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The compound diethyl 2,2'-(thiocarbonyl-bis(sulfanediyl))-diacetate 4 belongs to the trithiocarbonate class containing a trithiocarbonate function group flanked by ethyl acetate. In this procedure, a novel economic synthesis route to obtain compound 4 is described. This compound proved to possess broad-spectrum antimicrobial activity both in vitro and in vivo, and could be used as a lead compound. It is worth mentioning that this compound has been patented [No. US 9,988,348 B1; date of patent: June 5, 2018].
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Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Bacterias/efectos de los fármacos , Hongos/efectos de los fármacos , Tionas/química , Animales , Masculino , Ratones , Pruebas de Sensibilidad MicrobianaRESUMEN
The synthesis of the tetracyclic compounds 1-(4,5-dichloro-9,10-dihydro-9,10-ethanoanthracen-11-yl)-N-methylmethanamine (5) and 1-(1,8-dichloro-9,10-dihydro-9,10-ethanoanthracen-11-yl)-N-methylmethanamine (6) as a homologue of the anxiolytic and antidepressant drugs benzoctamine and maprotiline were described. The key intermediate aldehydes (3) and (4) were successfully synthesized via a [4 + 2] cycloaddition between acrolein and 1,8-dichloroanthracene. The synthesized compounds were investigated for antidepressant activity using the forced swimming test. Compounds (5), (6) and (3) showed significant reduction in the mice immobility indicating significant antidepressant effects. These compounds significantly reduced the immobility times at a dose 80 mg/kg by 84.0%, 86.7% and 71.1% respectively.
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Antracenos/síntesis química , Ansiolíticos/síntesis química , Antidepresivos/síntesis química , Hidrocarburos Clorados/síntesis química , Animales , Antracenos/química , Antracenos/farmacología , Ansiolíticos/química , Ansiolíticos/farmacología , Antidepresivos/química , Antidepresivos/farmacología , Hidrocarburos Clorados/química , Hidrocarburos Clorados/farmacología , Pérdida de Tono Postural/efectos de los fármacos , Maprotilina/química , Maprotilina/farmacología , Ratones , Estructura Molecular , NataciónRESUMEN
A theoretical study of the regioselectivity of the Diels-Alder reaction between 1,8-dichloroanthracene and acrolein is performed using DFT at the B3LYP/6-31G(d,p) level of theory. The FMO analysis, global and local reactivity indices confirmed the reported experimental results. Potential energy surface analysis showed that the cycloadditions (CAs) favor the formation of the anti product. These results are in good agreement with the reported results obtained experimentally where the anti is the major product.
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Acroleína/química , Antracenos/química , Modelos Químicos , Reacción de Cicloadición , EstereoisomerismoRESUMEN
A series of hitherto unreported anthracene-embedded dispirooxindoles has been synthesized via a one-pot three-component 1,3-dipolar cycloaddition reaction of an azomethine ylide, generated in situ from the reaction of isatin and sarcosine to 10-benzylideneanthracen-9(10H)-one as a dipolarophile in 1-butyl-3-methylimidazolium bromide([bmim]Br), an ionic liquid. This reaction proceeded regio- and diastereoselectively, in good to excellent yields.
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Antracenos/síntesis química , Indoles/síntesis química , Antracenos/química , Reacción de Cicloadición , Humanos , Indoles/química , Modelos Moleculares , Estructura MolecularRESUMEN
Objectives: Workplace safety is essential to occupational health practices among healthcare providers, especially for nurses vulnerable to work-related hazards such as needle stick and sharp injuries. In Yemen, the underestimation and absence of reporting system and lack of health supplies in a collapsed health system exacerbated the needle stick and sharp injuries. This study aimed to identify the prevalence and associated factors of needle stick and sharp injuries among nurses in Taiz, Yemen. Methods: A cross-sectional study was conducted on a sample of 151 nurses working in three public hospitals in Taiz City. A semi-structured questionnaire was designed and delivered to the participants. Results: The prevalence of needle stick and sharp injuries among nurses was very high (95.36%), and around half were injured more than five times. Female nurses and those in an emergency department were more likely to be subjected to needle stick and sharp injuries (p = 0.018 and 0.021, respectively). Needle stick was the most common cause of injury (62.77%), and the fingers were the most exposed injury site (79.17%). Non-reporting injuries were very high (73.61%), and only one-third (34.21%) of them proceeded in the process of management, and less than one-quarter (23.68%) had been vaccinated. Conclusion: The prevalence of needle stick and sharp injuries among nurses in Taiz was very high, and determined by gender and place of work. Post-injury reporting and precautions were poor, which may increase the prevalence of hospital-acquired infections among clients and healthcare providers.
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Objective. This study aims to highlight the low birth weight (LBW) in Taiz City (Yemen), as LBW is one of the public health challenges experiencing a profound effect on newborns. Methods. This was a cross-sectional study since the interview and medical records were the sources of data to be analyzed by SPSS. Results. The findings of this study include; a high prevalence of LBW (39.11%), the maternal age was not associated with LBW (P = .68), and education level, economic status, residence place, and health status were not associated with LBW (P < .05). Although the pre-pregnancy BMI, during-pregnancy BMI, MUAC, and gestational age were significantly associated with LBW (P < .05), the only risk factor was gestational age (OR = 9.606, CI = 3.988-23.135, P = .00). Conclusion. LBW is highly prevalent in Taiz (Yemen), so providing good healthcare services is essential to manage LBW incidence.
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Background and Objective: Despite that inherited (thalassemia and SCA) and infectious (hepatitis B, hepatitis C and AIDs) diseases and their risk factor consanguineous marriage are widespread among Yemen population, community-based awareness studies towards premarital screening (PMS) is extremely limited, so our study is designed to elicit knowledge and attitude of engaged and recently married couples in Taiz (Yemen) toward PMS. Methods: A cross-sectional study was conducted from April to September 2021 at Taiz. A well-structured questionnaire was designed and then delivered to participants to collect data. Results: The results revealed that majority of respondents (83.60%-94.18%) had knowledge about inherited and infectious diseases, respectively, and educational institution was the main knowledge source. Females had significantly higher knowledge than males (P ≤ .01), except about AIDs since no difference (P = .539). The results also revealed that majority of respondents had positive attitudes toward PMS, except toward AIDs testing since 70% of males and 68.91% of females had negative attitudes. The majority of respondents agreed that screening reduces the diseases incidence. Approximately half of respondents (50.79%-56.61%) tend to go ahead for marriage in case of positive results for inherited and infectious diseases respectively. Making PMS as an obligatory step prior engagement was agreed by 47.62% of respondents (45.71% of males, 48.74% of females). Conclusion: A high level of knowledge and positive attitudes toward inherited and infectious diseases and PMS were reported. This knowledge reflected on the agreement of majority of respondents regarding PMS importance in term of reduction of diseases incidence.
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Síndrome de Inmunodeficiencia Adquirida , Estudios Transversales , Femenino , Conocimientos, Actitudes y Práctica en Salud , Humanos , Masculino , Tamizaje Masivo , Encuestas y CuestionariosRESUMEN
Phytochemical studies on the alkaloids fraction of the entire plant of Isatis minima Bunge resulted in the alkaloids 1-4 isolation, which were first time isolated from this species. The 1D and 2D NMR spectroscopic data were used to identify their structures, and there was satisfactory compatibility of the data compared to those which were previously published. In the examined compounds 1-4, Isaindigotidione (3) and Isaindigotone (4) were shown as an effective urease inhibitor in such a concentration-dependent way against Jack bean and Bacillus pasteurii urease, with IC50 values 29.03 ± 0.04, 20.04 ± 0.09 and 34.03 ± 0.07, 26.13 ± 0.08 µM, respectively. Compounds 3 and 4 were likewise shown to be an effective inhibitor against α-chymotrypsin, exhibiting IC50 values 16.09 ± 0.07 and 22.01 ± 0.06 µM, correspondingly. The program MOE-Dock was used to perform a molecular docking analysis to confirm probable binding modes of the active complexes of the isolated compounds 1-4 and the crystal structure of urease and α-chymotrypsin enzymes. Compound 3 was the most active, having the highest docking scores against Bacillus pasteurii urease, α-chymotrypsin, and Jack bean (-8.6876), (-7.6647), and (-13.1927) µM, respectively. All four alkaloids (1-4) showed significant urease and protease inhibitory potential and further these activities were confirmed with the help of molecular docking study.
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Medical imaging is the process of visual representation of different tissues and organs of the human body to monitor the normal and abnormal anatomy and physiology of the body. There are many medical imaging techniques used for this purpose such as X-ray, computed tomography (CT), positron emission tomography (PET), magnetic resonance imaging (MRI), single-photon emission computed tomography (SPECT), digital mammography, and diagnostic sonography. These advanced medical imaging techniques have many applications in the diagnosis of myocardial diseases, cancer of different tissues, neurological disorders, congenital heart disease, abdominal illnesses, complex bone fractures, and other serious medical conditions. There are benefits as well as some risks to every imaging technique. There are some steps for minimizing the radiation exposure risks from imaging techniques. Advance medical imaging modalities such as PET/CT hybrid, three-dimensional ultrasound computed tomography (3D USCT), and simultaneous PET/MRI give high resolution, better reliability, and safety to diagnose, treat, and manage complex patient abnormalities. These techniques ensure the production of new accurate imaging tools with improving resolution, sensitivity, and specificity. In the future, with mounting innovations and advancements in technology systems, the medical diagnostic field will become a field of regular measurement of various complex diseases and will provide healthcare solutions.