and an overall yield of up to 63% was obtained. Photophysical properties of three representative 1,7-dipyridinyl-BPs (PBPs, 6a-6c) substituted at position 4 with different donor (D) or acceptor (A) groups were investigated. Compounds exhibited large Stokes shift in different solvents and strong blue light emission in both solution and solid state, and quantum yields were as high as 88% for some of them; thus, a twisted intramolecular charge transfer (TICT) fluorescence mechanism characteristic of the 1,4,7-triaryl-BPs was confirmed. The 4-phenyl-substituted probe (Ph-PBP, 6b) was used successfully in the detection of some metals (Cu2+, Co2+, Ni2+, and Hg2+) by fluorescence quenching phenomena, which could be reversed in the presence of ethylenediamine. This probe showed a greater sensitivity toward Cu2+ in concentrations as low as 26 nM, and in the process of "on-off-on" for this fluorescent molecular switch, only 1 equiv of the analyte was used.

12.
Sci Total Environ ; 671: 850-865, 2019 Jun 25.
Artigo em Inglês | MEDLINE | ID: mdl-30947056

RESUMO

Selenium is an essential micronutrient but at high concentrations can produce severe cytotoxicity and genomic damage. We have evaluated the cytotoxicity, ultrastructural and mitochondrial alterations of the two main selenium inorganic species; selenite and selenate, in the eukaryotic microorganism Tetrahymena thermophila. In this ciliate, selenite is more toxic than selenate. Their LC50 values were calculated as 27.65 µM for Se(IV) and 56.88 mM for Se(VI). Significant levels of peroxides/hydroperoxides are induced under low-moderate selenite or selenate concentrations. Se(VI) exposures induce an immediate mitochondrial membrane depolarization. Selenium treated cells show an intense vacuolization and some of them present numerous discrete and small electrondense particles, probably selenium deposits. Mitochondrial fusion, an intense swelling in peripheral mitochondria and mitophagy are detected in selenium treated cells, especially in those exposed to Se (IV). qRT-PCR analysis of diverse genes, encoding relevant antioxidant enzymes or other proteins, like metallothioneins, involved in an environmental general stress response, have shown that they may be crucial against Se(IV) and/or Se (VI) cytotoxicity.


Assuntos
Selênio/toxicidade , Tetrahymena thermophila/efeitos dos fármacos , Ácido Selênico/toxicidade , Ácido Selenioso/toxicidade , Tetrahymena thermophila/fisiologia , Testes de Toxicidade
13.
AIDS Res Ther ; 14(1): 60, 2017 Nov 13.
Artigo em Inglês | MEDLINE | ID: mdl-29132400

RESUMO

BACKGROUND: Antiretroviral therapy (ART) has modified the natural history of HIV-infection: the incidence of opportunistic infections (OIs) has decreased and mortality associated to HIV has improved dramatically. The reasons for hospitalization have changed; OIs are no longer the most common reason for admission. This study describes the patient population, admission diagnosis and hospital course of HIV patients in Colombia in the ART era. METHODS: Patients admitted with HIV/AIDS at six hospitals in Medellin, Colombia between August 1, 2014 and July 31, 2015 were included. Demographic, laboratory, and clinical data were prospectively collected. RESULTS: 551 HIV-infected patients were admitted: 76.0% were male, the median age was 37 (30-49). A new diagnosis of HIV was made in 22.0% of patients during the index admission. 56.0% of patients of the entire cohort had been diagnosed with HIV for more than 1 year and 68.9% were diagnosed in an advanced stage of the disease. More than 50.0% of patients had CD4 counts less than 200 CD4 cells/µL and viral loads greater than 100,000 copies. The main reasons for hospital admissions were OIs, tuberculosis, esophageal candidiasis and Toxoplasma encephalitis. The median hospital stay was 14 days (IQR 8-23). Admission to the intensive care unit (ICU) was required in 10.3% of patients and 14.3% were readmitted to the hospital; mortality was 5.4%. CONCLUSIONS: Similar to other countries in the developing world, in Colombia, the leading cause of hospitalization among HIV-infected patients remain opportunistic infections. However, in-hospital mortality was low, similar to those described for high-income countries. Strategies to monitor and optimize the adherence and retention in HIV programs are fundamental to maximize the benefit of ART.


Assuntos
Infecções Oportunistas Relacionadas com a AIDS/epidemiologia , Cuidados Críticos/estatística & dados numéricos , Infecções por HIV/epidemiologia , Hospitalização/estatística & dados numéricos , Tempo de Internação/estatística & dados numéricos , Adulto , Contagem de Linfócito CD4 , Colômbia/epidemiologia , Feminino , Infecções por HIV/diagnóstico , Infecções por HIV/tratamento farmacológico , Mortalidade Hospitalar , Humanos , Masculino , Pessoa de Meia-Idade , Carga Viral
14.
Ther Drug Monit ; 31(4): 436-42, 2009 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-19494792

RESUMO

There is evidence showing the importance of reaching immunosuppressant target concentrations as soon as possible. The aim of this study was to evaluate the relationship between tacrolimus trough concentrations within the first week after transplantation and the rate of acute rejection. In this descriptive-analytic study, we included 57 renal transplant patients receiving tacrolimus as the primary immunosuppressive drug. After univariate analysis, donor age, duration of hospital stay, and creatinine clearance (third month) showed significant differences between rejecters and nonrejecters. In addition, mean tacrolimus trough concentrations on day 5, day 7, mean of days 1-7, and mean of days 5-7 were found to be significantly lower in rejecters (P = 0.009, P = 0.012, P = 0.006, and P = 0.035, respectively). Receiver operating characteristic curve analysis with tacrolimus trough concentrations measured on days 5 and 7 was able to discriminate between patients with and without acute rejection (P = 0.028 and P = 0.048 after Bonferroni correction). The tacrolimus trough concentration with the best sensitivity-specificity balance was 9.3 ng/mL on day 5 and 8.7 ng/mL on day 7. In the Kaplan-Meier analysis, patients with tacrolimus trough concentrations below 9.3 mg/mL on day 5 showed a lower survival time without acute rejection (P = 0.048 after correction) in comparison with patients with tacrolimus trough concentrations above this concentration. After logistic regression, we obtained a model relating rejection with sex, donor age, and tacrolimus trough concentrations on day 5 (P = 0.004). No significant relationship between tacrolimus trough concentrations and delta creatinine clearance from week 1 to month 3 was obtained. These results confirm that tacrolimus trough concentrations during the first week are an important predictor of acute rejection. Therefore, it is critical to reach target blood concentrations of tacrolimus as soon as possible to improve allograft survival.


Assuntos
Rejeição de Enxerto , Tacrolimo/farmacologia , Rejeição de Enxerto/terapia , Humanos , Imunossupressores , Transplante de Rim , Complicações Pós-Operatórias , Tacrolimo/isolamento & purificação
15.
Retrovirology ; 6: 34, 2009 Apr 08.
Artigo em Inglês | MEDLINE | ID: mdl-19356241

RESUMO

BACKGROUND: Formation of an HIV-1 particle with a conical core structure is a prerequisite for the subsequent infectivity of the virus particle. We have previously described that glycineamide (G-NH2) when added to the culture medium of infected cells induces non-infectious HIV-1 particles with aberrant core structures. RESULTS: Here we demonstrate that it is not G-NH2 itself but a metabolite thereof that displays antiviral activity. We show that conversion of G-NH2 to its antiviral metabolite is catalyzed by an enzyme present in bovine and porcine but surprisingly not in human serum. Structure determination by NMR suggested that the active G-NH2 metabolite was alpha-hydroxy-glycineamide (alpha-HGA). Chemically synthesized alpha-HGA inhibited HIV-1 replication to the same degree as G-NH2, unlike a number of other synthesized analogues of G-NH2 which had no effect on HIV-1 replication. Comparisons by capillary electrophoresis and HPLC of the metabolite with the chemically synthesized alpha-HGA further confirmed that the antiviral G-NH2-metabolite indeed was alpha-HGA. CONCLUSION: alpha-HGA has an unusually simple structure and a novel mechanism of antiviral action. Thus, alpha-HGA could be a lead for new antiviral substances belonging to a new class of anti-HIV drugs, i.e. capsid assembly inhibitors.


Assuntos
Fármacos Anti-HIV , Capsídeo/efeitos dos fármacos , Glicina/análogos & derivados , HIV-1/efeitos dos fármacos , Soro/química , Animais , Fármacos Anti-HIV/química , Fármacos Anti-HIV/isolamento & purificação , Fármacos Anti-HIV/metabolismo , Fármacos Anti-HIV/farmacologia , Capsídeo/química , Capsídeo/metabolismo , Proteínas do Capsídeo/metabolismo , Bovinos , Linhagem Celular , Glicina/química , Glicina/isolamento & purificação , Glicina/metabolismo , Glicina/farmacologia , HIV-1/fisiologia , Humanos , Soro/metabolismo , Relação Estrutura-Atividade , Suínos , Vírion/metabolismo , Replicação Viral/efeitos dos fármacos
16.
Org Biomol Chem ; 1(19): 3396-403, 2003 Oct 07.
Artigo em Inglês | MEDLINE | ID: mdl-14584803

RESUMO

Treatment of N-(carboxymethyl)-anthranilic acids 1 with several dehydrating agents, gave the cyclic ortho amides 6, or the 7-membered anhydrides 7. After reaction of N-(carboxymethyl)-anthranilic acid (1a) with acetic anhydride, a diacetylated fused diketopiperazine indole dimer (18) could be isolated. Dehydrations of 2,2'-iminobis-benzoic acid led to the corresponding cyclic ortho amides 23. The dynamic behaviour of some of these compounds, and their precursors, was studied.

17.
J Org Chem ; 67(22): 7833-8, 2002 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-12398510

RESUMO

Nitration of some 2-substituted pyrimidine-4,6-diones in sulfuric acid was studied, which afforded previously unknown 5,5-gem-dinitropyrimidine-4,6-diones in high yields. The gem-dinitro products were easily attacked by nucleophiles with concomitant formation of gem-dinitroacetyl derivatives, which in turn could be further hydrolyzed to salts of dinitromethane and triureas.


Assuntos
Nitratos/química , Pirimidinas/química , Pirimidinas/síntese química , Cristalografia por Raios X , Espectroscopia de Ressonância Magnética , Conformação Molecular , Estrutura Molecular , Temperatura , Ureia/química
19.
Psicoactiva ; (18): 45-68, ene.-dic. 2000. tab, graf
Artigo em Espanhol | LILACS, LIPECS | ID: lil-281234

RESUMO

La microcomercialización de drogas ilegales es un problema multifactorial, de proporciones crecientes y en el cual la participación de la mujer va incrementándose en los últimos años. Se realizó un estudio de corte transversal en el último trimestre de 1998, empleando una muestra no probabilística por conveniencia, mediante la aplicación de una encuesta a 173 mujeres internadas por tráfico ilícito de drogas (TID) en el Penal de Santa Mónica (Chorrillos, Lima). Los datos integrados en una base de datos fue analizada con el programa SPSS for Windows v. 10.0. Las conclusiones del estudio fueron que el perfil de la mujer microcomercializadora de drogas en Lima que ingresa al penal por TID, usualmente tiene relación conyugal y uno o más hijos, algún grado de estudios secundarios o primaria completa, vende sola y es detenida durante el microcomercio en su casa o en la calle. Solo una pequeña proporción de mujeres jóvenes (menores de 25 años) se dedican al tráfico internacional (burriers)


Assuntos
Humanos , Feminino , Mulheres , Drogas Ilícitas , Peru
20.
Arq. bras. cardiol ; 65(4): 327-330, Out. 1995.
Artigo em Português | LILACS | ID: lil-319317

RESUMO

PURPOSE: To analyze clinical and surgical aspects of patients with anomalous left pulmonary venous drainage (ALPVD). METHODS: Seven patients, 3 males, with ages ranging from 18 months to 29 years were retrospectively studied, by analyzing the symptoms, electrocardiograms, chest X-ray, echocardiograms, angiography and surgical technique. RESULTS: All patients, but one, were symptomatic being the effort dyspnea the most prevalent symptom. Electrocardiogram showed incomplete right bundle branch block in all but one case. Chest X-ray showed prominent pulmonic vessels (6 patients), different degrees of cardiomegaly (6) and a left superior vena cava like image (3). Echocardiography correctly depicted the anomaly in 4 cases. The ALPVD was lobar in 4 cases and total in 3. In 3 patients there was pulmonary hypertension and in one venous drainage obstruction (8mmHg gradient). Six patients were operated on, 3 through a sternotomy approach with cardiopulmonary bypass and other 3 through a left thoracotomy without cardiopulmonary bypass. CONCLUSION: ALPVD has varying clinical repercussion and its clinical picture resembles atrial septal defect. Some cases may present diagnostic difficulties and echocardiograms may result in false negative findings. Cardiac catheterization is important to obtain detailed anatomic diagnosis, to evaluate the degree of pulmonary hypertension and to rule out venous obstruction. Left thoracotomy without extracorporeal circulation is indicated in ALPVD without associated defects.


Objetivo -Analisar aspectos clínicos e cirúrgicos de portadores de drenagem anômala de veias pulmonares esquerdas (DAVPE). Métodos - Estudaram-se, retrospectivamente, 7portadores de DAVPE, sendo 3 do sexo masculino, com idades variando de 18 meses a 29 anos, analisando-se as variáveis: sintomas, padrão eletrocardiográfico, achados radiológicos, ecocardiográficos, angiográficos e técnicas operatórias. Resultados - Todos os pacientes, exceto um, eram sintomáticos sendo a queixa predominante dispnéia aos esforços. Seis apresentavam bloqueio incompleto do ramo direito. Os achados radiológicos encontrados foram: aumento da trama vascularpulmonar (6 casos), cardiomegalia (6) e imagem tipo "cova esquerda" (3). 0 ecocardiograma demonstrou corretamente a anomalia em 4 casos. No estudo hemodinâmico a drenagem anômala era restrita ao lobo superior em 4 casos e em 3 envolvia todo o pulmão esquerdo. Em 3 havia hipertensão arterial pulmonar e em 1, foi observada obstrução da drenagem venosa com gradiente pressórico de 8mmHg. Seis pacientes foram operados até o momento, sem complicações, 3, através de esternotomia e utilização de circulação extracorpórea (CEC) para correção de defeitos associados, e 3, através de toracotomia lateral esquerda sem emprego de CEC. Conclusão -DAVPE tem repercussão clínica variáveL assemelhando-se em seu quadro clínico, achados eletrocardiográficos e radiológicos com comunicação interatrial. Alguns casos podem trazer dificuldades diagnósticas e a avaliação ecocardiográfica pode resultar em diagnósticos falso negativos. O estudo hemodinâmico é importante para diagnóstico anatômico, avaliação do grau de repercussão no território pulmonar e para descartar obstrução à drenagem venosa. Toracotomia lateral esquerda sem CEC está indicada para os casos deDAVPE sem defeitos associados


Assuntos
Humanos , Masculino , Feminino , Lactente , Pré-Escolar , Criança , Adolescente , Adulto , Veias Pulmonares , Ecocardiografia , Estudos Retrospectivos , Eletrocardiografia , Hemodinâmica
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